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ALKALOIDSALKALOIDS
K.Sudheer Kumar,
Assistant professor.
Dept.of Pharmacognosy
Chilkur Balaji college of Pharmacy
Hyderabad.
E-mail:sudheer.y2k8@gmail.com
Plants have been one of the important sources of medicines since the
beginning of human civilization. There is a growing demand for plant based
medicines, health products, pharmaceuticals, food supplements and
cosmetics.
According to the WHO survey 80% populations living in the developing
countries rely almost exclusively on traditional medicine for their primary
health care needs.
In addition, herbs have provided us some of the very important life saving
drugs used in the modern medicine. However among the estimated 2,50,000-
4,00,000 plant species, only 6% have been studied for biological activity and
about 15% have been investigated phytochemically.
INTRODUCTION
Plants have been one of the important sources of medicines since the
beginning of human civilization. There is a growing demand for plant based
medicines, health products, pharmaceuticals, food supplements and
cosmetics.
According to the WHO survey 80% populations living in the developing
countries rely almost exclusively on traditional medicine for their primary
health care needs.
In addition, herbs have provided us some of the very important life saving
drugs used in the modern medicine. However among the estimated 2,50,000-
4,00,000 plant species, only 6% have been studied for biological activity and
about 15% have been investigated phytochemically.
The term “alkaloid” (alkali-like) is commonly used to designate basic
heterocyclic nitrogenous compounds of plant origin that are physiologically
active. The name “alkaloid” comes from the Arabic word for ash
“al- qali”.
DEFINATION
HISTORY
most notorious poisons in the history of civilization.
Used by humanity for thousands of years. The first civilizations to use
them were probably the ancient Sumerians and Egyptians.it was called a
vegetable alkali.
HISTORY
most notorious poisons in the history of civilization.
Used by humanity for thousands of years. The first civilizations to use
them were probably the ancient Sumerians and Egyptians.it was called a
vegetable alkali.
Term alkaloid was coined by Meissner ,a German pharmacist (1819).
Derosne (French chemist) isolated Narcotine (1803).
Serturner (1803) isolated morphine from opium
“Basic nitrogenous compound, contains one or more nitrogen in heterocyclic
ring system having marked physiological action on human and animals
when use in small quantities””.”
OR
Naturally occurring nitrogenous substance which is isolated from plants
and reacts like bases”
FACTS ABOUT MANDRAKE
• Already used in Egypt 3500 years ago.
• Grecian times considered as an extremely
powerful aphrodisiac and fertility enhancer.
• Mentioned in the Koran, and strictly
forbidden.
• The sponge that was given to Jesus on the
cross is said to contain Mandragora juice.
• played a major role in witchcraft.
• Witches prepared mixtures of extracts of
henbane (Hyoscyamus niger), deadly
nightshade (Atropa belladonna) and
mandrake root, to be applied on the skin or
on the genitals.
Mandrake, also named Mandragora
(Mandragora officinarum) Most magic
plant.
FACTS ABOUT MANDRAKE
• Already used in Egypt 3500 years ago.
• Grecian times considered as an extremely
powerful aphrodisiac and fertility enhancer.
• Mentioned in the Koran, and strictly
forbidden.
• The sponge that was given to Jesus on the
cross is said to contain Mandragora juice.
• played a major role in witchcraft.
• Witches prepared mixtures of extracts of
henbane (Hyoscyamus niger), deadly
nightshade (Atropa belladonna) and
mandrake root, to be applied on the skin or
on the genitals.
The alkaloids represent a very extensive group of secondary metabolites, with
diverse structures, distribution in nature, and important biological activities.
‘‘An alkaloid is a cyclic compound containing nitrogen in a negative oxidation
state which is of limited distribution in living organisms’’.
This definition includes both alkaloids with nitrogen as part of a heterocyclic
system and many exceptions with exocyclic nitrogen, such as colchicines or
capsaicin.
Generally, the function of secondary metabolites in plants is not determined.
Concerning the alkaloids, their protective mechanism against herbivore animals and
possibly some parasites is assumed. In contrast, these plants can become the targets
for insects that specialize in the alkaloid-producing plants (e.g., bark tree).However,
strong physiological effects and the selectivity of some alkaloids present
opportunities for utilizing the alkaloids in human medicine.
The alkaloids represent a very extensive group of secondary metabolites, with
diverse structures, distribution in nature, and important biological activities.
‘‘An alkaloid is a cyclic compound containing nitrogen in a negative oxidation
state which is of limited distribution in living organisms’’.
This definition includes both alkaloids with nitrogen as part of a heterocyclic
system and many exceptions with exocyclic nitrogen, such as colchicines or
capsaicin.
Generally, the function of secondary metabolites in plants is not determined.
Concerning the alkaloids, their protective mechanism against herbivore animals and
possibly some parasites is assumed. In contrast, these plants can become the targets
for insects that specialize in the alkaloid-producing plants (e.g., bark tree).However,
strong physiological effects and the selectivity of some alkaloids present
opportunities for utilizing the alkaloids in human medicine.
ALKALOID DESCRIPTION
• Contains nitrogen -usually derived from an amino acid.
• Bitter tasting, generally white solids (exception -nicotine is a brown
liquid).
• They give a precipitate with heavy metal iodides.
• Caffeine, a purine derivative, does not precipitate like most alkaloids.
• Alkaloids are basic -they form water soluble salts. Most alkaloids are
well-defined crystalline substances which unite with acids to form salts.
In plants, they may exist
• In the free state.
ALKALOID DESCRIPTION
• Contains nitrogen -usually derived from an amino acid.
• Bitter tasting, generally white solids (exception -nicotine is a brown
liquid).
• They give a precipitate with heavy metal iodides.
• Caffeine, a purine derivative, does not precipitate like most alkaloids.
• Alkaloids are basic -they form water soluble salts. Most alkaloids are
well-defined crystalline substances which unite with acids to form salts.
In plants, they may exist
• In the free state.
TESTS FOR ALKALOIDS
• Most alkaloids are precipitated from neutral or slightly acidic
solution by
• Dragendorff's reagent (solution of potassium bismuth
iodide)orange coloured precipitate.
• Mayer's reagent (potassium mercuric iodide solution) Cream
coloured precipitate.
• Wagner’s reagent (iodine in potassium iodide) red-brown
precipitate
• Hager's reagent (picric acid) yellow precipitate.
TESTS FOR ALKALOIDS
• Most alkaloids are precipitated from neutral or slightly acidic
solution by
• Dragendorff's reagent (solution of potassium bismuth
iodide)orange coloured precipitate.
• Mayer's reagent (potassium mercuric iodide solution) Cream
coloured precipitate.
• Wagner’s reagent (iodine in potassium iodide) red-brown
precipitate
• Hager's reagent (picric acid) yellow precipitate.
PHYSICO-CHEMICAL PROPERTIES OF ALKALOIDS
• Molecular weight: 100 –900
• Most bases which do not contain O2 are liquid at room temperature
(nicotine), while those that do are solids. In rare cases they are coloured.
• Most solid bases rotate the plane of polarized light, have high melting points.
• Normally are not soluble in water (occasionally slightly soluble).
• Soluble in a polar or slightly polar organic solvents. Soluble in concentrated
hydro alcoholic solutions.
• Naturally occurring chemical compounds containing basic nitrogen atoms
• Physiologically active
• Insoluble or sparingly soluble in water
• Crystalline solids; a few are amorphous
PHYSICO-CHEMICAL PROPERTIES OF ALKALOIDS
• Molecular weight: 100 –900
• Most bases which do not contain O2 are liquid at room temperature
(nicotine), while those that do are solids. In rare cases they are coloured.
• Most solid bases rotate the plane of polarized light, have high melting points.
• Normally are not soluble in water (occasionally slightly soluble).
• Soluble in a polar or slightly polar organic solvents. Soluble in concentrated
hydro alcoholic solutions.
• Naturally occurring chemical compounds containing basic nitrogen atoms
• Physiologically active
• Insoluble or sparingly soluble in water
• Crystalline solids; a few are amorphous
PHYSICAL PROPERTIES
a).Most alkaloids are crystalline solid , some are Volatile; --Nicotine ,
Non-Volatile:- Pilocarpine , Hyoscine
b).Majority of alkaloids are colorless but some are colored,
e.g.,Colchicine and Berberine are Yellow.Canadine is Orange.
c). SOLUBILITY :-difference in solubility used as a base for their isolation
and purification from non- alkaloidal bases.
The following can be mentioned :-
i).Both alkaloidal base and there salts are soluble in alcohol.
ii).Genarally bases are soluble in organic solvent and alkaloidal salts are
soluble in water.
PHYSICAL PROPERTIES
a).Most alkaloids are crystalline solid , some are Volatile; --Nicotine ,
Non-Volatile:- Pilocarpine , Hyoscine
b).Majority of alkaloids are colorless but some are colored,
e.g.,Colchicine and Berberine are Yellow.Canadine is Orange.
c). SOLUBILITY :-difference in solubility used as a base for their isolation
and purification from non- alkaloidal bases.
The following can be mentioned :-
i).Both alkaloidal base and there salts are soluble in alcohol.
ii).Genarally bases are soluble in organic solvent and alkaloidal salts are
soluble in water.
1).Salt formation
Due to their basic character alkaloid reacts with acid to form salt.
Strong bases form salt with very weak acid.
Weak bases forms salt with strong acid
Very weak bases form unstable salts. e.g caffeine , Narcotine , piperine.
2).Effect of heat:-Alkaloids are decomposed by heat, except Strychnine and
caffeine (sublimable).
3).Effect of light and Oxygen :
 Decomposed when allowed to stand at a temperature above 70o C .for long time.
 Decomposition occur rapidly and easily when an alkaloid is in solution than
when it is in dry form.
CHEMICAL PROPERTIES
1).Salt formation
Due to their basic character alkaloid reacts with acid to form salt.
Strong bases form salt with very weak acid.
Weak bases forms salt with strong acid
Very weak bases form unstable salts. e.g caffeine , Narcotine , piperine.
2).Effect of heat:-Alkaloids are decomposed by heat, except Strychnine and
caffeine (sublimable).
3).Effect of light and Oxygen :
 Decomposed when allowed to stand at a temperature above 70o C .for long time.
 Decomposition occur rapidly and easily when an alkaloid is in solution than
when it is in dry form.
Functions:
1. Poisonous agents protecting the plant against insects and herbivores
2. End products of detoxification reactions representing a metabolic
locking up of compounds otherwise harmful to the plant
3. Regulatory growth factors
4. Reserve substances capable of supplying nitrogen or other elements
necessary to the plants economy.
Functions:
1. Poisonous agents protecting the plant against insects and herbivores
2. End products of detoxification reactions representing a metabolic
locking up of compounds otherwise harmful to the plant
3. Regulatory growth factors
4. Reserve substances capable of supplying nitrogen or other elements
necessary to the plants economy.
• Forms of Alkaloids:
• Free bases
• Salts with Organic acids e.g. Oxalic, acetic acids
• Salts with inorganic acids e.g. Hcl, H2SO4.
• Salts with special acids: e.g. Meconic acid in Opium, Quinic acid in Cinchona
• Glycosidal form e.g. Solanine in Solanum
Distribution in Plant:
All Parts e.g. Datura.
Barks e.g. Cinchona
Seeds e.g. Nux vomica
Roots e.g. Aconite
Fruits e.g. Black pepper
Leaves e.g. Vinca
Latex e.g. Opium
OTHER SOURCES
Castoramine :--- from Canadian beaver (The
Canadian beaver is the largest rodent in North
America).
• Forms of Alkaloids:
• Free bases
• Salts with Organic acids e.g. Oxalic, acetic acids
• Salts with inorganic acids e.g. Hcl, H2SO4.
• Salts with special acids: e.g. Meconic acid in Opium, Quinic acid in Cinchona
• Glycosidal form e.g. Solanine in Solanum
Distribution in Plant:
All Parts e.g. Datura.
Barks e.g. Cinchona
Seeds e.g. Nux vomica
Roots e.g. Aconite
Fruits e.g. Black pepper
Leaves e.g. Vinca
Latex e.g. Opium
OTHER SOURCES
Castoramine :--- from Canadian beaver (The
Canadian beaver is the largest rodent in North
America).
Pyocyanine :-- from
Pseudomonas aeruginosa
(a bacteria).
Muscopyridine :--From
Musk of an Deer.
OCCURANCE and DISTRIBUTION
a).Ranunculaceae : Aconitine (aconite).
b). Legumioceae : Physostigmine (physostigma)
c).Loganiaceae : Strychnine and Brucine (Nux-vomica).
d).Papavaraceae : Morphine, Codeine,Thebaine (Opium).
e).Solanaceae : Hyoscine (Belladona).
f).Berberidaceae ; Berberine (Berberis).
g).Rubiaceae : Quinine and Quinidine (Cinchona).
h). Apocyanaceae : Reserpine (Rauwolfia) ,Vincristine and Vinblastine (Vinca).
i). Liliaceae : Veriterine (Veratrum).
j).Clavicipitaceae : Ergotamine and Ergometrine (Ergot).
OCCURANCE and DISTRIBUTION
a).Ranunculaceae : Aconitine (aconite).
b). Legumioceae : Physostigmine (physostigma)
c).Loganiaceae : Strychnine and Brucine (Nux-vomica).
d).Papavaraceae : Morphine, Codeine,Thebaine (Opium).
e).Solanaceae : Hyoscine (Belladona).
f).Berberidaceae ; Berberine (Berberis).
g).Rubiaceae : Quinine and Quinidine (Cinchona).
h). Apocyanaceae : Reserpine (Rauwolfia) ,Vincristine and Vinblastine (Vinca).
i). Liliaceae : Veriterine (Veratrum).
j).Clavicipitaceae : Ergotamine and Ergometrine (Ergot).
Any method will be a good technique, if it will accelerate:
1.Wetting of the surface of the herb particles.
2. Permeability of cell walls.
3. Rate of dissolution of cell contents in the solvent.
4. Outward diffusion of the solution.
EXTRACTION
IDEAL PROPERTY OF SOLVENT
1. It should be non-toxic and selective.
2. It should not cause the extract to complex or dissociate.
3. It should be preservative in action.
4. It should promote rapid physiologic absorption of the extract.
5. It should be easily evaporated at low heat.
• NOTE:- Alcohol (Ethanol) will meet all above criteria.
IDEAL PROPERTY OF SOLVENT
1. It should be non-toxic and selective.
2. It should not cause the extract to complex or dissociate.
3. It should be preservative in action.
4. It should promote rapid physiologic absorption of the extract.
5. It should be easily evaporated at low heat.
• NOTE:- Alcohol (Ethanol) will meet all above criteria.
STAS-OTTO METHOD
The technique involve the distribution of alkaloidal bases between acid or
aqueous solution and immiscible organic solvent.
MethodI:
The powder is treated with alkalis to liberates the free bases that can
then be extracted with water immiscible organic solvents.
• A). stage1:--Powdered material is moistened with water and mixed with
alkali like sodium & potassium carbonate , ammonia, lime. Make a paste
with water ,dry ,repowder.
• Concept :--Lime(calcium hydroxide),combines with acid , tannins, and
other phenolic substances and sets free alkaloids.
MethodI:
The powder is treated with alkalis to liberates the free bases that can
then be extracted with water immiscible organic solvents.
• A). stage1:--Powdered material is moistened with water and mixed with
alkali like sodium & potassium carbonate , ammonia, lime. Make a paste
with water ,dry ,repowder.
• Concept :--Lime(calcium hydroxide),combines with acid , tannins, and
other phenolic substances and sets free alkaloids.
Powdered drug
Containing alkaloidal salts
Free alkaloids
Total extracts
Aq. Acid soln Residual organic fraction
(Alkaloidal salts) (pigments, fats & weak bases or
chloroform soluble alkaloids sulphates)
Residual aq. Fraction organic soln (alkaloidal bases)
crude alkaloidal mixture
Moisten & render alkaline with Na2CO3,
lime, NH3
Defatted if necessary
Exhaust with org. solvent like CHCl3, ether
Conc. & shake with acid like dil. H2SO4
Method 1 Powdered drug
Containing alkaloidal salts
Free alkaloids
Total extracts
Aq. Acid soln Residual organic fraction
(Alkaloidal salts) (pigments, fats & weak bases or
chloroform soluble alkaloids sulphates)
Residual aq. Fraction organic soln (alkaloidal bases)
crude alkaloidal mixture
Make alkaline extract with
immisicible solvent
Remove solvent
B).Stage2:-- Extract the free alkaloids by hot continous percolation with
chloroform or any other organic solvents.(Concept :-The free alkaloids
dissolve together with other substances soluble in solvent.)
C).Stage3:--Agitate the chloroform soln. with successive portion of
dil.sulphuric acid separating the aqueous layer before adding the next portion
of acid.(Concept :-The alkaloids are converted into alkaloidal sulphates,
which being soluble in water,pass into aqeous layer)
D).Stage4:--Make the mixed aqueous liquid alkaline with ammonia, collect
the precipitate that forms, wash with water and dry. (Concept :- Ammonia
decomposes the alkaloidal sulphates forming ammonium sulphates ,soluble
in water ,and the free alkaloid which being practically insoluble in water is
precipitated)
B).Stage2:-- Extract the free alkaloids by hot continous percolation with
chloroform or any other organic solvents.(Concept :-The free alkaloids
dissolve together with other substances soluble in solvent.)
C).Stage3:--Agitate the chloroform soln. with successive portion of
dil.sulphuric acid separating the aqueous layer before adding the next portion
of acid.(Concept :-The alkaloids are converted into alkaloidal sulphates,
which being soluble in water,pass into aqeous layer)
D).Stage4:--Make the mixed aqueous liquid alkaline with ammonia, collect
the precipitate that forms, wash with water and dry. (Concept :- Ammonia
decomposes the alkaloidal sulphates forming ammonium sulphates ,soluble
in water ,and the free alkaloid which being practically insoluble in water is
precipitated)
Method II:
The powder is extracted with
water soluble organic solvents
such as MeOH or EtOH which
are good solvents for both salts
and free bases. And the resultant
extract is submitted to same
process as that of method1.
ADVANTAGE :-- This method
requires no alkali, gives good
penetration of drug ,and
Economical.
Method II:
The powder is extracted with
water soluble organic solvents
such as MeOH or EtOH which
are good solvents for both salts
and free bases. And the resultant
extract is submitted to same
process as that of method1.
ADVANTAGE :-- This method
requires no alkali, gives good
penetration of drug ,and
Economical.
Method III
The powdered material is extracted with water or aqueous alcohol
containing dilute acid.
Disadvatage:-- Cheap but not used because it also extract impurities
like sugar, mucilage, tannins, colouring matter.
Method III
The powdered material is extracted with water or aqueous alcohol
containing dilute acid.
Disadvatage:-- Cheap but not used because it also extract impurities
like sugar, mucilage, tannins, colouring matter.
EXTRACTION OF ALKALOIDS
Plant material and solvent
Extract
Concentration
Acidified Extract (Alk. as salts)
Organic solvent dissove Impurities
Acidification
Alkalinization
Alkaline aqueous layer
Organic solvent dissove Alkaloids
Plant material and solvent
Extract
Concentration
Acidified Extract (Alk. as salts)
Organic solvent dissove Impurities
Acidification
Alkalinization
Alkaline aqueous layer
Organic solvent dissove Alkaloids
Extraction of liquid alkaloids
1-Plant powder is extracted directly with
acidified water
2-Plant powder is extracted with acidified
alcoholic or a hydro alcoholic solution.
This is then followed by distillation under
vacuum (eliminates that alcohol, leaving
behind and acidic aqueous solution of
alkaloid salts)
1-Plant powder is extracted directly with
acidified water
2-Plant powder is extracted with acidified
alcoholic or a hydro alcoholic solution.
This is then followed by distillation under
vacuum (eliminates that alcohol, leaving
behind and acidic aqueous solution of
alkaloid salts)
PURIFICATION OF ALKALOIDS
1.DIRECT CRYSTALLISATION FROM SOLVENT.
2.STEAM DISTILLATION.
3. CHROMATOGRAPHY TECHNIQUES.
4. GRADIENT pH TECHNIQUES
PURIFICATION OF ALKALOIDS
1.DIRECT CRYSTALLISATION FROM SOLVENT.
2.STEAM DISTILLATION.
3. CHROMATOGRAPHY TECHNIQUES.
4. GRADIENT pH TECHNIQUES
• GRADIENT pH TECHNIQUES
• Though alkaloids are basic in nature, there are variations in the extent in the basicity
of various alkaloids of the same plant
• Depending on this character, the crude alkaloidal mixture is dissolved in 2% tartaric
acid solution and extracted with benzene so that the first fraction contains natural
and/or very weakly basic alkaloids.
• pH of the aqueous solution is increased gradually by 0.5 increment upto pH 9, and
extraction is carried out at each pH level with organic solvent, by this way alkaloids
with different basicity are extracted.
• Strongly basic alkaloids are extracted at the end.
• GRADIENT pH TECHNIQUES
• Though alkaloids are basic in nature, there are variations in the extent in the basicity
of various alkaloids of the same plant
• Depending on this character, the crude alkaloidal mixture is dissolved in 2% tartaric
acid solution and extracted with benzene so that the first fraction contains natural
and/or very weakly basic alkaloids.
• pH of the aqueous solution is increased gradually by 0.5 increment upto pH 9, and
extraction is carried out at each pH level with organic solvent, by this way alkaloids
with different basicity are extracted.
• Strongly basic alkaloids are extracted at the end.
• PRECIPITATION REACTION :
1- Mayer's or Valser's reagent ( Potassium mercuric iodide)
gives white or yellow color mostly amorphous precipitates with alkaloids,except the
purine bases, ephedrine Colchicine and ricinine .
Mercuric chloride 1.36
Potassium iodide 5.00 g
Water to make 100 ml.
2. Wagner's reagent (Iodine- potassium iodide):-
It produces brown or reddish- brown precipitates with all alkaloids.
Iodine 1.3 g
Potassium iodide 2.0 g
Water to make 100 ml
• PRECIPITATION REACTION :
1- Mayer's or Valser's reagent ( Potassium mercuric iodide)
gives white or yellow color mostly amorphous precipitates with alkaloids,except the
purine bases, ephedrine Colchicine and ricinine .
Mercuric chloride 1.36
Potassium iodide 5.00 g
Water to make 100 ml.
2. Wagner's reagent (Iodine- potassium iodide):-
It produces brown or reddish- brown precipitates with all alkaloids.
Iodine 1.3 g
Potassium iodide 2.0 g
Water to make 100 ml
3.Dragendorff's or Krauts reagent ( potassium iodide+ bithmus nitrate):-
It produces orange red precipitate which is usually amorphous.
Bismuth nitrate 8.0 g
Nitric acid 20.5 g
Potassium iodide 27.2 g
Water to 100 ml
4. Hager's reagent (picric acid):- Gives yellow crystalline precipitate.
5. Tannic acid solution: (5%w/v) .:--gives buff colored ppt. which is soluble
in dil.acid or ammonia.
6.Ammonium reineckate solution : 2% solution, produces precipitates with
heterocyclic nitrogen alkaloids, with quaternary and some tertiary amines.
COLOUR REACTION
A). Van-Urks test: (Para-dimethyl-amino-benzaldehyde + sulphuric acid)-- (for
Egot alkaloids).-gives Blue colour.
B). Vitali-Morin test:-- test for solanceous alkaloids gives violet colour when
treated with conc. nitric acid and alcoholic KOH.
Mechanism :-- These color tests usually depend upon dehydration or oxidation
of the alkaloid with a resultant characteristic color.
COLOUR REACTION
A). Van-Urks test: (Para-dimethyl-amino-benzaldehyde + sulphuric acid)-- (for
Egot alkaloids).-gives Blue colour.
B). Vitali-Morin test:-- test for solanceous alkaloids gives violet colour when
treated with conc. nitric acid and alcoholic KOH.
Mechanism :-- These color tests usually depend upon dehydration or oxidation
of the alkaloid with a resultant characteristic color.
METHOD FOR STRUCTURE ELUCIDATION
 U.V. Spectroscopy
 IR Spectroscopy
 Nuclear Magnetic resonance spectroscopy
 Mass spectroscopy
 X-Ray diffraction
METHOD FOR STRUCTURE ELUCIDATION
 U.V. Spectroscopy
 IR Spectroscopy
 Nuclear Magnetic resonance spectroscopy
 Mass spectroscopy
 X-Ray diffraction
CLASSIFICATION
1. The pharmacological action (biological activity).
2. The chemical structure (heterocyclic or no-heterocyclic type of ring structure).
3. The biochemical origin (biosynthetic pathway of production in the plant).
4. The taxonomical origin (plant families rich in alkaloids).
CLASSIFICATION
1. The pharmacological action (biological activity).
2. The chemical structure (heterocyclic or no-heterocyclic type of ring structure).
3. The biochemical origin (biosynthetic pathway of production in the plant).
4. The taxonomical origin (plant families rich in alkaloids).
CLASSIFICATION BASED ON THE RING STRUCTURE OR NUCLEUS
Pyridine-Piperidine ----Lobiline
Tropane---- Atropine
Quinoline ----Quinine
Isoquinoline ---- Emetine
Indole--- Reserpine , Vincristine.
Imidazole --- Pilocarpine
Steroid ---- Solanidine
Alkaloidal amines ---- Ephedrine
Purine --- Caffeine , Theophylline
CLASSIFICATION BASED ON THE RING STRUCTURE OR NUCLEUS
Pyridine-Piperidine ----Lobiline
Tropane---- Atropine
Quinoline ----Quinine
Isoquinoline ---- Emetine
Indole--- Reserpine , Vincristine.
Imidazole --- Pilocarpine
Steroid ---- Solanidine
Alkaloidal amines ---- Ephedrine
Purine --- Caffeine , Theophylline
CLASSIFICATION BASED ON PHARMACOLOGICAL ACTIVITY
1. Analgesics and narcotics: Morphine and codeine.
2. CNS stimulants : Caffeine and strychnine.
3. Anticancer:Vincristine, vinblastine and taxol.
4. Mydriatics:Atropine.
5. Anti-asthmatics :Ephedrine.
6. Anti- tussive: Codeine.
7. Expectorants: Lobeline.
8. Anti- hypertensive:Reserpine.
9. Smooth muscle relaxants:Atropine and papaverine
10. Skeletal muscle relaxants: d- tubocurarine.
11. Anthelmintics:Pelletierine and arecoline.
12. Antiparasitics: Quinine and emetine.
1. Analgesics and narcotics: Morphine and codeine.
2. CNS stimulants : Caffeine and strychnine.
3. Anticancer:Vincristine, vinblastine and taxol.
4. Mydriatics:Atropine.
5. Anti-asthmatics :Ephedrine.
6. Anti- tussive: Codeine.
7. Expectorants: Lobeline.
8. Anti- hypertensive:Reserpine.
9. Smooth muscle relaxants:Atropine and papaverine
10. Skeletal muscle relaxants: d- tubocurarine.
11. Anthelmintics:Pelletierine and arecoline.
12. Antiparasitics: Quinine and emetine.
CLASSIFICATION BASED ON ROBINSON
( BASED ON BIOSYNTHESIS)
 Ornithine alkaloids ---- Pyrolline alkaloids (Nicotine)
 Lysine alkaloids ---- Anabasine , Lupinine
 Phenylalanine alkaloids ---- l-Hyoscyamine , Mescaline
 Tryptophan alkaloids ---- Strychnine , Ergotamine ,
Tyrosine alkaloids ---- Morphine , Papaverine , Codeine
Terpenoid alkaloids ----- Squalene , Carotenoids
 Purine alkaloids ---- Caffeine
CLASSIFICATION BASED ON ROBINSON
( BASED ON BIOSYNTHESIS)
 Ornithine alkaloids ---- Pyrolline alkaloids (Nicotine)
 Lysine alkaloids ---- Anabasine , Lupinine
 Phenylalanine alkaloids ---- l-Hyoscyamine , Mescaline
 Tryptophan alkaloids ---- Strychnine , Ergotamine ,
Tyrosine alkaloids ---- Morphine , Papaverine , Codeine
Terpenoid alkaloids ----- Squalene , Carotenoids
 Purine alkaloids ---- Caffeine
Classification of Alkaloids
• True (Typical) alkaloids that are derived from amino acids and
have nitrogen in a heterocyclic ring. e.g. Atropine
• Proto alkaloids that are derived from amino acids and do not have
nitrogen in a heterocyclic ring. e.g. Ephedrine
• Pseudo alkaloids that are not derived from amino acids but have
nitrogen in a heterocyclic ring. e.g. Caffeine
• False alkaloids are non alkaloids give false positive reaction with
alkaloidal reagents.
Classification of Alkaloids
• True (Typical) alkaloids that are derived from amino acids and
have nitrogen in a heterocyclic ring. e.g. Atropine
• Proto alkaloids that are derived from amino acids and do not have
nitrogen in a heterocyclic ring. e.g. Ephedrine
• Pseudo alkaloids that are not derived from amino acids but have
nitrogen in a heterocyclic ring. e.g. Caffeine
• False alkaloids are non alkaloids give false positive reaction with
alkaloidal reagents.
Hegnauer's classification
• 1)."True alkaloids", which contain nitrogen in the heterocyclic ring
and originate from amino acids. examples are atropine, nicotine and
morphine, Quinine.
• All the heterocyclic alkaloids are true alkaloids.
The true alkaloids should have following characters:
a)It should be sufficiently toxic.
b)should have marked physiological activity.
c)should be basic in nature.
d)Nitrogen should be present in a heterocyclic ring.
e)Should be derived from amino acids.
f)should occur in plant as salt of organic acids.
Hegnauer's classification
• 1)."True alkaloids", which contain nitrogen in the heterocyclic ring
and originate from amino acids. examples are atropine, nicotine and
morphine, Quinine.
• All the heterocyclic alkaloids are true alkaloids.
The true alkaloids should have following characters:
a)It should be sufficiently toxic.
b)should have marked physiological activity.
c)should be basic in nature.
d)Nitrogen should be present in a heterocyclic ring.
e)Should be derived from amino acids.
f)should occur in plant as salt of organic acids.
2)Proto alkaloids
• These are also called Non heterocyclic or Atypical alkaloids or
Biological amines.
• These are less commonly found in nature.
• These molecules have a nitrogen atom which is not a part of any ring
system.
• Examples of these include ephedrine, colchicine, erythromycin and
taxol etc.
• Table below shows the chemical structure and biological significance
of these compounds
• Examples include:- mescaline, adrenaline and ephedrine
• These are also called Non heterocyclic or Atypical alkaloids or
Biological amines.
• These are less commonly found in nature.
• These molecules have a nitrogen atom which is not a part of any ring
system.
• Examples of these include ephedrine, colchicine, erythromycin and
taxol etc.
• Table below shows the chemical structure and biological significance
of these compounds
• Examples include:- mescaline, adrenaline and ephedrine
3.Pseudo-Alkaloids:--They do not derived from amino acid but having
nitrogen in heterocyclic ring .
They do not show many of the typical characters of alkaloids , but give
standard qualitative test for alkaloids.
e.g. steroidal alkaloids:-conessine
Purine bases :-- Caffeiene
Name Structure
Biological
Significance
Ephedrine
Adrenergic agent-
used for asthma and
hay fever
Colchicine Relieves gout
Erythromycin Antibiotic
Name Structure
Biological
Significance
Ephedrine
Adrenergic agent-
used for asthma and
hay fever
Colchicine Relieves gout
Erythromycin Antibiotic
Taxol
(Paclitaxel)
Used in the treatment
of ovarian cancer,
breast cancer and
non-small cell lung
cancer
Taxol
(Paclitaxel)
Used in the treatment
of ovarian cancer,
breast cancer and
non-small cell lung
cancer
B. Heterocyclic Alkaloids or Typical Alkaloids:
• Structurally these have the nitrogen as a part of a cyclic ring system.
• These are more commonly found in nature.
• Heterocyclic alkaloids are further subdivided into 14 groups based on
the ring structure containing the nitrogen
B. Heterocyclic Alkaloids or Typical Alkaloids:
• Structurally these have the nitrogen as a part of a cyclic ring system.
• These are more commonly found in nature.
• Heterocyclic alkaloids are further subdivided into 14 groups based on
the ring structure containing the nitrogen
No. Heterocycle Example
1.
Pyrrole and
Pyrrolidine
Hygrine, Stachydrine
2.
Pyrrolizidine
Senecionine, Symphitine, Echimidine,
Seneciphylline
No. Heterocycle Example
1.
Pyrrole and
Pyrrolidine
Hygrine, Stachydrine
2.
Pyrrolizidine
Senecionine, Symphitine, Echimidine,
Seneciphylline
3.
Pyridine and Piperidine
Lobeline, Nicotine, Piperine, Conine,
Trigonelline
4.
Tropane (piperidine/N-methyl-
pyrrolidine)
Cocaine, Atropine, Hyoscyamine, Hyoscine
5.
Quinoline
Quinine, Quinidine, Cinchonine,
Cinchonidine
3.
Pyridine and Piperidine
Lobeline, Nicotine, Piperine, Conine,
Trigonelline
4.
Tropane (piperidine/N-methyl-
pyrrolidine)
Cocaine, Atropine, Hyoscyamine, Hyoscine
5.
Quinoline
Quinine, Quinidine, Cinchonine,
Cinchonidine
6.
Isoquinoline
Morphine, Emetine, Papaverine, Narcotine,
Tubocurarine, Codeine
7.
Aporphine (reduced
isoquinoline/naphthalene)
Boldine
8.
Quinolizidine
Lupanine, Cytisine, Laburnine, Sparteine
6.
Isoquinoline
Morphine, Emetine, Papaverine, Narcotine,
Tubocurarine, Codeine
7.
Aporphine (reduced
isoquinoline/naphthalene)
Boldine
8.
Quinolizidine
Lupanine, Cytisine, Laburnine, Sparteine
9.
Indole or
Benzopyrole
Ergometrine, Vinblastine, Vincristine, Strychnine, Brucine,
Ergotamine, Yohimbine, Reserpine, Serpentine,
Physostigmine
10.
Indolizidine
Castanospermine, Swainsonine
11.
Imidazole or
glyoxaline
Pilocarpine, Pilosine
9.
Indole or
Benzopyrole
Ergometrine, Vinblastine, Vincristine, Strychnine, Brucine,
Ergotamine, Yohimbine, Reserpine, Serpentine,
Physostigmine
10.
Indolizidine
Castanospermine, Swainsonine
11.
Imidazole or
glyoxaline
Pilocarpine, Pilosine
12.
Purine (pyrimidine/imidazole)
Caffeine, Theobromine
13.
Steroidal (some combined as
glycosides)*
Conessine, Solanidine
14. Terpenoid*
Aconitine, lycaconitine, Aconine
*Note- Steroidal and terpenoid classes are also treated as separate classes or along with glycosides.
12.
Purine (pyrimidine/imidazole)
Caffeine, Theobromine
13.
Steroidal (some combined as
glycosides)*
Conessine, Solanidine
14. Terpenoid*
Aconitine, lycaconitine, Aconine
*Note- Steroidal and terpenoid classes are also treated as separate classes or along with glycosides.
SYSTAMATIC PHARMACOGNOSTIC
STUDY OF ALKALOIDS
SYSTAMATIC PHARMACOGNOSTIC
STUDY OF ALKALOIDS
Biological source : It is the Dried bark of cultivated trees of Cinchona officinalis
belonging in to the family Rubiaceae.(NLT 6% Alkaloids)
Synonyms: Jesuil’ bark, Peruvian bark
Macroscopical characters:
Odour - Slight & characteristic
Taste - Astringent & intensely bitter
Stem bark
Colour:
(outer surface) Dull to brown or grey pale(inner surface)
yellowish brown to reddish brown
 Fracture- Short & fibrous
 Size- 30cm long, 2-6mm thick
Root bark- Colour- outer & inner surfaces are similar
Size- 207cm long
CINCHONA
Macroscopical characters:
Odour - Slight & characteristic
Taste - Astringent & intensely bitter
Stem bark
Colour:
(outer surface) Dull to brown or grey pale(inner surface)
yellowish brown to reddish brown
 Fracture- Short & fibrous
 Size- 30cm long, 2-6mm thick
Root bark- Colour- outer & inner surfaces are similar
Size- 207cm long
Other features: Number of transverse cracks are present
Powder is Yellow in colour, 12mm diameter ,1.5mm thick
MICROSCOPY
Cinchona exhibits following Histological
characters
Cork cells are thin walled.
Cortex consists of secretary channels and
phloem fibres.
Medullary rays are radially arranged.
Idioblasts of calcium oxalate is the specific
characteristic of cinchona bark.
Starch grains are present in parenchymatous
tissue.
Medullary rays are 2 to 3 walled.
Cinchona exhibits following Histological
characters
Cork cells are thin walled.
Cortex consists of secretary channels and
phloem fibres.
Medullary rays are radially arranged.
Idioblasts of calcium oxalate is the specific
characteristic of cinchona bark.
Starch grains are present in parenchymatous
tissue.
Medullary rays are 2 to 3 walled.
T.S of Cinchona bark
Cultivation and collection
Most of the cinchona found in tropical & sub tropical regions about 1000-3000 m.
Rainfall required are uniform 250-380 cm/year .Favorable growth is achieved at 60-
75ºF.
Cinchona requires light well drained forest soil with rich organic matter.
The acidic soil having a PH of 4 -5.6 and small amount of nitrogen imp for favorable
growth.
It requires high humidity and slopping situation, protection from wind.
The propagation is done by seeds or budding or layering.
The seeds of cinchona are very small, light in weight ( 1 gm = 3500 seeds).
Germination takes place in 3-6 weeks.
The seedlings with 2 pairs of leaves are transplanted and space of 6 – 10 cm, at a
distance of 2 x 2 meters .
Plants of 4 to 20 years are selected for harvesting, bark is collected by coppicing
method, dried at 175 ºF.(care to be take to avoid fermentation) .
Cultivation and collection
Most of the cinchona found in tropical & sub tropical regions about 1000-3000 m.
Rainfall required are uniform 250-380 cm/year .Favorable growth is achieved at 60-
75ºF.
Cinchona requires light well drained forest soil with rich organic matter.
The acidic soil having a PH of 4 -5.6 and small amount of nitrogen imp for favorable
growth.
It requires high humidity and slopping situation, protection from wind.
The propagation is done by seeds or budding or layering.
The seeds of cinchona are very small, light in weight ( 1 gm = 3500 seeds).
Germination takes place in 3-6 weeks.
The seedlings with 2 pairs of leaves are transplanted and space of 6 – 10 cm, at a
distance of 2 x 2 meters .
Plants of 4 to 20 years are selected for harvesting, bark is collected by coppicing
method, dried at 175 ºF.(care to be take to avoid fermentation) .
EXTRACTION
Step 1: The cinchona bark is dried, powdered, sieved and treated with calcium oxide (slaked
lime), NaOH solution (10% w/v) and water and kept as such for 6-8 hours.
Step II: The resulting mixture is treated with benzene in sufficient quantity and refluxed for
12-16 hours. The mixture is then filtered while it is hot.
Step III: The hot filtrate is extracted successively with 6N. sulphuric acid. The mixture of
alkaloidal bisulphate is heated up to 90°C and maintained at this temperature up to 20-30 m
Step IV: The resulting solution is cooled to room temperature and made alkaline by the
addition of solid pure sodium carbonate till a pH 6.5 is attained.
Step V: The alkaloidal sulphate solution thus obtained is treated with sufficient quantity of
activated charcoal powder (1g per 1L), boil, shake vigorously and filter.
Step VI: Cool the hot filtrate slowly in a refrigerator (2-10°C) overnight and again filter.
Collect the residue and the filtrate separately.
Step VII: The residue (or precipitate) of quinine sulphate is boiled with water and made
alkaline by adding cautiously solid sodium carbonate. The resulting precipitate is that
of quinine.
EXTRACTION
Step 1: The cinchona bark is dried, powdered, sieved and treated with calcium oxide (slaked
lime), NaOH solution (10% w/v) and water and kept as such for 6-8 hours.
Step II: The resulting mixture is treated with benzene in sufficient quantity and refluxed for
12-16 hours. The mixture is then filtered while it is hot.
Step III: The hot filtrate is extracted successively with 6N. sulphuric acid. The mixture of
alkaloidal bisulphate is heated up to 90°C and maintained at this temperature up to 20-30 m
Step IV: The resulting solution is cooled to room temperature and made alkaline by the
addition of solid pure sodium carbonate till a pH 6.5 is attained.
Step V: The alkaloidal sulphate solution thus obtained is treated with sufficient quantity of
activated charcoal powder (1g per 1L), boil, shake vigorously and filter.
Step VI: Cool the hot filtrate slowly in a refrigerator (2-10°C) overnight and again filter.
Collect the residue and the filtrate separately.
Step VII: The residue (or precipitate) of quinine sulphate is boiled with water and made
alkaline by adding cautiously solid sodium carbonate. The resulting precipitate is that
of quinine.
CHEMICAL CONSTITUENTS
Cinchona bark contain many alkaloids the majors are:
1- Quinine and Quinidine. 2- Cinchonine and Cinchonidine.
Cinchona alkaloids are present as salts with Quinic and Cincho tannic acids.
They are diacidic bases form two types of salts:
1- Neutral salts (Monoacidic) (less water soluble.
2- Acidic salts (Diacidic) water soluble.
Both Quinine and Quinidine, Cinchonine and Cinchonidine are Diastereoisomers. Each
pair differs in the stereochemistry at C-8 and C-9.
CHEMICAL CONSTITUENTS
Cinchona bark contain many alkaloids the majors are:
1- Quinine and Quinidine. 2- Cinchonine and Cinchonidine.
Cinchona alkaloids are present as salts with Quinic and Cincho tannic acids.
They are diacidic bases form two types of salts:
1- Neutral salts (Monoacidic) (less water soluble.
2- Acidic salts (Diacidic) water soluble.
Both Quinine and Quinidine, Cinchonine and Cinchonidine are Diastereoisomers. Each
pair differs in the stereochemistry at C-8 and C-9.
N
N
H3CO
HO
H H
N
N
H3CO
HO
H H
89
Quinine Quinidine
Tests for identification
may be identified either by a series of Colour Tests
1- Fluorescence test:
Solution of the alkaloid in oxygenated acids (e.g H2SO4, HNO3 or
phosphoric acid)  blue fluorescence (+ ve with quinine and quinidine).
2- Thalleoquine test:
Aqueous solution of the alkaloidal salt + Br2 /H2O (few drops till the
appearance of yellow color) + NH4OH  emerald green color
(+ ve with quinine and quinidine).
3- Rosequin test (Erythroquinine test):
Aqueous solution of the alkaloidal salt + dil HCl + Br2 /H2O (few drops till
the appearance of yellow color) + CHCl3 + pot. Ferrocyanide + NH4OH

red color in the CHCl3 layer (+ ve with quinine and quinidine).
Tests for identification
may be identified either by a series of Colour Tests
1- Fluorescence test:
Solution of the alkaloid in oxygenated acids (e.g H2SO4, HNO3 or
phosphoric acid)  blue fluorescence (+ ve with quinine and quinidine).
2- Thalleoquine test:
Aqueous solution of the alkaloidal salt + Br2 /H2O (few drops till the
appearance of yellow color) + NH4OH  emerald green color
(+ ve with quinine and quinidine).
3- Rosequin test (Erythroquinine test):
Aqueous solution of the alkaloidal salt + dil HCl + Br2 /H2O (few drops till
the appearance of yellow color) + CHCl3 + pot. Ferrocyanide + NH4OH

red color in the CHCl3 layer (+ ve with quinine and quinidine).
Uses:
1. It is frequently employed as a flavour in carbonated beverages.
2. It is used as an Antimalarial agent.
3. It is also employed as a Skeletal muscle relaxant.
4. It has been used to treat Hemorrhoids and varicose veins.
5. Quinine is also used as a Oxytocic agent.
6. Quinine is supposed to be Prophylactic for flu.
Dose: Cinchona powder-0.3-1 g
Quinine sulphate - 1 g daily for 2 days 600 mg daily 5 days
quinidine sulphate 0.2 to 0.4 g every 2 – 4 hrs total dose of 3 g daily
in atrial fibrillation.
Uses:
1. It is frequently employed as a flavour in carbonated beverages.
2. It is used as an Antimalarial agent.
3. It is also employed as a Skeletal muscle relaxant.
4. It has been used to treat Hemorrhoids and varicose veins.
5. Quinine is also used as a Oxytocic agent.
6. Quinine is supposed to be Prophylactic for flu.
Dose: Cinchona powder-0.3-1 g
Quinine sulphate - 1 g daily for 2 days 600 mg daily 5 days
quinidine sulphate 0.2 to 0.4 g every 2 – 4 hrs total dose of 3 g daily
in atrial fibrillation.
ERGOT
Biological source: ergot is the dried sclerotium of the fungus Claviceps
purpurea (Fries) belonging to the family Clavicipitaceae developed in the ovary of
rye, Secale cereale (Germinae/ Poaceae).
Ergot is a fungal disease very commonly and widely observed on a good number
of wild as well as cultivated grasses, and is produced by different species
of claviceps.
This particular disease is usually characterized by the formation of hard and seed
like ‘ergots’ in place of the normal seeds. However, these specific structures are
frequently termed as sclerotia, which represent the ‘resting stage’ of the fungus.
The generic name, ‘claviceps’, usually refers to the club-like nature of
the sclerotium, where as purpurea signifies its purple colour. As these sclerotia are
elongated and somewhat pointed in shape and appearance, hence the common name
of spurred rye has been assigned to the drug.
Synonyms: Ergot; Rye Ergot. spurred rye
Ergot is a fungal disease very commonly and widely observed on a good number
of wild as well as cultivated grasses, and is produced by different species
of claviceps.
This particular disease is usually characterized by the formation of hard and seed
like ‘ergots’ in place of the normal seeds. However, these specific structures are
frequently termed as sclerotia, which represent the ‘resting stage’ of the fungus.
The generic name, ‘claviceps’, usually refers to the club-like nature of
the sclerotium, where as purpurea signifies its purple colour. As these sclerotia are
elongated and somewhat pointed in shape and appearance, hence the common name
of spurred rye has been assigned to the drug.
Ergot fungus
Clavicepspurpurea
Categories of ergot alkaloids:
four main categories of ergot alkaloids which may be distinguished, namely
(a) Clavine alkaloids.
(b) Lysergic acids.
(c) Lysergic acid amides.
(d) Ergot peptide alkaloids.
There are ten Ergot peptide alkaloids which are: Ergotamine, Ergosine,
Ergocristine, Ergocryptine, Ergocornine, Ergotaminine, Ergosinine, Ergocristinine,
Ergocryptinine, and Ergocorninine
Categories of ergot alkaloids:
four main categories of ergot alkaloids which may be distinguished, namely
(a) Clavine alkaloids.
(b) Lysergic acids.
(c) Lysergic acid amides.
(d) Ergot peptide alkaloids.
There are ten Ergot peptide alkaloids which are: Ergotamine, Ergosine,
Ergocristine, Ergocryptine, Ergocornine, Ergotaminine, Ergosinine, Ergocristinine,
Ergocryptinine, and Ergocorninine
The poisonous properties of ergots in grain, specifically rye, for animal as well as
human consumption, purposefully and unknowingly, have long been recognized.
The dreadful causative agents are collectively termed as the ‘ergot alkaloids’,
containing essentially an Indole nucleus.
Cultivation
The life cycle of the fungus, claviceps purpurea, which is a parasite, passes
through the following characteristics stages
The genus Claviceps is a group of phytopathogenic ascomycetes that is composed
of approximately 36 different species of filamentous fungi.
Ergot is a French word derived from argot (a spur) and represents the dark brown,
horn-shaped pegs that project from ripening ears of rye in place of rye grains.
These tuberous projections are collected before and during harvesting or are
separated from the threshed rye.
In a histologic sense, these bodies consist of compactly inter woven hyphae of the
filamentous fungus Claviceps purpurea but biologically these compact grains are
designated as sclerotia, the form in which the fungus passes the winter.
Cultivation
The life cycle of the fungus, claviceps purpurea, which is a parasite, passes
through the following characteristics stages
The genus Claviceps is a group of phytopathogenic ascomycetes that is composed
of approximately 36 different species of filamentous fungi.
Ergot is a French word derived from argot (a spur) and represents the dark brown,
horn-shaped pegs that project from ripening ears of rye in place of rye grains.
These tuberous projections are collected before and during harvesting or are
separated from the threshed rye.
In a histologic sense, these bodies consist of compactly inter woven hyphae of the
filamentous fungus Claviceps purpurea but biologically these compact grains are
designated as sclerotia, the form in which the fungus passes the winter.
1. The parasitic life cycle of the ergot fungi begins in the spring, with wind-borne
ascopores landing on susceptible host plants.
2. Hyphae invade and colonize the ovary, producing masses of anamorphic spores
that are exuded into a syrupy fluid (honeydew).
3. Insect vectors, rain splash, or head-to-head contact transfer this honeydew to
other blooming florets, allowing the spread of the ergot fungi in a field.
4. When the sclerotia begin to form, production of honeydew and condiation
cease, and the sclerotia mature in about 5 weeks.
5. The sclerotia are considered as the early stage of sexual differentiation of
Claviceps. In autumn, the ripe pigmented sclerotium leaves the spike and falls
to the ground, ultimately producing asci and non seprate ascospores, thereby
completing the cycle.
LIFE CYCLE OF ERGOT
1. The parasitic life cycle of the ergot fungi begins in the spring, with wind-borne
ascopores landing on susceptible host plants.
2. Hyphae invade and colonize the ovary, producing masses of anamorphic spores
that are exuded into a syrupy fluid (honeydew).
3. Insect vectors, rain splash, or head-to-head contact transfer this honeydew to
other blooming florets, allowing the spread of the ergot fungi in a field.
4. When the sclerotia begin to form, production of honeydew and condiation
cease, and the sclerotia mature in about 5 weeks.
5. The sclerotia are considered as the early stage of sexual differentiation of
Claviceps. In autumn, the ripe pigmented sclerotium leaves the spike and falls
to the ground, ultimately producing asci and non seprate ascospores, thereby
completing the cycle.
1.Sphacelia or Honeydew or Asexual stage
The rye plant becomes infected by the spores of the fungus in the spring session.
The spores are carried out by the wind or by insect to the flowers and collected at
the base of the young ovary where moisture is present. There germination of the
spores takes place.
A filamentous hyphae is formed which enters into the wall of the ovary by
enzymatic action.
A soft, white mass over the surface of ovary is formed which is known as
honeydew, is secreted during the sphacelia stage which contains reducing sugars.
From the ends of some hyphae small oval conidiophores (asexual spores) are
abstracted which remain suspended on honeydew.
The sweet taste of honeydew attracts some insect like ants and weevils. Insects
suck the sweet liquid and carry the conidiophores to the plants and spread the
fungal infection in the rye plants.
1.Sphacelia or Honeydew or Asexual stage
The rye plant becomes infected by the spores of the fungus in the spring session.
The spores are carried out by the wind or by insect to the flowers and collected at
the base of the young ovary where moisture is present. There germination of the
spores takes place.
A filamentous hyphae is formed which enters into the wall of the ovary by
enzymatic action.
A soft, white mass over the surface of ovary is formed which is known as
honeydew, is secreted during the sphacelia stage which contains reducing sugars.
From the ends of some hyphae small oval conidiophores (asexual spores) are
abstracted which remain suspended on honeydew.
The sweet taste of honeydew attracts some insect like ants and weevils. Insects
suck the sweet liquid and carry the conidiophores to the plants and spread the
fungal infection in the rye plants.
2.Sclerotinum or Ascigerous or Sexual stage
During the sphacelia stage the hyphae enter only wall of the ovary. On further
development they penetrate into deeper parts, feed on the ovarian tissues and
replace it by a compact, dark purple hard tissue known as pseudo parenchyma.
It forms the sclerotinum or resting state of the fungus. During summer the
sclerotinum or ergot increases in size and projects on the rye, showing sphacelia
remains at its apex. It is collected at this stage by hands or machine and used as a
drug. Ergot is then dried to remove moisture.
3.Ascospores stage
If ergot is not collected, it falls on the ground. In the next spring session they
produce stalked projections known as stromata which have globular heads.
In the inner surface of the heads there are a large number of flask shaped pockets
known as perithesia. Each of these perithesia contains many sacs (asci) which
possesses eight of the threads-like ascospores.
2.Sclerotinum or Ascigerous or Sexual stage
During the sphacelia stage the hyphae enter only wall of the ovary. On further
development they penetrate into deeper parts, feed on the ovarian tissues and
replace it by a compact, dark purple hard tissue known as pseudo parenchyma.
It forms the sclerotinum or resting state of the fungus. During summer the
sclerotinum or ergot increases in size and projects on the rye, showing sphacelia
remains at its apex. It is collected at this stage by hands or machine and used as a
drug. Ergot is then dried to remove moisture.
3.Ascospores stage
If ergot is not collected, it falls on the ground. In the next spring session they
produce stalked projections known as stromata which have globular heads.
In the inner surface of the heads there are a large number of flask shaped pockets
known as perithesia. Each of these perithesia contains many sacs (asci) which
possesses eight of the threads-like ascospores.
Ascospores
Hyphae
(asci)
HyphaeHyphaeSclerotia
Macroscopical characters
(i) Size:
Sclerotium is about 1-4 cm long, 2-7 mm broad.
(ii) Shape:
Fusiform, slightly curved, Subcylendrical, tapering at the both ends.
(iii) Outer surface:
Darks or violet-black in colour is longitudinal furrows and sometimes small
transverse cracks.
(iv) Fracture surface:
Thin, dark outer layer a whitish or pinkish-white central zone of pseudo parenchyma
in which darker lines radiate from the centre.
(v) Odour:
Characteristics.
(vi) Taste:Unpleasant.
Macroscopical characters
(i) Size:
Sclerotium is about 1-4 cm long, 2-7 mm broad.
(ii) Shape:
Fusiform, slightly curved, Subcylendrical, tapering at the both ends.
(iii) Outer surface:
Darks or violet-black in colour is longitudinal furrows and sometimes small
transverse cracks.
(iv) Fracture surface:
Thin, dark outer layer a whitish or pinkish-white central zone of pseudo parenchyma
in which darker lines radiate from the centre.
(v) Odour:
Characteristics.
(vi) Taste:Unpleasant.
Microscopical characters
The outermost layer of the sclerotium is
made up of flattened thin walled cells
While inner layer is made up of dense
pseudo parenchymatous cells composed of
chitin
The mycelial cells are round or oval ,
thick .
These are also composed of fixed oils
Sclerotium doesn’t contains any
materials like starch grains, calcium
oxalate crystals, and lignified cells.
The outermost layer of the sclerotium is
made up of flattened thin walled cells
While inner layer is made up of dense
pseudo parenchymatous cells composed of
chitin
The mycelial cells are round or oval ,
thick .
These are also composed of fixed oils
Sclerotium doesn’t contains any
materials like starch grains, calcium
oxalate crystals, and lignified cells.
T.S of sclerotium of Ergot
1. The powdered dried ergot is first defatted with n-hexane or petroleum ether (40-60°)
2. The marc is thoroughly mixed with aluminium sulphate and water , so as to fix the
alkaloids by converting them into the double salts.
3. The resulting alkaloidal double salts are subjected to continuous extraction with hot
benzene that removes the alkaloid exclusively on one hand; and the unwanted
substances e.g., ergot oil, soluble acid, neutral substances like- phytosterol, colouring matter
and organic acids on the other.
4. The benzene is removed under vacum and the residue thus obtained is stirred for several
hours with a large volume of benzene and subsequently made alkaline by passing NH3 gas.
5. The resulting solution is filtered and the benzene extract is concentrated under vacum,
whereupon ergotamine crystallizes out.
6. An additional quantity of ergotamine may also be crystallized from the mother liquour
by treatment with petroleum ether.
7. Ergotamine may be further purified by crystallization from aqueous acetone.
EXTRACTION
1. The powdered dried ergot is first defatted with n-hexane or petroleum ether (40-60°)
2. The marc is thoroughly mixed with aluminium sulphate and water , so as to fix the
alkaloids by converting them into the double salts.
3. The resulting alkaloidal double salts are subjected to continuous extraction with hot
benzene that removes the alkaloid exclusively on one hand; and the unwanted
substances e.g., ergot oil, soluble acid, neutral substances like- phytosterol, colouring matter
and organic acids on the other.
4. The benzene is removed under vacum and the residue thus obtained is stirred for several
hours with a large volume of benzene and subsequently made alkaline by passing NH3 gas.
5. The resulting solution is filtered and the benzene extract is concentrated under vacum,
whereupon ergotamine crystallizes out.
6. An additional quantity of ergotamine may also be crystallized from the mother liquour
by treatment with petroleum ether.
7. Ergotamine may be further purified by crystallization from aqueous acetone.
Chemical constituents
Most important Ergot alkaloids are
Ergometrine group (Water soluble)
Ergometrine , Ergometrinine.
Ergotamine group (water -insoluble)
Ergotamine , Ergotaminine , Ergosine.
Ergotoxine group (Water-insoluble)
Ergocristine , Ergocristinine , Ergocryptine , Ergocryptinine , Ergocornine
2. Alkaloids obtained from lysergic acid are physiological active.
3. Histamine , tyramine
4. Sterols like ergosterol and fungisterol,
5. Elymoclavine , sclerythrin , ergonovine,
7. Clavicepsin , ergoflavin , ergotic acid betaine
8. Clavine, mannitol, lactic acid and succinic acid.
Chemical constituents
Most important Ergot alkaloids are
Ergometrine group (Water soluble)
Ergometrine , Ergometrinine.
Ergotamine group (water -insoluble)
Ergotamine , Ergotaminine , Ergosine.
Ergotoxine group (Water-insoluble)
Ergocristine , Ergocristinine , Ergocryptine , Ergocryptinine , Ergocornine
2. Alkaloids obtained from lysergic acid are physiological active.
3. Histamine , tyramine
4. Sterols like ergosterol and fungisterol,
5. Elymoclavine , sclerythrin , ergonovine,
7. Clavicepsin , ergoflavin , ergotic acid betaine
8. Clavine, mannitol, lactic acid and succinic acid.
Identification Tests
The ergot alkaloids are readily precipitated by the alkaloidal reagents. However,
Mayer's reagent is regarded to be the most sensitive test
Iodine solution in KI also gives an instant precipitate with very dilute solutions
of ergot alkaloids.
Keller's Test: To a solution of the alkaloid in glacial acetic acid add a few mg of
solid FeCl3 and then add 1-2 ml of concentrated sulphuric acid along the side of the
tube. The appearance of an intense blue colouration is accomplished at the junction
of the two layers.
Fluorescence Test: The aqueous solution of the salts of ergot alkaloids produce a
distinct blue fluorescence..
Van Urk Test: When a solution containing an ergot alkaloid is mixed with Van
Urk Reagent**, it gives rise to a characteristic deep blue colouration.
Identification Tests
The ergot alkaloids are readily precipitated by the alkaloidal reagents. However,
Mayer's reagent is regarded to be the most sensitive test
Iodine solution in KI also gives an instant precipitate with very dilute solutions
of ergot alkaloids.
Keller's Test: To a solution of the alkaloid in glacial acetic acid add a few mg of
solid FeCl3 and then add 1-2 ml of concentrated sulphuric acid along the side of the
tube. The appearance of an intense blue colouration is accomplished at the junction
of the two layers.
Fluorescence Test: The aqueous solution of the salts of ergot alkaloids produce a
distinct blue fluorescence..
Van Urk Test: When a solution containing an ergot alkaloid is mixed with Van
Urk Reagent**, it gives rise to a characteristic deep blue colouration.
USES
1. Ergonovine is used as an oxytocic.
2. Ergonovine maleate also acts as an oxytocic and produces much faster
stimulation of the uterine muscles as compared to other drugs
3. It is employed as a potent antimigraine drug.
4. Ergotamine possesses oxytocic properties.
5. Ergotamine tartrate is used invariably to prevent or abort vascular headaches,
including migraine and cluster headaches. The mechanism of action is perhaps
due to direct vasoconstriction of the dilated carotid artery bed with concomitant
lowering in the amplitude of pulsations.
6. Ergotamine tartrate is also an antagonist of the serotonin activity.
7. Ergotamine tartrate is frequently used along with caffeine for the management
and control of migraine headache. Both serve as cerebral vasoconstrictors
USES
1. Ergonovine is used as an oxytocic.
2. Ergonovine maleate also acts as an oxytocic and produces much faster
stimulation of the uterine muscles as compared to other drugs
3. It is employed as a potent antimigraine drug.
4. Ergotamine possesses oxytocic properties.
5. Ergotamine tartrate is used invariably to prevent or abort vascular headaches,
including migraine and cluster headaches. The mechanism of action is perhaps
due to direct vasoconstriction of the dilated carotid artery bed with concomitant
lowering in the amplitude of pulsations.
6. Ergotamine tartrate is also an antagonist of the serotonin activity.
7. Ergotamine tartrate is frequently used along with caffeine for the management
and control of migraine headache. Both serve as cerebral vasoconstrictors
IPECAC
Biological source: Ipecac is the dried roots and rhizomes of Cephalis ipecacuanha
(Brazilian ipecacuanha) belonging to the Family Rubiaceae. It contains several
alkaloids (2 –2.5 %), mainly emetine (50- 70 % of total alkaloids), with cephaline
and psychotrine.
Synonyms: Ipecacuanha.
Cultivation
The propagation is done by seed sowing
Germination of the seed increased by treatment of the seed with lime water /
hydrogen peroxide
Seedlings are transplanted at 10 x 10 cm at a room temperature of 23 – 38°C
It requires a rain fall of 30 cm , humidity helps the plant
Nitrogenous fertilizers have significant effect in quality of plant
Character Root part Rhizome part
Color Dark brick red to brown Brick red to brown
Odour Faint Faint
Taste Bitter Bitter
Size 150 mm length; 60 mm thickness 2 mm in diameter
Shape Tortuous , pieces cylindrical
Macroscopical characters
T.S shows cork cells followed by phelloderma.
Composed by parenchymatous cells
Shows presence of starch grains, calcium oxalate crystals.
It also shows presence of tracheids
Microscopical characters
Root part
Pericycle are thick walled
Protoxylem are spiral
Starch grains are presentStarch grains are present
Rhizome part
Pericycle are thick walled
Sclereids are present
Starch grains are present in larger size
T.S of : Ipecacuanha
P o w d e re d ro o t a n d rh iz o m e
- E xt. a lco h o l,C o nc., lea d a ceta te.
- Filtratio n
F iltra te R e s id u e
N on -a lka loida l su b.
- E vap ., d il. H C l & Filtratio n
A lka loida l ba ses a n d sa lts
F iltra te (A lka loida l H C l sa lts)
- A lk . w ith N a O H & E xt. w ith eth er
E th e r la ye r
E m etin e
(P h en olic a lka loids)
- H C l (A lk alo id al salts)
- A lk . N H 4 O H E xt. eth er
A q u e o u s la ye r E th e r la ye r
(P sy ch otrin e) (C eph a lin e)
A q .a lk . s o lu tio n
ISOLATION OF IPECAC ALKALOIDS
P o w d e re d ro o t a n d rh iz o m e
- E xt. a lco h o l,C o nc., lea d a ceta te.
- Filtratio n
F iltra te R e s id u e
N on -a lka loida l su b.
- E vap ., d il. H C l & Filtratio n
A lka loida l ba ses a n d sa lts
F iltra te (A lka loida l H C l sa lts)
- A lk . w ith N a O H & E xt. w ith eth er
E th e r la ye r
E m etin e
(P h en olic a lka loids)
- H C l (A lk alo id al salts)
- A lk . N H 4 O H E xt. eth er
A q u e o u s la ye r E th e r la ye r
(P sy ch otrin e) (C eph a lin e)
A q .a lk . s o lu tio n
CHEMICAL CONSTITUENTS
N
MeO
RO
N
OMe
OMe
H
H
R = Me Emetine
R = H Cephaline
N
MeO
HO
N
OMe
OMe
H
Psychotrine
Emetine:
It is non phenolic and levorotatory.
It contains 2 basic nitrogens.
Psychotrine:
Occurs as yellow prisms.
It is phenolic and gives cephaline on reduction.
It gives emetine on reduction followed by methylation.
N
MeO
RO
N
OMe
OMe
H
H
R = Me Emetine
R = H Cephaline
N
MeO
HO
N
OMe
OMe
H
Psychotrine
Cephaline:
It is phenolic and levorotatory.
It gives emetine on methylation with
(CH3)2 SO4.
Alkaloidal solution in HCl + Ca hypochlorite  orange color.
Emetine and cephaline + Froehd's reagent: dirty green color (the color with
emetine fades by addition of HCl).
Psychotrine + Froehd's reagent: pale green color.
Cephaline and psychotrine + p-nitrodiazobenzene  dye soluble in NaOH 
purple color.
Psychotrine + conc. H2SO4 + HNO3  cherry red color.
Emetine + Liebermann's reagent  black color.
IDENTIFICATION TESTS
Alkaloidal solution in HCl + Ca hypochlorite  orange color.
Emetine and cephaline + Froehd's reagent: dirty green color (the color with
emetine fades by addition of HCl).
Psychotrine + Froehd's reagent: pale green color.
Cephaline and psychotrine + p-nitrodiazobenzene  dye soluble in NaOH 
purple color.
Psychotrine + conc. H2SO4 + HNO3  cherry red color.
Emetine + Liebermann's reagent  black color.
Uses
Emetine and cephaeline have antitumour and antiviral activity, but are too
toxic for therapeutic use.
Emetine and psychotrine are mainly used as emetic drugs.
The crude drug is used as expectorant (due to its saponin content) .
Emetine HCl and Dehydroemetine (DHE) have an antiamoebic effect, and
are used for the treatment of amoebic dysentry
Ipeca alkaloids are diaphoretic,
Dose :1 mg / kg of body weight,(IM or IV)
Emetine and cephaeline have antitumour and antiviral activity, but are too
toxic for therapeutic use.
Emetine and psychotrine are mainly used as emetic drugs.
The crude drug is used as expectorant (due to its saponin content) .
Emetine HCl and Dehydroemetine (DHE) have an antiamoebic effect, and
are used for the treatment of amoebic dysentry
Ipeca alkaloids are diaphoretic,
Dose :1 mg / kg of body weight,(IM or IV)
OPIUM
Biological Source: Opium or gum opium is the air dried milky exudates obtained
by incising the unripe capsules of Papaver somniferum. family - Papaveraceae .
History: In 1806 Serturner isolated the alkaloid morphine from Opium. The
opium poppy is grown commercially now in many countries throughout the world.
Cultivation and Collection: The cultivation of Opium poppy is controlled
internationally by the International Narcotics Control Board of the United Nations.
Synonym : Poppy Latex , Gum opium.
Cultivation and Collection: The cultivation of Opium poppy is controlled
internationally by the International Narcotics Control Board of the United Nations.
The seeds of opium are cultivated in batches. This is to ensure that the entire
crop is not affected by climatic conditions like frost or drought.
The cultivation is done in the months between September and April.
A gap of 25 cm should be maintained between two consecutive plants.
Before sowing the seeds, they are mixed with sands properly.
About five to six capsules appear on each plant and it flowers in the month of
May-June.
After the petals fall from the poppy, the pod, which is about the size of a golf
ball, is lanced, and the opium latex is exuded.
Poppies are lanced in the afternoon and the latex is scraped off the next
morning.
Pods ripen (soften) at different times in the field. Each pod can be lanced from 4
to 7 times.
The seeds of opium are cultivated in batches. This is to ensure that the entire
crop is not affected by climatic conditions like frost or drought.
The cultivation is done in the months between September and April.
A gap of 25 cm should be maintained between two consecutive plants.
Before sowing the seeds, they are mixed with sands properly.
About five to six capsules appear on each plant and it flowers in the month of
May-June.
After the petals fall from the poppy, the pod, which is about the size of a golf
ball, is lanced, and the opium latex is exuded.
Poppies are lanced in the afternoon and the latex is scraped off the next
morning.
Pods ripen (soften) at different times in the field. Each pod can be lanced from 4
to 7 times.
Commercial varieties include Turkish, Persian, Indian & Yugoslavian opium.
Macroscopic Character
Odor: Strong , characteristic.
Taste: Bitter.
Color: Varies depending on the type of
opium. For instance, Indian opium is dark
brown while manipulated Turkish opium is
chocolate brown in color.
Chemical constituents
Opium contains more than 19 alkaloids, some of which are
combined with Meconic acid, others with sulfuric acid and some as
free alkaloids.
There are 3 main classes
Phenanthrene.-----------------Morphine ,Thebeine , Codeine.
Benzyl Isoquinoline. ------- Noscapine , Papaverine
Phenyl alkyl amine --------- Narceine
Chemical constituents
Opium contains more than 19 alkaloids, some of which are
combined with Meconic acid, others with sulfuric acid and some as
free alkaloids.
There are 3 main classes
Phenanthrene.-----------------Morphine ,Thebeine , Codeine.
Benzyl Isoquinoline. ------- Noscapine , Papaverine
Phenyl alkyl amine --------- Narceine
Extraction from Opium
Powdered Opium
Shaken with Calcium chloride solution and filteredShaken with Calcium chloride solution and filtered
Filtrate concentrated+10% NaOH solution
Precipitate
(Narcotine, Papaverine, Thebaine)
Filtrate
(Morphine, Codeine,)
1.Opium is dissolved in water and then ferric chloride solution is
added. It results in reddish purple color. The change in color occurs
due to presence of Meconic acid in opium.
2.When opium is treated with small amount of nitric acid, orange red
color is produced. This test occurs due to the presence of morphine
in opium
CHEMICAL TESTS
1.Opium is dissolved in water and then ferric chloride solution is
added. It results in reddish purple color. The change in color occurs
due to presence of Meconic acid in opium.
2.When opium is treated with small amount of nitric acid, orange red
color is produced. This test occurs due to the presence of morphine
in opium
Morphine
1. Most powerful analgesic used in cases of severe pain as post operative pain,
bone fractures, cancer patients & in cases of angina.
2. Remedy in convulsions.
3. Precede the use of anesthetics to increase their efficacy
4. Used as an antagonists for poisonous effects of other alkaloids as strychnine,
atropine, phytostigmine.
USESMorphine
1. Most powerful analgesic used in cases of severe pain as post operative pain,
bone fractures, cancer patients & in cases of angina.
2. Remedy in convulsions.
3. Precede the use of anesthetics to increase their efficacy
4. Used as an antagonists for poisonous effects of other alkaloids as strychnine,
atropine, phytostigmine.
Dose: Morphine Sulfate parentrally is 10mg 6 / day.
Codeine
1. is weaker in intensity than morphine.
2. produces less tendencies to addiction.
3. Codeine depresses the cough center in the brain.
4. Causes constipation & hypnosis.
Dose:
Usual doses of codeine phosphate and Codeine sulfate are
As analgesic: 15-60 mg every 4 hrs.
As antitussive:10-20 mg every 4-6 hrs.
Dose:
Usual doses of codeine phosphate and Codeine sulfate are
As analgesic: 15-60 mg every 4 hrs.
As antitussive:10-20 mg every 4-6 hrs.
Heroin
1. It is the synthetic diacetyl derivative of morphine.
2. It is 5 X more potent as morphine.
Papaverine
Occurs naturally in opium to the extent of about
1%.Used as Smooth muscle relaxant and an
anti-tussive in combination with Codeine
sulfate. Dose: Orally 150 mg, IM 30 mg.
• As antitussive 15mg.
Synosym: Belladonna leaf, Deadly night shade
Biological source: Belladonna herb consists of dried leafs and other aerial parts of
Atropa belladonna, belonging to the family Solanaceae
Macroscopy
Colour: leaves are green to brownish
Flowers are purple to yellowish
Fruits are green to brown
Odour : slight and characteristic
Taste : Bitter acrid
Size : Leaves-5 to 25 cm long,2.5 to 12 cm wide
Flowers –corolla 3 cm long 2 cm wide
Fruits- 10 cm diameter
Shape : leaves are ovate , lanceolate , acuminate
Flowers : campanulate , small
Fruits : Berries , subglobular ,
BELLADONNA
Colour: leaves are green to brownish
Flowers are purple to yellowish
Fruits are green to brown
Odour : slight and characteristic
Taste : Bitter acrid
Size : Leaves-5 to 25 cm long,2.5 to 12 cm wide
Flowers –corolla 3 cm long 2 cm wide
Fruits- 10 cm diameter
Shape : leaves are ovate , lanceolate , acuminate
Flowers : campanulate , small
Fruits : Berries , subglobular ,
Microscopy
Epidermal cells are slightly anticlinical
Anisocytic stomata is present, uniserrate , covering trichomes also present
Palisade ration is 5-7
Chemical constituents : l- Hyoscyamine , Belladonine ,Scopolamine.
Uses :Parasympatholytic , Anti- cholenergic , reduces sweat , saliva , Gastric
juice , spasm , also used as Antidote
Dose : 0.6 - 1 ml Belladonna tincture 4 times / day.
Epidermal cells are slightly anticlinical
Anisocytic stomata is present, uniserrate , covering trichomes also present
Palisade ration is 5-7
Chemical constituents : l- Hyoscyamine , Belladonine ,Scopolamine.
Uses :Parasympatholytic , Anti- cholenergic , reduces sweat , saliva , Gastric
juice , spasm , also used as Antidote
Dose : 0.6 - 1 ml Belladonna tincture 4 times / day.
S.NO PLANT NAME IDENTIFICATION
1 Plytolacca americanna ( leaves ) Presence of Idioblasts
2 Solanum nigrum Presence Thick lamina , Anomocytic stomata
3 Ailanthus glandulosa Presence cluster of calcium oxalate crystals
Adulterants
Synosym: Periwinkle , Vinca
Biological source: Dried whole plant of Catharanthus roses , belonging to the
family Apocynaceae.
Macroscopy
VINCA
Colour: leaves are green , pale grey ,
flowers are violet , pink , white , carmine red.
Odour : Bitter and characteristic
Taste : Bitter
Shape : leaves are ovate , petiolate , oblong , unicostate ,
reticulate , acute , apex , entire , brittle , glossy in appearance ,
Flowers : Bracteates , pedicellate , complex , hermaphodite ,
2-3 cm cymose.
Colour: leaves are green , pale grey ,
flowers are violet , pink , white , carmine red.
Odour : Bitter and characteristic
Taste : Bitter
Shape : leaves are ovate , petiolate , oblong , unicostate ,
reticulate , acute , apex , entire , brittle , glossy in appearance ,
Flowers : Bracteates , pedicellate , complex , hermaphodite ,
2-3 cm cymose.
Microscopy
Upper surface is single layered rectangular in shape
Epidermis consists of unicellular ,
 covering trichomes .
Palisade is single layered
5- 8 layered Spongy parenchyma is present
Mid rib consists of collenchyma , xylem ,
phloem present in centre
Stomata is of cruciferous
Lower epidermis contains Calcium oxalate crystals
Upper surface is single layered rectangular in shape
Epidermis consists of unicellular ,
 covering trichomes .
Palisade is single layered
5- 8 layered Spongy parenchyma is present
Mid rib consists of collenchyma , xylem ,
phloem present in centre
Stomata is of cruciferous
Lower epidermis contains Calcium oxalate crystals
Chemical constituents : mainly contains Indole group with oncocytic action
like Vincristine , Vinblastine , ajmalicine ,
Dose : Vincristine-10 to 30 mg / body wt : Vinblastine 100 µg / body wt
T.S of : Vinca
Antineoplastic agents
Vinblastine
Arrests mitosis in metaphase
Gives intravenously in acute leukemia in
children
Vincristine
Arrests mitosis in metaphase
Interferes amino acid metabolism treats
Hodgkin's disease
Hypertensive and anti diabetic
Uses
Antineoplastic agents
Vinblastine
Arrests mitosis in metaphase
Gives intravenously in acute leukemia in
children
Vincristine
Arrests mitosis in metaphase
Interferes amino acid metabolism treats
Hodgkin's disease
Hypertensive and anti diabetic
EPHEDRA Synosym: Ma-Huang
Biological source: It consists of dried young stem of Ephedra gerardiana and
Ephedra nebrodensis. Belonging in to the Family Gnetaceae (Ephedraceae).
MACROSCOPY
Ephedra is Gymnospermous bearing thin stem which
are woody ,cylindrical in nature 5 mm in diameter.
Ephedra consists of scaly leaves ,
The bases of the leaves are dark brown and they are
joined on all sides of the node forming a sheath .
Which bears a terminal bud, which is short , usually
constricted at the base.
The male spikes are solitary , ovate , sessile and
crowded.
“ma”=astringent, “huang”=yellow
MACROSCOPY
Ephedra is Gymnospermous bearing thin stem which
are woody ,cylindrical in nature 5 mm in diameter.
Ephedra consists of scaly leaves ,
The bases of the leaves are dark brown and they are
joined on all sides of the node forming a sheath .
Which bears a terminal bud, which is short , usually
constricted at the base.
The male spikes are solitary , ovate , sessile and
crowded.
MICROSCOPY
Unicellular epidermis made up of
quadrangular cells along with thick
walled cuticle
Vertical rows of sunken stomata and
papillae on ridges
Cortex is collenchymatous
Hypodermal fibers are non-lignified
Pericyclic fibres are lignified
Calcium oxalate crystals are present
in cortex
Pith is of parenchymatous dark in
color
Unicellular epidermis made up of
quadrangular cells along with thick
walled cuticle
Vertical rows of sunken stomata and
papillae on ridges
Cortex is collenchymatous
Hypodermal fibers are non-lignified
Pericyclic fibres are lignified
Calcium oxalate crystals are present
in cortex
Pith is of parenchymatous dark in
color T.S of : Ephedra
Chemical constituents :It contains the amino alkaloids : Ephedrine, nor-ephedrine,
n-methyl ephedrine, pseudo-ephedrine.
Ephedrine Produced commercially by:
Extraction of the plant material
Chemical procedure involving a reductive condensation between L-1-phenyl-1-
acetylcarbinol and methylamine
Occurs as white, rosette or needle crystals, or as an unctuous mass
Soluble in water, alcohol, chloroform, ether, and liquid petrolatum
Melts between 33 and 400C, depending on its water content
Chemical constituents :It contains the amino alkaloids : Ephedrine, nor-ephedrine,
n-methyl ephedrine, pseudo-ephedrine.
Ephedrine Produced commercially by:
Extraction of the plant material
Chemical procedure involving a reductive condensation between L-1-phenyl-1-
acetylcarbinol and methylamine
Occurs as white, rosette or needle crystals, or as an unctuous mass
Soluble in water, alcohol, chloroform, ether, and liquid petrolatum
Melts between 33 and 400C, depending on its water content
Identification Test :-- Ephedrine is dissolved in water and dil.hcl ,then treated
separately with copper sulphate and sodium hydroxide. The solution gives Violet
colour. If shaken with ether the organic layer shows purple colour and aqueous
layer shows blue colour.
USES:
Sympathomimetic (stimulates α, β1, & β2 adrenergic receptors)
Ephedrine Sulfate – crystals of the sulfate of Ephedrine Used to combat
hypotensive states, for allergic disorders, and for nasal decongestion.
bronchodilator in asthma.
Usual dose is:
25-50mg, 6-8x a day as necessary (oral & parenteral)
0.1-0.15mL of a 1-3% solution, 2-3x a day (intranasal)
USES:
Sympathomimetic (stimulates α, β1, & β2 adrenergic receptors)
Ephedrine Sulfate – crystals of the sulfate of Ephedrine Used to combat
hypotensive states, for allergic disorders, and for nasal decongestion.
bronchodilator in asthma.
Usual dose is:
25-50mg, 6-8x a day as necessary (oral & parenteral)
0.1-0.15mL of a 1-3% solution, 2-3x a day (intranasal)
Synonyms :Coffee bean, coffee seedCOFFEE
Biological Source : It is the dried ripe seed of Coffea arabica. It belongs to family
Rubiaceae.
Coffee plant is an evergreen shrub which bears drupe type of fruit with an
ellipsoidal or spheroidal shape.
Each fruit has 2 locules, containing one seed in each chamber.
 Each plant gives about 2 -3 kg of coffee seeds. The fruit are dried to separate the
seeds.
The seeds are separated by wetting them and mechanically separating, followed
by drying in heaps, which causes fermentation.
The separated seeds or beans are green in colour.
They are roasted by which the colour and odour is effected.
The seeds acquire dark brown colour and possess an agreeable odour and bitter
taste.
Coffee plant is an evergreen shrub which bears drupe type of fruit with an
ellipsoidal or spheroidal shape.
Each fruit has 2 locules, containing one seed in each chamber.
 Each plant gives about 2 -3 kg of coffee seeds. The fruit are dried to separate the
seeds.
The seeds are separated by wetting them and mechanically separating, followed
by drying in heaps, which causes fermentation.
The separated seeds or beans are green in colour.
They are roasted by which the colour and odour is effected.
The seeds acquire dark brown colour and possess an agreeable odour and bitter
taste.
CHEMICAL CONSTITUENTS
The main constituents of coffee bean are caffeine, tannin, fixed oil and
proteins.
It contains 2-3% caffeine, 3-5% tannins, 13% proteins, 10-15% fixed oils,
Caffeine chlorogenic or caffeotannic acid and sugars in the form of dextrin,
glucose, etc. in the seeds, caffeine is present as a salt of chlorogenic acid.
During roasting process, the agreeable smell of coffee is developed which is
due to an oil called caffeol composed of mainly furfural along with minor
quantities of phenol, pyridine and valerianic acid.
CHEMICAL CONSTITUENTS
The main constituents of coffee bean are caffeine, tannin, fixed oil and
proteins.
It contains 2-3% caffeine, 3-5% tannins, 13% proteins, 10-15% fixed oils,
Caffeine chlorogenic or caffeotannic acid and sugars in the form of dextrin,
glucose, etc. in the seeds, caffeine is present as a salt of chlorogenic acid.
During roasting process, the agreeable smell of coffee is developed which is
due to an oil called caffeol composed of mainly furfural along with minor
quantities of phenol, pyridine and valerianic acid.
Chemical Test:
1. Murexide test: caffeine when heated with Hcl & potassium chlorate gives a
residue which turns purple when exposed to ammonia vapours
2. Caffeine forms a white precipitate with tannin solution
EXTRACTION OF CAFFEINE
Caffeine is prepared either by synthesis or extracted from natural sources.
Coffee bean is one of the major sources for it.
For the extraction, coffee roasters are used in which caffeine sublimed during
roasting is recovered.
USES
It is used as the source of caffeine.
The main effects of coffee i.e. stimulant and
diuretic actions are due to caffeine.
Chemical Test:
1. Murexide test: caffeine when heated with Hcl & potassium chlorate gives a
residue which turns purple when exposed to ammonia vapours
2. Caffeine forms a white precipitate with tannin solution
COLCHICUM Synosym: meadow saffron seed , autumn crocus
Biological source: It consists of dried ripe seeds of Colchicum luteum and
Colchicum autumnale. Belonging in to the family Liliaceae.
Character Colchicum seed Colchicum corms
Color Very hard and reddish brown testa Yellowish brown
Odour None None
Taste Bitter acrid Bitter acrid
Size 2 – 3 mm in diameter Slices are 2 – 5 mm thickSize 2 – 3 mm in diameter Slices are 2 – 5 mm thick
Shape Projection at hilum Ovate ,sub- reniform
Extra features Presence of Strophiole at hilum Fracture is short and cut surface ,
shows grayish points
MICROSCOPY
The section of seed shows parenchyma and endosperm.
The parenchymatous cells are reddish brown with thick walls.
The endodermic cells shows pitted walls and contains aleurone grains and fixed oils.
The Strophiole portion contains starch.
The corm has epidermis , parenchyma and vascular tissue .
Parenchymatous cells shows presence of starch.
Epidermis shows presence of circular stomata.
Vascular bundles are present with spiral annular xylems.
The section of seed shows parenchyma and endosperm.
The parenchymatous cells are reddish brown with thick walls.
The endodermic cells shows pitted walls and contains aleurone grains and fixed oils.
The Strophiole portion contains starch.
The corm has epidermis , parenchyma and vascular tissue .
Parenchymatous cells shows presence of starch.
Epidermis shows presence of circular stomata.
Vascular bundles are present with spiral annular xylems.
Chemical constituents : Colchicine and Demi-colchicine.(both the alkaloids
contain Tropolone ring structure).
Colchicine is freely soluble in alcohol and chloroform , soluble in 25 parts of water
and in 220 parts of ether.
Identification Test :-- - Colchicine + 70% H2SO4 gives Yellow colour.
Colchicine + alcoholic solution + Fecl3 gives red color
Uses :--
Specific drug for treatment of Gout and also having Anti-Tumor activity.
Apart from medicinal also shows mutations in as a chemical agent in
horticulture.
Dose :500-650 µg , orally 1 – 3 times daily orally
500 µg to 1 mg , 1-2 times a day intravenously
Allied drugs:
1.Dipadax 2.Bulbocodium 3. Gloriosa
Uses :--
Specific drug for treatment of Gout and also having Anti-Tumor activity.
Apart from medicinal also shows mutations in as a chemical agent in
horticulture.
Dose :500-650 µg , orally 1 – 3 times daily orally
500 µg to 1 mg , 1-2 times a day intravenously
Allied drugs:
1.Dipadax 2.Bulbocodium 3. Gloriosa
HYOSCYAMUS Synosym: Henbane , Hyoscyamus leaf
Biological source: Dried leafs of Hyoscyamus Niger belonging to the family
solanaceae , it consists of NLT 0.05 % Hyoscyamus , l- Hyoscyamine.
MACROSCOPY
Color :leaves are pale green in color
Odor :characteristic
Taste :bitter , acrid
Size : Lamina is 25 cm long
Shape :Ovate , Oblong , Triangular , with
petiole ,
Leaf margins are irregular , dentate
Apex is covered with hairs , shows pinnate
venetation
Flowers are funnel shaped
MACROSCOPY
Color :leaves are pale green in color
Odor :characteristic
Taste :bitter , acrid
Size : Lamina is 25 cm long
Shape :Ovate , Oblong , Triangular , with
petiole ,
Leaf margins are irregular , dentate
Apex is covered with hairs , shows pinnate
venetation
Flowers are funnel shaped
MICROSCOPY
Leaves are Dorsiventral
Epidermis covered with smooth cuticle
Numerous glandular trichomes are present
Palisade cells are appear in single layer
Idioblasts are also present
Chemical constituents : Scopolamine
, l- hyoscyamine. Atropine
T.S of : Hyoscyamus leafChemical constituents : Scopolamine
, l- hyoscyamine. Atropine
Uses :--Purgative , Sedative , Expectorant , Anti-spasmodic , Anti-histamatic
Scopolamine patch is used for: Preventing nausea and vomiting associated with
motion sickness and recovery from anesthesia and surgery.
Identification Test :-- vitali-Morin
test is +ve alkaloids gives violet
colour when treated with conc. nitric
acid and alcoholic KOH.
DUBOISIA
Biological source: Dried leafs of Duboisia myoporoides belonging to the family
solanaceae .
Synosym: Cork wood
MACROSCOPY Duboisia is a perennial herb / surb 3.0 m
Color :Brown to purple
Odor :characteristic
Taste :bitter , acrid
Size : Leaves are 3- 10 cm ling
Shape : Tapering ends with
alternate arrangement
MACROSCOPY Duboisia is a perennial herb / surb 3.0 m
Color :Brown to purple
Odor :characteristic
Taste :bitter , acrid
Size : Leaves are 3- 10 cm ling
Shape : Tapering ends with
alternate arrangement
Chemical constituents : Scopolamine , l- hyoscyamine. Atropine , Valtropine
Identification Test :-- vitali-Morin test is +ve alkaloids gives violet colour when
treated with conc. nitric acid and alcoholic KOH.
Uses :Parasympatholytic , Anti- cholenergic , reduces sweat , saliva , Gastric juice
, spasm , also used as Antidote
Identification Test :-- vitali-Morin test is +ve alkaloids gives violet colour when
treated with conc. nitric acid and alcoholic KOH.
Uses :Parasympatholytic , Anti- cholenergic , reduces sweat , saliva , Gastric juice
, spasm , also used as Antidote
NUX VOMICA
Biological source: Nux vomica consists of dried ripe seeds of Strycnos nux vomica
Linn, belonging to family Loganiaceae
Strycnos=poison vomica =nut with vomiting effect
Synonym: crow fig, strychni,Nux vomica seed
MACROSCOPY
Colour: Greenish –brown
Odour: None
Taste :Bitter
Size: Seeds are 10 -30 mm in diameter
4-6 mm thickness
Extra features: seeds are radial disc
shaped, Endosperm, cotyledons
seen in L.S of seed
MACROSCOPY
Colour: Greenish –brown
Odour: None
Taste :Bitter
Size: Seeds are 10 -30 mm in diameter
4-6 mm thickness
Extra features: seeds are radial disc
shaped, Endosperm, cotyledons
seen in L.S of seed
MICROSCOPIC STUDY
Epidermis contains thickened, lignified trichomes followed by layer of
collapsed cells.
Endo dermis contains thickened polyhedral un- lignified cells with plasma
derma.
Oil globules, calcium oxalate crystals, starch grains are absent
Chemical constituents: Indole alkaloids –strychine,brucine ,strychnine
Chemical tests:
T.S of Nux vomica with ammonium vandate and sulphuric acid (manddin’s
test) gives purple colour – Strychine
T.S of Nux vomica with Con,nitic acid gives yellow color- Brucine.
Uses:1.stomachic ,tonic due to bitter taste
2.CNS Stimulant ,
3.Action on CVS increase blood pressure
MICROSCOPIC STUDY
Epidermis contains thickened, lignified trichomes followed by layer of
collapsed cells.
Endo dermis contains thickened polyhedral un- lignified cells with plasma
derma.
Oil globules, calcium oxalate crystals, starch grains are absent
Chemical constituents: Indole alkaloids –strychine,brucine ,strychnine
Chemical tests:
T.S of Nux vomica with ammonium vandate and sulphuric acid (manddin’s
test) gives purple colour – Strychine
T.S of Nux vomica with Con,nitic acid gives yellow color- Brucine.
Uses:1.stomachic ,tonic due to bitter taste
2.CNS Stimulant ,
3.Action on CVS increase blood pressure
WITHANIA Synonyms: Withania root, asgandh, winter cherry.
Biological source: It consists of dried roots & stem bases of withania somnifera
belonging to the family solanaceae.
Macroscopy:
Colour - Buff or grey yellow
Odour - Similar to urine of horse
Taste - Bitter
Fracture- Smooth & powdery
Extra features:
The root has longitudinal wrinkles
They are un-branched, straight, conical & some of them
bear a crown.
Root crown shows a number of bud scars
Roots are bitter in taste , fresh root gives smell similar to
horse urine
Macroscopy:
Colour - Buff or grey yellow
Odour - Similar to urine of horse
Taste - Bitter
Fracture- Smooth & powdery
Extra features:
The root has longitudinal wrinkles
They are un-branched, straight, conical & some of them
bear a crown.
Root crown shows a number of bud scars
Roots are bitter in taste , fresh root gives smell similar to
horse urine
Microscopic study
The T.S of root shows presence of cork with non lignified cells of 2 – 4 layers
It also shows presence of vascular tissue like cambium , phloem , sieve tubes
Secondary xylem is hard in nature
Starch grains are present in stem bases , it also shows tracheids.
Chemical constituents:
The main constituents are alkaloids & steroidal lactones. Withanine is the main
constituent. The other alkaloids are somniferine, somnine, pseudo withanine.
Steroidal lactones are also called withanolides. The drug also contains somnitol &
somnirol.
Uses: It has sedative & hypnotic effects.
It has hypotensive, Respiratory, stimulant actions.
It is an immunomodulatory agent.
It is used in the treatment of rheumatism, gout & skin diseases.
It is widely used as sex stimulant & rejuvenator.
Also used against staphylococcus aureus
Microscopic study
The T.S of root shows presence of cork with non lignified cells of 2 – 4 layers
It also shows presence of vascular tissue like cambium , phloem , sieve tubes
Secondary xylem is hard in nature
Starch grains are present in stem bases , it also shows tracheids.
Chemical constituents:
The main constituents are alkaloids & steroidal lactones. Withanine is the main
constituent. The other alkaloids are somniferine, somnine, pseudo withanine.
Steroidal lactones are also called withanolides. The drug also contains somnitol &
somnirol.
Uses: It has sedative & hypnotic effects.
It has hypotensive, Respiratory, stimulant actions.
It is an immunomodulatory agent.
It is used in the treatment of rheumatism, gout & skin diseases.
It is widely used as sex stimulant & rejuvenator.
Also used against staphylococcus aureus
Biological source: It is the dried stem bark of Holarrhena antidysentrica /
Holarrhena pubescens belonging to the family Apocynacece. It is collected from
8 to 10 years old plant and freed from attached wood and peeled into small pieces.
It should contain NLT 2% of total alkaloids of kurchi
Macroscopy:
Colour - Buff to pale brown on outer surface
Slightly brownish on inner surface
Odour - No odour
Taste - Bitter and Acrid
Macroscopy:
Colour - Buff to pale brown on outer surface
Slightly brownish on inner surface
Odour - No odour
Taste - Bitter and Acrid
Extra features:
Shape :- Longitudinally RECURVED pieces
Size :- Variable
Outer surface :-It is longitudinally wrinkled and bears horizontal lenticels
Inner surface :- Brownish rough and with irregular transverse cracks
Fracture :- Short and granular
MICROSCOPIC STUDY
CORK CELLS
Thin walled few colorless and few are with yellowish
brown matter
STONE CELLS / SCLERIDS
Rectangular to oval in shape, walls striated, pitted and
lignified. surrounded by sheath of parenchymatous cells
containing calcium oxalate crystals.
MEDULLARY RAYS
Phloem parenchyma traverse the medullary rays at right
angles through such pieces are not seen many in number
CALCIUM OXALATE CRYSTALS
Present in the form of prisms scattered all over in the
powder
STARCH GRAINS
Few in number, simple grains
CORK CELLS
Thin walled few colorless and few are with yellowish
brown matter
STONE CELLS / SCLERIDS
Rectangular to oval in shape, walls striated, pitted and
lignified. surrounded by sheath of parenchymatous cells
containing calcium oxalate crystals.
MEDULLARY RAYS
Phloem parenchyma traverse the medullary rays at right
angles through such pieces are not seen many in number
CALCIUM OXALATE CRYSTALS
Present in the form of prisms scattered all over in the
powder
STARCH GRAINS
Few in number, simple grains
Kurchi bark contains steroidal alkaloid up to about 1.8 to 4.5%
They are C21 group of steroidal alkaloids
The active alkaloids are conessine (kurchicine), norconessine, isoconessine,
dioxyconessine, conessimine, holarrhimine, holarrhidine,
Conessine is also present in root bark along with some other steroidal alkaloids
In addition to alkaloids kurchi contains gums, resins, tannins, lupeal and
beta- sitosterol
Chemical constituents
Kurchi bark contains steroidal alkaloid up to about 1.8 to 4.5%
They are C21 group of steroidal alkaloids
The active alkaloids are conessine (kurchicine), norconessine, isoconessine,
dioxyconessine, conessimine, holarrhimine, holarrhidine,
Conessine is also present in root bark along with some other steroidal alkaloids
In addition to alkaloids kurchi contains gums, resins, tannins, lupeal and
beta- sitosterol
HOLARRHIDINECONESSINE
CHEMICAL TESTSCHEMICAL TESTS
SALKOWSKI REACTION:- To 20 ml of extract add 2ml of chloroform and 2ml
of concentrated sulphuric acid shake well. chloroform layer appears red and
acid layer shows greenish yellow fluorescence. Indicates the presence of
steroidal moiety .
LIBERMANN-BURCHARD REACTION:-Mix 2ml of extract with chloroform
add 1-2ml of acetic anhydride and 2drops of concentrated sulphuric acid
from sides of the test tube. First red then blue and finally green color
appears. Indicates the presence of steroidal moiety.
LIBERMANN’S REACTION:-Mix 3ml extract with 3ml acetic anhydride heat
and cool, add few drops of concentrated sulphuric acid. Blue color
appears. Indicates the presence of steroidal moiety .
CHEMICAL TESTSCHEMICAL TESTS
SALKOWSKI REACTION:- To 20 ml of extract add 2ml of chloroform and 2ml
of concentrated sulphuric acid shake well. chloroform layer appears red and
acid layer shows greenish yellow fluorescence. Indicates the presence of
steroidal moiety .
LIBERMANN-BURCHARD REACTION:-Mix 2ml of extract with chloroform
add 1-2ml of acetic anhydride and 2drops of concentrated sulphuric acid
from sides of the test tube. First red then blue and finally green color
appears. Indicates the presence of steroidal moiety.
LIBERMANN’S REACTION:-Mix 3ml extract with 3ml acetic anhydride heat
and cool, add few drops of concentrated sulphuric acid. Blue color
appears. Indicates the presence of steroidal moiety .
THERAPEUTIC USESTHERAPEUTIC USES
• Kurchi bark is antiprotozoal in activity and used to treat amoebic
dysentery
• Kurchi bark is considered to be stomachic, astringent, tonic, anti-
dysenteric, febrifuge and anthelmintic
• The dried bark is rubbed over the body in dropsy
• Conessine is highly active against Entamoeba histolytica
• A traditional preparation of kurchi bark i.e. “kutajarishta” is commonly
used specially for chronic amoebiasis
THERAPEUTIC USESTHERAPEUTIC USES
• Kurchi bark is antiprotozoal in activity and used to treat amoebic
dysentery
• Kurchi bark is considered to be stomachic, astringent, tonic, anti-
dysenteric, febrifuge and anthelmintic
• The dried bark is rubbed over the body in dropsy
• Conessine is highly active against Entamoeba histolytica
• A traditional preparation of kurchi bark i.e. “kutajarishta” is commonly
used specially for chronic amoebiasis
DATURA Synonyms: hell’s bells, devil’s trumpet, Nightshade, Datura metal
Biological source: Dried leaves & flowering tops of Datura stramonium ,
belonging to the family solanaceae , it consists of NLT 0.20 % alkaloids
l-hyoscyamine
Macroscopy
Colour - Green
Odour - Unpleasant and bitter
Taste - Bitter
Size - 9-18 cm length
8-13 cm width
Leaves are entire , broken wrinkled , un equal
bases , acute apex , flowers are funnel shaped
,seeds are brown in color , found in thorny
capsules
Macroscopy
Colour - Green
Odour - Unpleasant and bitter
Taste - Bitter
Size - 9-18 cm length
8-13 cm width
Leaves are entire , broken wrinkled , un equal
bases , acute apex , flowers are funnel shaped
,seeds are brown in color , found in thorny
capsules
Microscopic study
Datura is a Dorsiventral leaf
Collenchyma appears above & below the mid rib regions
Unicellular covering & glandular trichomes are present
Xylem is surrounded by phloem
Presence of Anisocytic stomata
Alkaloids: Properties and Sources
Alkaloids: Properties and Sources
Alkaloids: Properties and Sources
Alkaloids: Properties and Sources
Alkaloids: Properties and Sources
Alkaloids: Properties and Sources
Alkaloids: Properties and Sources
Alkaloids: Properties and Sources
Alkaloids: Properties and Sources
Alkaloids: Properties and Sources
Alkaloids: Properties and Sources
Alkaloids: Properties and Sources
Alkaloids: Properties and Sources
Alkaloids: Properties and Sources
Alkaloids: Properties and Sources
Alkaloids: Properties and Sources
Alkaloids: Properties and Sources
Alkaloids: Properties and Sources

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Alkaloids: Properties and Sources

  • 1. ALKALOIDSALKALOIDS K.Sudheer Kumar, Assistant professor. Dept.of Pharmacognosy Chilkur Balaji college of Pharmacy Hyderabad. E-mail:sudheer.y2k8@gmail.com
  • 2. Plants have been one of the important sources of medicines since the beginning of human civilization. There is a growing demand for plant based medicines, health products, pharmaceuticals, food supplements and cosmetics. According to the WHO survey 80% populations living in the developing countries rely almost exclusively on traditional medicine for their primary health care needs. In addition, herbs have provided us some of the very important life saving drugs used in the modern medicine. However among the estimated 2,50,000- 4,00,000 plant species, only 6% have been studied for biological activity and about 15% have been investigated phytochemically. INTRODUCTION Plants have been one of the important sources of medicines since the beginning of human civilization. There is a growing demand for plant based medicines, health products, pharmaceuticals, food supplements and cosmetics. According to the WHO survey 80% populations living in the developing countries rely almost exclusively on traditional medicine for their primary health care needs. In addition, herbs have provided us some of the very important life saving drugs used in the modern medicine. However among the estimated 2,50,000- 4,00,000 plant species, only 6% have been studied for biological activity and about 15% have been investigated phytochemically.
  • 3. The term “alkaloid” (alkali-like) is commonly used to designate basic heterocyclic nitrogenous compounds of plant origin that are physiologically active. The name “alkaloid” comes from the Arabic word for ash “al- qali”. DEFINATION HISTORY most notorious poisons in the history of civilization. Used by humanity for thousands of years. The first civilizations to use them were probably the ancient Sumerians and Egyptians.it was called a vegetable alkali. HISTORY most notorious poisons in the history of civilization. Used by humanity for thousands of years. The first civilizations to use them were probably the ancient Sumerians and Egyptians.it was called a vegetable alkali. Term alkaloid was coined by Meissner ,a German pharmacist (1819). Derosne (French chemist) isolated Narcotine (1803). Serturner (1803) isolated morphine from opium
  • 4. “Basic nitrogenous compound, contains one or more nitrogen in heterocyclic ring system having marked physiological action on human and animals when use in small quantities””.” OR Naturally occurring nitrogenous substance which is isolated from plants and reacts like bases”
  • 5. FACTS ABOUT MANDRAKE • Already used in Egypt 3500 years ago. • Grecian times considered as an extremely powerful aphrodisiac and fertility enhancer. • Mentioned in the Koran, and strictly forbidden. • The sponge that was given to Jesus on the cross is said to contain Mandragora juice. • played a major role in witchcraft. • Witches prepared mixtures of extracts of henbane (Hyoscyamus niger), deadly nightshade (Atropa belladonna) and mandrake root, to be applied on the skin or on the genitals. Mandrake, also named Mandragora (Mandragora officinarum) Most magic plant. FACTS ABOUT MANDRAKE • Already used in Egypt 3500 years ago. • Grecian times considered as an extremely powerful aphrodisiac and fertility enhancer. • Mentioned in the Koran, and strictly forbidden. • The sponge that was given to Jesus on the cross is said to contain Mandragora juice. • played a major role in witchcraft. • Witches prepared mixtures of extracts of henbane (Hyoscyamus niger), deadly nightshade (Atropa belladonna) and mandrake root, to be applied on the skin or on the genitals.
  • 6. The alkaloids represent a very extensive group of secondary metabolites, with diverse structures, distribution in nature, and important biological activities. ‘‘An alkaloid is a cyclic compound containing nitrogen in a negative oxidation state which is of limited distribution in living organisms’’. This definition includes both alkaloids with nitrogen as part of a heterocyclic system and many exceptions with exocyclic nitrogen, such as colchicines or capsaicin. Generally, the function of secondary metabolites in plants is not determined. Concerning the alkaloids, their protective mechanism against herbivore animals and possibly some parasites is assumed. In contrast, these plants can become the targets for insects that specialize in the alkaloid-producing plants (e.g., bark tree).However, strong physiological effects and the selectivity of some alkaloids present opportunities for utilizing the alkaloids in human medicine. The alkaloids represent a very extensive group of secondary metabolites, with diverse structures, distribution in nature, and important biological activities. ‘‘An alkaloid is a cyclic compound containing nitrogen in a negative oxidation state which is of limited distribution in living organisms’’. This definition includes both alkaloids with nitrogen as part of a heterocyclic system and many exceptions with exocyclic nitrogen, such as colchicines or capsaicin. Generally, the function of secondary metabolites in plants is not determined. Concerning the alkaloids, their protective mechanism against herbivore animals and possibly some parasites is assumed. In contrast, these plants can become the targets for insects that specialize in the alkaloid-producing plants (e.g., bark tree).However, strong physiological effects and the selectivity of some alkaloids present opportunities for utilizing the alkaloids in human medicine.
  • 7. ALKALOID DESCRIPTION • Contains nitrogen -usually derived from an amino acid. • Bitter tasting, generally white solids (exception -nicotine is a brown liquid). • They give a precipitate with heavy metal iodides. • Caffeine, a purine derivative, does not precipitate like most alkaloids. • Alkaloids are basic -they form water soluble salts. Most alkaloids are well-defined crystalline substances which unite with acids to form salts. In plants, they may exist • In the free state. ALKALOID DESCRIPTION • Contains nitrogen -usually derived from an amino acid. • Bitter tasting, generally white solids (exception -nicotine is a brown liquid). • They give a precipitate with heavy metal iodides. • Caffeine, a purine derivative, does not precipitate like most alkaloids. • Alkaloids are basic -they form water soluble salts. Most alkaloids are well-defined crystalline substances which unite with acids to form salts. In plants, they may exist • In the free state.
  • 8. TESTS FOR ALKALOIDS • Most alkaloids are precipitated from neutral or slightly acidic solution by • Dragendorff's reagent (solution of potassium bismuth iodide)orange coloured precipitate. • Mayer's reagent (potassium mercuric iodide solution) Cream coloured precipitate. • Wagner’s reagent (iodine in potassium iodide) red-brown precipitate • Hager's reagent (picric acid) yellow precipitate. TESTS FOR ALKALOIDS • Most alkaloids are precipitated from neutral or slightly acidic solution by • Dragendorff's reagent (solution of potassium bismuth iodide)orange coloured precipitate. • Mayer's reagent (potassium mercuric iodide solution) Cream coloured precipitate. • Wagner’s reagent (iodine in potassium iodide) red-brown precipitate • Hager's reagent (picric acid) yellow precipitate.
  • 9. PHYSICO-CHEMICAL PROPERTIES OF ALKALOIDS • Molecular weight: 100 –900 • Most bases which do not contain O2 are liquid at room temperature (nicotine), while those that do are solids. In rare cases they are coloured. • Most solid bases rotate the plane of polarized light, have high melting points. • Normally are not soluble in water (occasionally slightly soluble). • Soluble in a polar or slightly polar organic solvents. Soluble in concentrated hydro alcoholic solutions. • Naturally occurring chemical compounds containing basic nitrogen atoms • Physiologically active • Insoluble or sparingly soluble in water • Crystalline solids; a few are amorphous PHYSICO-CHEMICAL PROPERTIES OF ALKALOIDS • Molecular weight: 100 –900 • Most bases which do not contain O2 are liquid at room temperature (nicotine), while those that do are solids. In rare cases they are coloured. • Most solid bases rotate the plane of polarized light, have high melting points. • Normally are not soluble in water (occasionally slightly soluble). • Soluble in a polar or slightly polar organic solvents. Soluble in concentrated hydro alcoholic solutions. • Naturally occurring chemical compounds containing basic nitrogen atoms • Physiologically active • Insoluble or sparingly soluble in water • Crystalline solids; a few are amorphous
  • 10. PHYSICAL PROPERTIES a).Most alkaloids are crystalline solid , some are Volatile; --Nicotine , Non-Volatile:- Pilocarpine , Hyoscine b).Majority of alkaloids are colorless but some are colored, e.g.,Colchicine and Berberine are Yellow.Canadine is Orange. c). SOLUBILITY :-difference in solubility used as a base for their isolation and purification from non- alkaloidal bases. The following can be mentioned :- i).Both alkaloidal base and there salts are soluble in alcohol. ii).Genarally bases are soluble in organic solvent and alkaloidal salts are soluble in water. PHYSICAL PROPERTIES a).Most alkaloids are crystalline solid , some are Volatile; --Nicotine , Non-Volatile:- Pilocarpine , Hyoscine b).Majority of alkaloids are colorless but some are colored, e.g.,Colchicine and Berberine are Yellow.Canadine is Orange. c). SOLUBILITY :-difference in solubility used as a base for their isolation and purification from non- alkaloidal bases. The following can be mentioned :- i).Both alkaloidal base and there salts are soluble in alcohol. ii).Genarally bases are soluble in organic solvent and alkaloidal salts are soluble in water.
  • 11. 1).Salt formation Due to their basic character alkaloid reacts with acid to form salt. Strong bases form salt with very weak acid. Weak bases forms salt with strong acid Very weak bases form unstable salts. e.g caffeine , Narcotine , piperine. 2).Effect of heat:-Alkaloids are decomposed by heat, except Strychnine and caffeine (sublimable). 3).Effect of light and Oxygen :  Decomposed when allowed to stand at a temperature above 70o C .for long time.  Decomposition occur rapidly and easily when an alkaloid is in solution than when it is in dry form. CHEMICAL PROPERTIES 1).Salt formation Due to their basic character alkaloid reacts with acid to form salt. Strong bases form salt with very weak acid. Weak bases forms salt with strong acid Very weak bases form unstable salts. e.g caffeine , Narcotine , piperine. 2).Effect of heat:-Alkaloids are decomposed by heat, except Strychnine and caffeine (sublimable). 3).Effect of light and Oxygen :  Decomposed when allowed to stand at a temperature above 70o C .for long time.  Decomposition occur rapidly and easily when an alkaloid is in solution than when it is in dry form.
  • 12. Functions: 1. Poisonous agents protecting the plant against insects and herbivores 2. End products of detoxification reactions representing a metabolic locking up of compounds otherwise harmful to the plant 3. Regulatory growth factors 4. Reserve substances capable of supplying nitrogen or other elements necessary to the plants economy. Functions: 1. Poisonous agents protecting the plant against insects and herbivores 2. End products of detoxification reactions representing a metabolic locking up of compounds otherwise harmful to the plant 3. Regulatory growth factors 4. Reserve substances capable of supplying nitrogen or other elements necessary to the plants economy.
  • 13. • Forms of Alkaloids: • Free bases • Salts with Organic acids e.g. Oxalic, acetic acids • Salts with inorganic acids e.g. Hcl, H2SO4. • Salts with special acids: e.g. Meconic acid in Opium, Quinic acid in Cinchona • Glycosidal form e.g. Solanine in Solanum Distribution in Plant: All Parts e.g. Datura. Barks e.g. Cinchona Seeds e.g. Nux vomica Roots e.g. Aconite Fruits e.g. Black pepper Leaves e.g. Vinca Latex e.g. Opium OTHER SOURCES Castoramine :--- from Canadian beaver (The Canadian beaver is the largest rodent in North America). • Forms of Alkaloids: • Free bases • Salts with Organic acids e.g. Oxalic, acetic acids • Salts with inorganic acids e.g. Hcl, H2SO4. • Salts with special acids: e.g. Meconic acid in Opium, Quinic acid in Cinchona • Glycosidal form e.g. Solanine in Solanum Distribution in Plant: All Parts e.g. Datura. Barks e.g. Cinchona Seeds e.g. Nux vomica Roots e.g. Aconite Fruits e.g. Black pepper Leaves e.g. Vinca Latex e.g. Opium OTHER SOURCES Castoramine :--- from Canadian beaver (The Canadian beaver is the largest rodent in North America). Pyocyanine :-- from Pseudomonas aeruginosa (a bacteria). Muscopyridine :--From Musk of an Deer.
  • 14. OCCURANCE and DISTRIBUTION a).Ranunculaceae : Aconitine (aconite). b). Legumioceae : Physostigmine (physostigma) c).Loganiaceae : Strychnine and Brucine (Nux-vomica). d).Papavaraceae : Morphine, Codeine,Thebaine (Opium). e).Solanaceae : Hyoscine (Belladona). f).Berberidaceae ; Berberine (Berberis). g).Rubiaceae : Quinine and Quinidine (Cinchona). h). Apocyanaceae : Reserpine (Rauwolfia) ,Vincristine and Vinblastine (Vinca). i). Liliaceae : Veriterine (Veratrum). j).Clavicipitaceae : Ergotamine and Ergometrine (Ergot). OCCURANCE and DISTRIBUTION a).Ranunculaceae : Aconitine (aconite). b). Legumioceae : Physostigmine (physostigma) c).Loganiaceae : Strychnine and Brucine (Nux-vomica). d).Papavaraceae : Morphine, Codeine,Thebaine (Opium). e).Solanaceae : Hyoscine (Belladona). f).Berberidaceae ; Berberine (Berberis). g).Rubiaceae : Quinine and Quinidine (Cinchona). h). Apocyanaceae : Reserpine (Rauwolfia) ,Vincristine and Vinblastine (Vinca). i). Liliaceae : Veriterine (Veratrum). j).Clavicipitaceae : Ergotamine and Ergometrine (Ergot).
  • 15. Any method will be a good technique, if it will accelerate: 1.Wetting of the surface of the herb particles. 2. Permeability of cell walls. 3. Rate of dissolution of cell contents in the solvent. 4. Outward diffusion of the solution. EXTRACTION IDEAL PROPERTY OF SOLVENT 1. It should be non-toxic and selective. 2. It should not cause the extract to complex or dissociate. 3. It should be preservative in action. 4. It should promote rapid physiologic absorption of the extract. 5. It should be easily evaporated at low heat. • NOTE:- Alcohol (Ethanol) will meet all above criteria. IDEAL PROPERTY OF SOLVENT 1. It should be non-toxic and selective. 2. It should not cause the extract to complex or dissociate. 3. It should be preservative in action. 4. It should promote rapid physiologic absorption of the extract. 5. It should be easily evaporated at low heat. • NOTE:- Alcohol (Ethanol) will meet all above criteria.
  • 16. STAS-OTTO METHOD The technique involve the distribution of alkaloidal bases between acid or aqueous solution and immiscible organic solvent. MethodI: The powder is treated with alkalis to liberates the free bases that can then be extracted with water immiscible organic solvents. • A). stage1:--Powdered material is moistened with water and mixed with alkali like sodium & potassium carbonate , ammonia, lime. Make a paste with water ,dry ,repowder. • Concept :--Lime(calcium hydroxide),combines with acid , tannins, and other phenolic substances and sets free alkaloids. MethodI: The powder is treated with alkalis to liberates the free bases that can then be extracted with water immiscible organic solvents. • A). stage1:--Powdered material is moistened with water and mixed with alkali like sodium & potassium carbonate , ammonia, lime. Make a paste with water ,dry ,repowder. • Concept :--Lime(calcium hydroxide),combines with acid , tannins, and other phenolic substances and sets free alkaloids.
  • 17. Powdered drug Containing alkaloidal salts Free alkaloids Total extracts Aq. Acid soln Residual organic fraction (Alkaloidal salts) (pigments, fats & weak bases or chloroform soluble alkaloids sulphates) Residual aq. Fraction organic soln (alkaloidal bases) crude alkaloidal mixture Moisten & render alkaline with Na2CO3, lime, NH3 Defatted if necessary Exhaust with org. solvent like CHCl3, ether Conc. & shake with acid like dil. H2SO4 Method 1 Powdered drug Containing alkaloidal salts Free alkaloids Total extracts Aq. Acid soln Residual organic fraction (Alkaloidal salts) (pigments, fats & weak bases or chloroform soluble alkaloids sulphates) Residual aq. Fraction organic soln (alkaloidal bases) crude alkaloidal mixture Make alkaline extract with immisicible solvent Remove solvent
  • 18. B).Stage2:-- Extract the free alkaloids by hot continous percolation with chloroform or any other organic solvents.(Concept :-The free alkaloids dissolve together with other substances soluble in solvent.) C).Stage3:--Agitate the chloroform soln. with successive portion of dil.sulphuric acid separating the aqueous layer before adding the next portion of acid.(Concept :-The alkaloids are converted into alkaloidal sulphates, which being soluble in water,pass into aqeous layer) D).Stage4:--Make the mixed aqueous liquid alkaline with ammonia, collect the precipitate that forms, wash with water and dry. (Concept :- Ammonia decomposes the alkaloidal sulphates forming ammonium sulphates ,soluble in water ,and the free alkaloid which being practically insoluble in water is precipitated) B).Stage2:-- Extract the free alkaloids by hot continous percolation with chloroform or any other organic solvents.(Concept :-The free alkaloids dissolve together with other substances soluble in solvent.) C).Stage3:--Agitate the chloroform soln. with successive portion of dil.sulphuric acid separating the aqueous layer before adding the next portion of acid.(Concept :-The alkaloids are converted into alkaloidal sulphates, which being soluble in water,pass into aqeous layer) D).Stage4:--Make the mixed aqueous liquid alkaline with ammonia, collect the precipitate that forms, wash with water and dry. (Concept :- Ammonia decomposes the alkaloidal sulphates forming ammonium sulphates ,soluble in water ,and the free alkaloid which being practically insoluble in water is precipitated)
  • 19. Method II: The powder is extracted with water soluble organic solvents such as MeOH or EtOH which are good solvents for both salts and free bases. And the resultant extract is submitted to same process as that of method1. ADVANTAGE :-- This method requires no alkali, gives good penetration of drug ,and Economical. Method II: The powder is extracted with water soluble organic solvents such as MeOH or EtOH which are good solvents for both salts and free bases. And the resultant extract is submitted to same process as that of method1. ADVANTAGE :-- This method requires no alkali, gives good penetration of drug ,and Economical.
  • 20. Method III The powdered material is extracted with water or aqueous alcohol containing dilute acid. Disadvatage:-- Cheap but not used because it also extract impurities like sugar, mucilage, tannins, colouring matter. Method III The powdered material is extracted with water or aqueous alcohol containing dilute acid. Disadvatage:-- Cheap but not used because it also extract impurities like sugar, mucilage, tannins, colouring matter.
  • 21. EXTRACTION OF ALKALOIDS Plant material and solvent Extract Concentration Acidified Extract (Alk. as salts) Organic solvent dissove Impurities Acidification Alkalinization Alkaline aqueous layer Organic solvent dissove Alkaloids Plant material and solvent Extract Concentration Acidified Extract (Alk. as salts) Organic solvent dissove Impurities Acidification Alkalinization Alkaline aqueous layer Organic solvent dissove Alkaloids
  • 22. Extraction of liquid alkaloids 1-Plant powder is extracted directly with acidified water 2-Plant powder is extracted with acidified alcoholic or a hydro alcoholic solution. This is then followed by distillation under vacuum (eliminates that alcohol, leaving behind and acidic aqueous solution of alkaloid salts) 1-Plant powder is extracted directly with acidified water 2-Plant powder is extracted with acidified alcoholic or a hydro alcoholic solution. This is then followed by distillation under vacuum (eliminates that alcohol, leaving behind and acidic aqueous solution of alkaloid salts)
  • 23. PURIFICATION OF ALKALOIDS 1.DIRECT CRYSTALLISATION FROM SOLVENT. 2.STEAM DISTILLATION. 3. CHROMATOGRAPHY TECHNIQUES. 4. GRADIENT pH TECHNIQUES PURIFICATION OF ALKALOIDS 1.DIRECT CRYSTALLISATION FROM SOLVENT. 2.STEAM DISTILLATION. 3. CHROMATOGRAPHY TECHNIQUES. 4. GRADIENT pH TECHNIQUES • GRADIENT pH TECHNIQUES • Though alkaloids are basic in nature, there are variations in the extent in the basicity of various alkaloids of the same plant • Depending on this character, the crude alkaloidal mixture is dissolved in 2% tartaric acid solution and extracted with benzene so that the first fraction contains natural and/or very weakly basic alkaloids. • pH of the aqueous solution is increased gradually by 0.5 increment upto pH 9, and extraction is carried out at each pH level with organic solvent, by this way alkaloids with different basicity are extracted. • Strongly basic alkaloids are extracted at the end. • GRADIENT pH TECHNIQUES • Though alkaloids are basic in nature, there are variations in the extent in the basicity of various alkaloids of the same plant • Depending on this character, the crude alkaloidal mixture is dissolved in 2% tartaric acid solution and extracted with benzene so that the first fraction contains natural and/or very weakly basic alkaloids. • pH of the aqueous solution is increased gradually by 0.5 increment upto pH 9, and extraction is carried out at each pH level with organic solvent, by this way alkaloids with different basicity are extracted. • Strongly basic alkaloids are extracted at the end.
  • 24. • PRECIPITATION REACTION : 1- Mayer's or Valser's reagent ( Potassium mercuric iodide) gives white or yellow color mostly amorphous precipitates with alkaloids,except the purine bases, ephedrine Colchicine and ricinine . Mercuric chloride 1.36 Potassium iodide 5.00 g Water to make 100 ml. 2. Wagner's reagent (Iodine- potassium iodide):- It produces brown or reddish- brown precipitates with all alkaloids. Iodine 1.3 g Potassium iodide 2.0 g Water to make 100 ml • PRECIPITATION REACTION : 1- Mayer's or Valser's reagent ( Potassium mercuric iodide) gives white or yellow color mostly amorphous precipitates with alkaloids,except the purine bases, ephedrine Colchicine and ricinine . Mercuric chloride 1.36 Potassium iodide 5.00 g Water to make 100 ml. 2. Wagner's reagent (Iodine- potassium iodide):- It produces brown or reddish- brown precipitates with all alkaloids. Iodine 1.3 g Potassium iodide 2.0 g Water to make 100 ml 3.Dragendorff's or Krauts reagent ( potassium iodide+ bithmus nitrate):- It produces orange red precipitate which is usually amorphous. Bismuth nitrate 8.0 g Nitric acid 20.5 g Potassium iodide 27.2 g Water to 100 ml
  • 25. 4. Hager's reagent (picric acid):- Gives yellow crystalline precipitate. 5. Tannic acid solution: (5%w/v) .:--gives buff colored ppt. which is soluble in dil.acid or ammonia. 6.Ammonium reineckate solution : 2% solution, produces precipitates with heterocyclic nitrogen alkaloids, with quaternary and some tertiary amines. COLOUR REACTION A). Van-Urks test: (Para-dimethyl-amino-benzaldehyde + sulphuric acid)-- (for Egot alkaloids).-gives Blue colour. B). Vitali-Morin test:-- test for solanceous alkaloids gives violet colour when treated with conc. nitric acid and alcoholic KOH. Mechanism :-- These color tests usually depend upon dehydration or oxidation of the alkaloid with a resultant characteristic color. COLOUR REACTION A). Van-Urks test: (Para-dimethyl-amino-benzaldehyde + sulphuric acid)-- (for Egot alkaloids).-gives Blue colour. B). Vitali-Morin test:-- test for solanceous alkaloids gives violet colour when treated with conc. nitric acid and alcoholic KOH. Mechanism :-- These color tests usually depend upon dehydration or oxidation of the alkaloid with a resultant characteristic color.
  • 26. METHOD FOR STRUCTURE ELUCIDATION  U.V. Spectroscopy  IR Spectroscopy  Nuclear Magnetic resonance spectroscopy  Mass spectroscopy  X-Ray diffraction METHOD FOR STRUCTURE ELUCIDATION  U.V. Spectroscopy  IR Spectroscopy  Nuclear Magnetic resonance spectroscopy  Mass spectroscopy  X-Ray diffraction
  • 27. CLASSIFICATION 1. The pharmacological action (biological activity). 2. The chemical structure (heterocyclic or no-heterocyclic type of ring structure). 3. The biochemical origin (biosynthetic pathway of production in the plant). 4. The taxonomical origin (plant families rich in alkaloids). CLASSIFICATION 1. The pharmacological action (biological activity). 2. The chemical structure (heterocyclic or no-heterocyclic type of ring structure). 3. The biochemical origin (biosynthetic pathway of production in the plant). 4. The taxonomical origin (plant families rich in alkaloids).
  • 28. CLASSIFICATION BASED ON THE RING STRUCTURE OR NUCLEUS Pyridine-Piperidine ----Lobiline Tropane---- Atropine Quinoline ----Quinine Isoquinoline ---- Emetine Indole--- Reserpine , Vincristine. Imidazole --- Pilocarpine Steroid ---- Solanidine Alkaloidal amines ---- Ephedrine Purine --- Caffeine , Theophylline CLASSIFICATION BASED ON THE RING STRUCTURE OR NUCLEUS Pyridine-Piperidine ----Lobiline Tropane---- Atropine Quinoline ----Quinine Isoquinoline ---- Emetine Indole--- Reserpine , Vincristine. Imidazole --- Pilocarpine Steroid ---- Solanidine Alkaloidal amines ---- Ephedrine Purine --- Caffeine , Theophylline
  • 29. CLASSIFICATION BASED ON PHARMACOLOGICAL ACTIVITY 1. Analgesics and narcotics: Morphine and codeine. 2. CNS stimulants : Caffeine and strychnine. 3. Anticancer:Vincristine, vinblastine and taxol. 4. Mydriatics:Atropine. 5. Anti-asthmatics :Ephedrine. 6. Anti- tussive: Codeine. 7. Expectorants: Lobeline. 8. Anti- hypertensive:Reserpine. 9. Smooth muscle relaxants:Atropine and papaverine 10. Skeletal muscle relaxants: d- tubocurarine. 11. Anthelmintics:Pelletierine and arecoline. 12. Antiparasitics: Quinine and emetine. 1. Analgesics and narcotics: Morphine and codeine. 2. CNS stimulants : Caffeine and strychnine. 3. Anticancer:Vincristine, vinblastine and taxol. 4. Mydriatics:Atropine. 5. Anti-asthmatics :Ephedrine. 6. Anti- tussive: Codeine. 7. Expectorants: Lobeline. 8. Anti- hypertensive:Reserpine. 9. Smooth muscle relaxants:Atropine and papaverine 10. Skeletal muscle relaxants: d- tubocurarine. 11. Anthelmintics:Pelletierine and arecoline. 12. Antiparasitics: Quinine and emetine.
  • 30. CLASSIFICATION BASED ON ROBINSON ( BASED ON BIOSYNTHESIS)  Ornithine alkaloids ---- Pyrolline alkaloids (Nicotine)  Lysine alkaloids ---- Anabasine , Lupinine  Phenylalanine alkaloids ---- l-Hyoscyamine , Mescaline  Tryptophan alkaloids ---- Strychnine , Ergotamine , Tyrosine alkaloids ---- Morphine , Papaverine , Codeine Terpenoid alkaloids ----- Squalene , Carotenoids  Purine alkaloids ---- Caffeine CLASSIFICATION BASED ON ROBINSON ( BASED ON BIOSYNTHESIS)  Ornithine alkaloids ---- Pyrolline alkaloids (Nicotine)  Lysine alkaloids ---- Anabasine , Lupinine  Phenylalanine alkaloids ---- l-Hyoscyamine , Mescaline  Tryptophan alkaloids ---- Strychnine , Ergotamine , Tyrosine alkaloids ---- Morphine , Papaverine , Codeine Terpenoid alkaloids ----- Squalene , Carotenoids  Purine alkaloids ---- Caffeine
  • 31. Classification of Alkaloids • True (Typical) alkaloids that are derived from amino acids and have nitrogen in a heterocyclic ring. e.g. Atropine • Proto alkaloids that are derived from amino acids and do not have nitrogen in a heterocyclic ring. e.g. Ephedrine • Pseudo alkaloids that are not derived from amino acids but have nitrogen in a heterocyclic ring. e.g. Caffeine • False alkaloids are non alkaloids give false positive reaction with alkaloidal reagents. Classification of Alkaloids • True (Typical) alkaloids that are derived from amino acids and have nitrogen in a heterocyclic ring. e.g. Atropine • Proto alkaloids that are derived from amino acids and do not have nitrogen in a heterocyclic ring. e.g. Ephedrine • Pseudo alkaloids that are not derived from amino acids but have nitrogen in a heterocyclic ring. e.g. Caffeine • False alkaloids are non alkaloids give false positive reaction with alkaloidal reagents.
  • 32. Hegnauer's classification • 1)."True alkaloids", which contain nitrogen in the heterocyclic ring and originate from amino acids. examples are atropine, nicotine and morphine, Quinine. • All the heterocyclic alkaloids are true alkaloids. The true alkaloids should have following characters: a)It should be sufficiently toxic. b)should have marked physiological activity. c)should be basic in nature. d)Nitrogen should be present in a heterocyclic ring. e)Should be derived from amino acids. f)should occur in plant as salt of organic acids. Hegnauer's classification • 1)."True alkaloids", which contain nitrogen in the heterocyclic ring and originate from amino acids. examples are atropine, nicotine and morphine, Quinine. • All the heterocyclic alkaloids are true alkaloids. The true alkaloids should have following characters: a)It should be sufficiently toxic. b)should have marked physiological activity. c)should be basic in nature. d)Nitrogen should be present in a heterocyclic ring. e)Should be derived from amino acids. f)should occur in plant as salt of organic acids.
  • 33. 2)Proto alkaloids • These are also called Non heterocyclic or Atypical alkaloids or Biological amines. • These are less commonly found in nature. • These molecules have a nitrogen atom which is not a part of any ring system. • Examples of these include ephedrine, colchicine, erythromycin and taxol etc. • Table below shows the chemical structure and biological significance of these compounds • Examples include:- mescaline, adrenaline and ephedrine • These are also called Non heterocyclic or Atypical alkaloids or Biological amines. • These are less commonly found in nature. • These molecules have a nitrogen atom which is not a part of any ring system. • Examples of these include ephedrine, colchicine, erythromycin and taxol etc. • Table below shows the chemical structure and biological significance of these compounds • Examples include:- mescaline, adrenaline and ephedrine
  • 34. 3.Pseudo-Alkaloids:--They do not derived from amino acid but having nitrogen in heterocyclic ring . They do not show many of the typical characters of alkaloids , but give standard qualitative test for alkaloids. e.g. steroidal alkaloids:-conessine Purine bases :-- Caffeiene
  • 35. Name Structure Biological Significance Ephedrine Adrenergic agent- used for asthma and hay fever Colchicine Relieves gout Erythromycin Antibiotic Name Structure Biological Significance Ephedrine Adrenergic agent- used for asthma and hay fever Colchicine Relieves gout Erythromycin Antibiotic
  • 36. Taxol (Paclitaxel) Used in the treatment of ovarian cancer, breast cancer and non-small cell lung cancer Taxol (Paclitaxel) Used in the treatment of ovarian cancer, breast cancer and non-small cell lung cancer
  • 37. B. Heterocyclic Alkaloids or Typical Alkaloids: • Structurally these have the nitrogen as a part of a cyclic ring system. • These are more commonly found in nature. • Heterocyclic alkaloids are further subdivided into 14 groups based on the ring structure containing the nitrogen B. Heterocyclic Alkaloids or Typical Alkaloids: • Structurally these have the nitrogen as a part of a cyclic ring system. • These are more commonly found in nature. • Heterocyclic alkaloids are further subdivided into 14 groups based on the ring structure containing the nitrogen
  • 38. No. Heterocycle Example 1. Pyrrole and Pyrrolidine Hygrine, Stachydrine 2. Pyrrolizidine Senecionine, Symphitine, Echimidine, Seneciphylline No. Heterocycle Example 1. Pyrrole and Pyrrolidine Hygrine, Stachydrine 2. Pyrrolizidine Senecionine, Symphitine, Echimidine, Seneciphylline
  • 39. 3. Pyridine and Piperidine Lobeline, Nicotine, Piperine, Conine, Trigonelline 4. Tropane (piperidine/N-methyl- pyrrolidine) Cocaine, Atropine, Hyoscyamine, Hyoscine 5. Quinoline Quinine, Quinidine, Cinchonine, Cinchonidine 3. Pyridine and Piperidine Lobeline, Nicotine, Piperine, Conine, Trigonelline 4. Tropane (piperidine/N-methyl- pyrrolidine) Cocaine, Atropine, Hyoscyamine, Hyoscine 5. Quinoline Quinine, Quinidine, Cinchonine, Cinchonidine
  • 40. 6. Isoquinoline Morphine, Emetine, Papaverine, Narcotine, Tubocurarine, Codeine 7. Aporphine (reduced isoquinoline/naphthalene) Boldine 8. Quinolizidine Lupanine, Cytisine, Laburnine, Sparteine 6. Isoquinoline Morphine, Emetine, Papaverine, Narcotine, Tubocurarine, Codeine 7. Aporphine (reduced isoquinoline/naphthalene) Boldine 8. Quinolizidine Lupanine, Cytisine, Laburnine, Sparteine
  • 41. 9. Indole or Benzopyrole Ergometrine, Vinblastine, Vincristine, Strychnine, Brucine, Ergotamine, Yohimbine, Reserpine, Serpentine, Physostigmine 10. Indolizidine Castanospermine, Swainsonine 11. Imidazole or glyoxaline Pilocarpine, Pilosine 9. Indole or Benzopyrole Ergometrine, Vinblastine, Vincristine, Strychnine, Brucine, Ergotamine, Yohimbine, Reserpine, Serpentine, Physostigmine 10. Indolizidine Castanospermine, Swainsonine 11. Imidazole or glyoxaline Pilocarpine, Pilosine
  • 42. 12. Purine (pyrimidine/imidazole) Caffeine, Theobromine 13. Steroidal (some combined as glycosides)* Conessine, Solanidine 14. Terpenoid* Aconitine, lycaconitine, Aconine *Note- Steroidal and terpenoid classes are also treated as separate classes or along with glycosides. 12. Purine (pyrimidine/imidazole) Caffeine, Theobromine 13. Steroidal (some combined as glycosides)* Conessine, Solanidine 14. Terpenoid* Aconitine, lycaconitine, Aconine *Note- Steroidal and terpenoid classes are also treated as separate classes or along with glycosides.
  • 43. SYSTAMATIC PHARMACOGNOSTIC STUDY OF ALKALOIDS SYSTAMATIC PHARMACOGNOSTIC STUDY OF ALKALOIDS
  • 44. Biological source : It is the Dried bark of cultivated trees of Cinchona officinalis belonging in to the family Rubiaceae.(NLT 6% Alkaloids) Synonyms: Jesuil’ bark, Peruvian bark Macroscopical characters: Odour - Slight & characteristic Taste - Astringent & intensely bitter Stem bark Colour: (outer surface) Dull to brown or grey pale(inner surface) yellowish brown to reddish brown  Fracture- Short & fibrous  Size- 30cm long, 2-6mm thick Root bark- Colour- outer & inner surfaces are similar Size- 207cm long CINCHONA Macroscopical characters: Odour - Slight & characteristic Taste - Astringent & intensely bitter Stem bark Colour: (outer surface) Dull to brown or grey pale(inner surface) yellowish brown to reddish brown  Fracture- Short & fibrous  Size- 30cm long, 2-6mm thick Root bark- Colour- outer & inner surfaces are similar Size- 207cm long Other features: Number of transverse cracks are present Powder is Yellow in colour, 12mm diameter ,1.5mm thick
  • 45. MICROSCOPY Cinchona exhibits following Histological characters Cork cells are thin walled. Cortex consists of secretary channels and phloem fibres. Medullary rays are radially arranged. Idioblasts of calcium oxalate is the specific characteristic of cinchona bark. Starch grains are present in parenchymatous tissue. Medullary rays are 2 to 3 walled. Cinchona exhibits following Histological characters Cork cells are thin walled. Cortex consists of secretary channels and phloem fibres. Medullary rays are radially arranged. Idioblasts of calcium oxalate is the specific characteristic of cinchona bark. Starch grains are present in parenchymatous tissue. Medullary rays are 2 to 3 walled. T.S of Cinchona bark
  • 46. Cultivation and collection Most of the cinchona found in tropical & sub tropical regions about 1000-3000 m. Rainfall required are uniform 250-380 cm/year .Favorable growth is achieved at 60- 75ºF. Cinchona requires light well drained forest soil with rich organic matter. The acidic soil having a PH of 4 -5.6 and small amount of nitrogen imp for favorable growth. It requires high humidity and slopping situation, protection from wind. The propagation is done by seeds or budding or layering. The seeds of cinchona are very small, light in weight ( 1 gm = 3500 seeds). Germination takes place in 3-6 weeks. The seedlings with 2 pairs of leaves are transplanted and space of 6 – 10 cm, at a distance of 2 x 2 meters . Plants of 4 to 20 years are selected for harvesting, bark is collected by coppicing method, dried at 175 ºF.(care to be take to avoid fermentation) . Cultivation and collection Most of the cinchona found in tropical & sub tropical regions about 1000-3000 m. Rainfall required are uniform 250-380 cm/year .Favorable growth is achieved at 60- 75ºF. Cinchona requires light well drained forest soil with rich organic matter. The acidic soil having a PH of 4 -5.6 and small amount of nitrogen imp for favorable growth. It requires high humidity and slopping situation, protection from wind. The propagation is done by seeds or budding or layering. The seeds of cinchona are very small, light in weight ( 1 gm = 3500 seeds). Germination takes place in 3-6 weeks. The seedlings with 2 pairs of leaves are transplanted and space of 6 – 10 cm, at a distance of 2 x 2 meters . Plants of 4 to 20 years are selected for harvesting, bark is collected by coppicing method, dried at 175 ºF.(care to be take to avoid fermentation) .
  • 47. EXTRACTION Step 1: The cinchona bark is dried, powdered, sieved and treated with calcium oxide (slaked lime), NaOH solution (10% w/v) and water and kept as such for 6-8 hours. Step II: The resulting mixture is treated with benzene in sufficient quantity and refluxed for 12-16 hours. The mixture is then filtered while it is hot. Step III: The hot filtrate is extracted successively with 6N. sulphuric acid. The mixture of alkaloidal bisulphate is heated up to 90°C and maintained at this temperature up to 20-30 m Step IV: The resulting solution is cooled to room temperature and made alkaline by the addition of solid pure sodium carbonate till a pH 6.5 is attained. Step V: The alkaloidal sulphate solution thus obtained is treated with sufficient quantity of activated charcoal powder (1g per 1L), boil, shake vigorously and filter. Step VI: Cool the hot filtrate slowly in a refrigerator (2-10°C) overnight and again filter. Collect the residue and the filtrate separately. Step VII: The residue (or precipitate) of quinine sulphate is boiled with water and made alkaline by adding cautiously solid sodium carbonate. The resulting precipitate is that of quinine. EXTRACTION Step 1: The cinchona bark is dried, powdered, sieved and treated with calcium oxide (slaked lime), NaOH solution (10% w/v) and water and kept as such for 6-8 hours. Step II: The resulting mixture is treated with benzene in sufficient quantity and refluxed for 12-16 hours. The mixture is then filtered while it is hot. Step III: The hot filtrate is extracted successively with 6N. sulphuric acid. The mixture of alkaloidal bisulphate is heated up to 90°C and maintained at this temperature up to 20-30 m Step IV: The resulting solution is cooled to room temperature and made alkaline by the addition of solid pure sodium carbonate till a pH 6.5 is attained. Step V: The alkaloidal sulphate solution thus obtained is treated with sufficient quantity of activated charcoal powder (1g per 1L), boil, shake vigorously and filter. Step VI: Cool the hot filtrate slowly in a refrigerator (2-10°C) overnight and again filter. Collect the residue and the filtrate separately. Step VII: The residue (or precipitate) of quinine sulphate is boiled with water and made alkaline by adding cautiously solid sodium carbonate. The resulting precipitate is that of quinine.
  • 48. CHEMICAL CONSTITUENTS Cinchona bark contain many alkaloids the majors are: 1- Quinine and Quinidine. 2- Cinchonine and Cinchonidine. Cinchona alkaloids are present as salts with Quinic and Cincho tannic acids. They are diacidic bases form two types of salts: 1- Neutral salts (Monoacidic) (less water soluble. 2- Acidic salts (Diacidic) water soluble. Both Quinine and Quinidine, Cinchonine and Cinchonidine are Diastereoisomers. Each pair differs in the stereochemistry at C-8 and C-9. CHEMICAL CONSTITUENTS Cinchona bark contain many alkaloids the majors are: 1- Quinine and Quinidine. 2- Cinchonine and Cinchonidine. Cinchona alkaloids are present as salts with Quinic and Cincho tannic acids. They are diacidic bases form two types of salts: 1- Neutral salts (Monoacidic) (less water soluble. 2- Acidic salts (Diacidic) water soluble. Both Quinine and Quinidine, Cinchonine and Cinchonidine are Diastereoisomers. Each pair differs in the stereochemistry at C-8 and C-9. N N H3CO HO H H N N H3CO HO H H 89 Quinine Quinidine
  • 49. Tests for identification may be identified either by a series of Colour Tests 1- Fluorescence test: Solution of the alkaloid in oxygenated acids (e.g H2SO4, HNO3 or phosphoric acid)  blue fluorescence (+ ve with quinine and quinidine). 2- Thalleoquine test: Aqueous solution of the alkaloidal salt + Br2 /H2O (few drops till the appearance of yellow color) + NH4OH  emerald green color (+ ve with quinine and quinidine). 3- Rosequin test (Erythroquinine test): Aqueous solution of the alkaloidal salt + dil HCl + Br2 /H2O (few drops till the appearance of yellow color) + CHCl3 + pot. Ferrocyanide + NH4OH  red color in the CHCl3 layer (+ ve with quinine and quinidine). Tests for identification may be identified either by a series of Colour Tests 1- Fluorescence test: Solution of the alkaloid in oxygenated acids (e.g H2SO4, HNO3 or phosphoric acid)  blue fluorescence (+ ve with quinine and quinidine). 2- Thalleoquine test: Aqueous solution of the alkaloidal salt + Br2 /H2O (few drops till the appearance of yellow color) + NH4OH  emerald green color (+ ve with quinine and quinidine). 3- Rosequin test (Erythroquinine test): Aqueous solution of the alkaloidal salt + dil HCl + Br2 /H2O (few drops till the appearance of yellow color) + CHCl3 + pot. Ferrocyanide + NH4OH  red color in the CHCl3 layer (+ ve with quinine and quinidine).
  • 50. Uses: 1. It is frequently employed as a flavour in carbonated beverages. 2. It is used as an Antimalarial agent. 3. It is also employed as a Skeletal muscle relaxant. 4. It has been used to treat Hemorrhoids and varicose veins. 5. Quinine is also used as a Oxytocic agent. 6. Quinine is supposed to be Prophylactic for flu. Dose: Cinchona powder-0.3-1 g Quinine sulphate - 1 g daily for 2 days 600 mg daily 5 days quinidine sulphate 0.2 to 0.4 g every 2 – 4 hrs total dose of 3 g daily in atrial fibrillation. Uses: 1. It is frequently employed as a flavour in carbonated beverages. 2. It is used as an Antimalarial agent. 3. It is also employed as a Skeletal muscle relaxant. 4. It has been used to treat Hemorrhoids and varicose veins. 5. Quinine is also used as a Oxytocic agent. 6. Quinine is supposed to be Prophylactic for flu. Dose: Cinchona powder-0.3-1 g Quinine sulphate - 1 g daily for 2 days 600 mg daily 5 days quinidine sulphate 0.2 to 0.4 g every 2 – 4 hrs total dose of 3 g daily in atrial fibrillation.
  • 51. ERGOT Biological source: ergot is the dried sclerotium of the fungus Claviceps purpurea (Fries) belonging to the family Clavicipitaceae developed in the ovary of rye, Secale cereale (Germinae/ Poaceae). Ergot is a fungal disease very commonly and widely observed on a good number of wild as well as cultivated grasses, and is produced by different species of claviceps. This particular disease is usually characterized by the formation of hard and seed like ‘ergots’ in place of the normal seeds. However, these specific structures are frequently termed as sclerotia, which represent the ‘resting stage’ of the fungus. The generic name, ‘claviceps’, usually refers to the club-like nature of the sclerotium, where as purpurea signifies its purple colour. As these sclerotia are elongated and somewhat pointed in shape and appearance, hence the common name of spurred rye has been assigned to the drug. Synonyms: Ergot; Rye Ergot. spurred rye Ergot is a fungal disease very commonly and widely observed on a good number of wild as well as cultivated grasses, and is produced by different species of claviceps. This particular disease is usually characterized by the formation of hard and seed like ‘ergots’ in place of the normal seeds. However, these specific structures are frequently termed as sclerotia, which represent the ‘resting stage’ of the fungus. The generic name, ‘claviceps’, usually refers to the club-like nature of the sclerotium, where as purpurea signifies its purple colour. As these sclerotia are elongated and somewhat pointed in shape and appearance, hence the common name of spurred rye has been assigned to the drug.
  • 53. Categories of ergot alkaloids: four main categories of ergot alkaloids which may be distinguished, namely (a) Clavine alkaloids. (b) Lysergic acids. (c) Lysergic acid amides. (d) Ergot peptide alkaloids. There are ten Ergot peptide alkaloids which are: Ergotamine, Ergosine, Ergocristine, Ergocryptine, Ergocornine, Ergotaminine, Ergosinine, Ergocristinine, Ergocryptinine, and Ergocorninine Categories of ergot alkaloids: four main categories of ergot alkaloids which may be distinguished, namely (a) Clavine alkaloids. (b) Lysergic acids. (c) Lysergic acid amides. (d) Ergot peptide alkaloids. There are ten Ergot peptide alkaloids which are: Ergotamine, Ergosine, Ergocristine, Ergocryptine, Ergocornine, Ergotaminine, Ergosinine, Ergocristinine, Ergocryptinine, and Ergocorninine The poisonous properties of ergots in grain, specifically rye, for animal as well as human consumption, purposefully and unknowingly, have long been recognized. The dreadful causative agents are collectively termed as the ‘ergot alkaloids’, containing essentially an Indole nucleus.
  • 54. Cultivation The life cycle of the fungus, claviceps purpurea, which is a parasite, passes through the following characteristics stages The genus Claviceps is a group of phytopathogenic ascomycetes that is composed of approximately 36 different species of filamentous fungi. Ergot is a French word derived from argot (a spur) and represents the dark brown, horn-shaped pegs that project from ripening ears of rye in place of rye grains. These tuberous projections are collected before and during harvesting or are separated from the threshed rye. In a histologic sense, these bodies consist of compactly inter woven hyphae of the filamentous fungus Claviceps purpurea but biologically these compact grains are designated as sclerotia, the form in which the fungus passes the winter. Cultivation The life cycle of the fungus, claviceps purpurea, which is a parasite, passes through the following characteristics stages The genus Claviceps is a group of phytopathogenic ascomycetes that is composed of approximately 36 different species of filamentous fungi. Ergot is a French word derived from argot (a spur) and represents the dark brown, horn-shaped pegs that project from ripening ears of rye in place of rye grains. These tuberous projections are collected before and during harvesting or are separated from the threshed rye. In a histologic sense, these bodies consist of compactly inter woven hyphae of the filamentous fungus Claviceps purpurea but biologically these compact grains are designated as sclerotia, the form in which the fungus passes the winter.
  • 55. 1. The parasitic life cycle of the ergot fungi begins in the spring, with wind-borne ascopores landing on susceptible host plants. 2. Hyphae invade and colonize the ovary, producing masses of anamorphic spores that are exuded into a syrupy fluid (honeydew). 3. Insect vectors, rain splash, or head-to-head contact transfer this honeydew to other blooming florets, allowing the spread of the ergot fungi in a field. 4. When the sclerotia begin to form, production of honeydew and condiation cease, and the sclerotia mature in about 5 weeks. 5. The sclerotia are considered as the early stage of sexual differentiation of Claviceps. In autumn, the ripe pigmented sclerotium leaves the spike and falls to the ground, ultimately producing asci and non seprate ascospores, thereby completing the cycle. LIFE CYCLE OF ERGOT 1. The parasitic life cycle of the ergot fungi begins in the spring, with wind-borne ascopores landing on susceptible host plants. 2. Hyphae invade and colonize the ovary, producing masses of anamorphic spores that are exuded into a syrupy fluid (honeydew). 3. Insect vectors, rain splash, or head-to-head contact transfer this honeydew to other blooming florets, allowing the spread of the ergot fungi in a field. 4. When the sclerotia begin to form, production of honeydew and condiation cease, and the sclerotia mature in about 5 weeks. 5. The sclerotia are considered as the early stage of sexual differentiation of Claviceps. In autumn, the ripe pigmented sclerotium leaves the spike and falls to the ground, ultimately producing asci and non seprate ascospores, thereby completing the cycle.
  • 56. 1.Sphacelia or Honeydew or Asexual stage The rye plant becomes infected by the spores of the fungus in the spring session. The spores are carried out by the wind or by insect to the flowers and collected at the base of the young ovary where moisture is present. There germination of the spores takes place. A filamentous hyphae is formed which enters into the wall of the ovary by enzymatic action. A soft, white mass over the surface of ovary is formed which is known as honeydew, is secreted during the sphacelia stage which contains reducing sugars. From the ends of some hyphae small oval conidiophores (asexual spores) are abstracted which remain suspended on honeydew. The sweet taste of honeydew attracts some insect like ants and weevils. Insects suck the sweet liquid and carry the conidiophores to the plants and spread the fungal infection in the rye plants. 1.Sphacelia or Honeydew or Asexual stage The rye plant becomes infected by the spores of the fungus in the spring session. The spores are carried out by the wind or by insect to the flowers and collected at the base of the young ovary where moisture is present. There germination of the spores takes place. A filamentous hyphae is formed which enters into the wall of the ovary by enzymatic action. A soft, white mass over the surface of ovary is formed which is known as honeydew, is secreted during the sphacelia stage which contains reducing sugars. From the ends of some hyphae small oval conidiophores (asexual spores) are abstracted which remain suspended on honeydew. The sweet taste of honeydew attracts some insect like ants and weevils. Insects suck the sweet liquid and carry the conidiophores to the plants and spread the fungal infection in the rye plants.
  • 57. 2.Sclerotinum or Ascigerous or Sexual stage During the sphacelia stage the hyphae enter only wall of the ovary. On further development they penetrate into deeper parts, feed on the ovarian tissues and replace it by a compact, dark purple hard tissue known as pseudo parenchyma. It forms the sclerotinum or resting state of the fungus. During summer the sclerotinum or ergot increases in size and projects on the rye, showing sphacelia remains at its apex. It is collected at this stage by hands or machine and used as a drug. Ergot is then dried to remove moisture. 3.Ascospores stage If ergot is not collected, it falls on the ground. In the next spring session they produce stalked projections known as stromata which have globular heads. In the inner surface of the heads there are a large number of flask shaped pockets known as perithesia. Each of these perithesia contains many sacs (asci) which possesses eight of the threads-like ascospores. 2.Sclerotinum or Ascigerous or Sexual stage During the sphacelia stage the hyphae enter only wall of the ovary. On further development they penetrate into deeper parts, feed on the ovarian tissues and replace it by a compact, dark purple hard tissue known as pseudo parenchyma. It forms the sclerotinum or resting state of the fungus. During summer the sclerotinum or ergot increases in size and projects on the rye, showing sphacelia remains at its apex. It is collected at this stage by hands or machine and used as a drug. Ergot is then dried to remove moisture. 3.Ascospores stage If ergot is not collected, it falls on the ground. In the next spring session they produce stalked projections known as stromata which have globular heads. In the inner surface of the heads there are a large number of flask shaped pockets known as perithesia. Each of these perithesia contains many sacs (asci) which possesses eight of the threads-like ascospores.
  • 59.
  • 60. Macroscopical characters (i) Size: Sclerotium is about 1-4 cm long, 2-7 mm broad. (ii) Shape: Fusiform, slightly curved, Subcylendrical, tapering at the both ends. (iii) Outer surface: Darks or violet-black in colour is longitudinal furrows and sometimes small transverse cracks. (iv) Fracture surface: Thin, dark outer layer a whitish or pinkish-white central zone of pseudo parenchyma in which darker lines radiate from the centre. (v) Odour: Characteristics. (vi) Taste:Unpleasant. Macroscopical characters (i) Size: Sclerotium is about 1-4 cm long, 2-7 mm broad. (ii) Shape: Fusiform, slightly curved, Subcylendrical, tapering at the both ends. (iii) Outer surface: Darks or violet-black in colour is longitudinal furrows and sometimes small transverse cracks. (iv) Fracture surface: Thin, dark outer layer a whitish or pinkish-white central zone of pseudo parenchyma in which darker lines radiate from the centre. (v) Odour: Characteristics. (vi) Taste:Unpleasant.
  • 61. Microscopical characters The outermost layer of the sclerotium is made up of flattened thin walled cells While inner layer is made up of dense pseudo parenchymatous cells composed of chitin The mycelial cells are round or oval , thick . These are also composed of fixed oils Sclerotium doesn’t contains any materials like starch grains, calcium oxalate crystals, and lignified cells. The outermost layer of the sclerotium is made up of flattened thin walled cells While inner layer is made up of dense pseudo parenchymatous cells composed of chitin The mycelial cells are round or oval , thick . These are also composed of fixed oils Sclerotium doesn’t contains any materials like starch grains, calcium oxalate crystals, and lignified cells. T.S of sclerotium of Ergot
  • 62. 1. The powdered dried ergot is first defatted with n-hexane or petroleum ether (40-60°) 2. The marc is thoroughly mixed with aluminium sulphate and water , so as to fix the alkaloids by converting them into the double salts. 3. The resulting alkaloidal double salts are subjected to continuous extraction with hot benzene that removes the alkaloid exclusively on one hand; and the unwanted substances e.g., ergot oil, soluble acid, neutral substances like- phytosterol, colouring matter and organic acids on the other. 4. The benzene is removed under vacum and the residue thus obtained is stirred for several hours with a large volume of benzene and subsequently made alkaline by passing NH3 gas. 5. The resulting solution is filtered and the benzene extract is concentrated under vacum, whereupon ergotamine crystallizes out. 6. An additional quantity of ergotamine may also be crystallized from the mother liquour by treatment with petroleum ether. 7. Ergotamine may be further purified by crystallization from aqueous acetone. EXTRACTION 1. The powdered dried ergot is first defatted with n-hexane or petroleum ether (40-60°) 2. The marc is thoroughly mixed with aluminium sulphate and water , so as to fix the alkaloids by converting them into the double salts. 3. The resulting alkaloidal double salts are subjected to continuous extraction with hot benzene that removes the alkaloid exclusively on one hand; and the unwanted substances e.g., ergot oil, soluble acid, neutral substances like- phytosterol, colouring matter and organic acids on the other. 4. The benzene is removed under vacum and the residue thus obtained is stirred for several hours with a large volume of benzene and subsequently made alkaline by passing NH3 gas. 5. The resulting solution is filtered and the benzene extract is concentrated under vacum, whereupon ergotamine crystallizes out. 6. An additional quantity of ergotamine may also be crystallized from the mother liquour by treatment with petroleum ether. 7. Ergotamine may be further purified by crystallization from aqueous acetone.
  • 63. Chemical constituents Most important Ergot alkaloids are Ergometrine group (Water soluble) Ergometrine , Ergometrinine. Ergotamine group (water -insoluble) Ergotamine , Ergotaminine , Ergosine. Ergotoxine group (Water-insoluble) Ergocristine , Ergocristinine , Ergocryptine , Ergocryptinine , Ergocornine 2. Alkaloids obtained from lysergic acid are physiological active. 3. Histamine , tyramine 4. Sterols like ergosterol and fungisterol, 5. Elymoclavine , sclerythrin , ergonovine, 7. Clavicepsin , ergoflavin , ergotic acid betaine 8. Clavine, mannitol, lactic acid and succinic acid. Chemical constituents Most important Ergot alkaloids are Ergometrine group (Water soluble) Ergometrine , Ergometrinine. Ergotamine group (water -insoluble) Ergotamine , Ergotaminine , Ergosine. Ergotoxine group (Water-insoluble) Ergocristine , Ergocristinine , Ergocryptine , Ergocryptinine , Ergocornine 2. Alkaloids obtained from lysergic acid are physiological active. 3. Histamine , tyramine 4. Sterols like ergosterol and fungisterol, 5. Elymoclavine , sclerythrin , ergonovine, 7. Clavicepsin , ergoflavin , ergotic acid betaine 8. Clavine, mannitol, lactic acid and succinic acid.
  • 64. Identification Tests The ergot alkaloids are readily precipitated by the alkaloidal reagents. However, Mayer's reagent is regarded to be the most sensitive test Iodine solution in KI also gives an instant precipitate with very dilute solutions of ergot alkaloids. Keller's Test: To a solution of the alkaloid in glacial acetic acid add a few mg of solid FeCl3 and then add 1-2 ml of concentrated sulphuric acid along the side of the tube. The appearance of an intense blue colouration is accomplished at the junction of the two layers. Fluorescence Test: The aqueous solution of the salts of ergot alkaloids produce a distinct blue fluorescence.. Van Urk Test: When a solution containing an ergot alkaloid is mixed with Van Urk Reagent**, it gives rise to a characteristic deep blue colouration. Identification Tests The ergot alkaloids are readily precipitated by the alkaloidal reagents. However, Mayer's reagent is regarded to be the most sensitive test Iodine solution in KI also gives an instant precipitate with very dilute solutions of ergot alkaloids. Keller's Test: To a solution of the alkaloid in glacial acetic acid add a few mg of solid FeCl3 and then add 1-2 ml of concentrated sulphuric acid along the side of the tube. The appearance of an intense blue colouration is accomplished at the junction of the two layers. Fluorescence Test: The aqueous solution of the salts of ergot alkaloids produce a distinct blue fluorescence.. Van Urk Test: When a solution containing an ergot alkaloid is mixed with Van Urk Reagent**, it gives rise to a characteristic deep blue colouration.
  • 65. USES 1. Ergonovine is used as an oxytocic. 2. Ergonovine maleate also acts as an oxytocic and produces much faster stimulation of the uterine muscles as compared to other drugs 3. It is employed as a potent antimigraine drug. 4. Ergotamine possesses oxytocic properties. 5. Ergotamine tartrate is used invariably to prevent or abort vascular headaches, including migraine and cluster headaches. The mechanism of action is perhaps due to direct vasoconstriction of the dilated carotid artery bed with concomitant lowering in the amplitude of pulsations. 6. Ergotamine tartrate is also an antagonist of the serotonin activity. 7. Ergotamine tartrate is frequently used along with caffeine for the management and control of migraine headache. Both serve as cerebral vasoconstrictors USES 1. Ergonovine is used as an oxytocic. 2. Ergonovine maleate also acts as an oxytocic and produces much faster stimulation of the uterine muscles as compared to other drugs 3. It is employed as a potent antimigraine drug. 4. Ergotamine possesses oxytocic properties. 5. Ergotamine tartrate is used invariably to prevent or abort vascular headaches, including migraine and cluster headaches. The mechanism of action is perhaps due to direct vasoconstriction of the dilated carotid artery bed with concomitant lowering in the amplitude of pulsations. 6. Ergotamine tartrate is also an antagonist of the serotonin activity. 7. Ergotamine tartrate is frequently used along with caffeine for the management and control of migraine headache. Both serve as cerebral vasoconstrictors
  • 66. IPECAC Biological source: Ipecac is the dried roots and rhizomes of Cephalis ipecacuanha (Brazilian ipecacuanha) belonging to the Family Rubiaceae. It contains several alkaloids (2 –2.5 %), mainly emetine (50- 70 % of total alkaloids), with cephaline and psychotrine. Synonyms: Ipecacuanha. Cultivation The propagation is done by seed sowing Germination of the seed increased by treatment of the seed with lime water / hydrogen peroxide Seedlings are transplanted at 10 x 10 cm at a room temperature of 23 – 38°C It requires a rain fall of 30 cm , humidity helps the plant Nitrogenous fertilizers have significant effect in quality of plant
  • 67. Character Root part Rhizome part Color Dark brick red to brown Brick red to brown Odour Faint Faint Taste Bitter Bitter Size 150 mm length; 60 mm thickness 2 mm in diameter Shape Tortuous , pieces cylindrical Macroscopical characters
  • 68. T.S shows cork cells followed by phelloderma. Composed by parenchymatous cells Shows presence of starch grains, calcium oxalate crystals. It also shows presence of tracheids Microscopical characters Root part Pericycle are thick walled Protoxylem are spiral Starch grains are presentStarch grains are present Rhizome part Pericycle are thick walled Sclereids are present Starch grains are present in larger size T.S of : Ipecacuanha
  • 69. P o w d e re d ro o t a n d rh iz o m e - E xt. a lco h o l,C o nc., lea d a ceta te. - Filtratio n F iltra te R e s id u e N on -a lka loida l su b. - E vap ., d il. H C l & Filtratio n A lka loida l ba ses a n d sa lts F iltra te (A lka loida l H C l sa lts) - A lk . w ith N a O H & E xt. w ith eth er E th e r la ye r E m etin e (P h en olic a lka loids) - H C l (A lk alo id al salts) - A lk . N H 4 O H E xt. eth er A q u e o u s la ye r E th e r la ye r (P sy ch otrin e) (C eph a lin e) A q .a lk . s o lu tio n ISOLATION OF IPECAC ALKALOIDS P o w d e re d ro o t a n d rh iz o m e - E xt. a lco h o l,C o nc., lea d a ceta te. - Filtratio n F iltra te R e s id u e N on -a lka loida l su b. - E vap ., d il. H C l & Filtratio n A lka loida l ba ses a n d sa lts F iltra te (A lka loida l H C l sa lts) - A lk . w ith N a O H & E xt. w ith eth er E th e r la ye r E m etin e (P h en olic a lka loids) - H C l (A lk alo id al salts) - A lk . N H 4 O H E xt. eth er A q u e o u s la ye r E th e r la ye r (P sy ch otrin e) (C eph a lin e) A q .a lk . s o lu tio n
  • 70. CHEMICAL CONSTITUENTS N MeO RO N OMe OMe H H R = Me Emetine R = H Cephaline N MeO HO N OMe OMe H Psychotrine Emetine: It is non phenolic and levorotatory. It contains 2 basic nitrogens. Psychotrine: Occurs as yellow prisms. It is phenolic and gives cephaline on reduction. It gives emetine on reduction followed by methylation. N MeO RO N OMe OMe H H R = Me Emetine R = H Cephaline N MeO HO N OMe OMe H Psychotrine Cephaline: It is phenolic and levorotatory. It gives emetine on methylation with (CH3)2 SO4.
  • 71. Alkaloidal solution in HCl + Ca hypochlorite  orange color. Emetine and cephaline + Froehd's reagent: dirty green color (the color with emetine fades by addition of HCl). Psychotrine + Froehd's reagent: pale green color. Cephaline and psychotrine + p-nitrodiazobenzene  dye soluble in NaOH  purple color. Psychotrine + conc. H2SO4 + HNO3  cherry red color. Emetine + Liebermann's reagent  black color. IDENTIFICATION TESTS Alkaloidal solution in HCl + Ca hypochlorite  orange color. Emetine and cephaline + Froehd's reagent: dirty green color (the color with emetine fades by addition of HCl). Psychotrine + Froehd's reagent: pale green color. Cephaline and psychotrine + p-nitrodiazobenzene  dye soluble in NaOH  purple color. Psychotrine + conc. H2SO4 + HNO3  cherry red color. Emetine + Liebermann's reagent  black color.
  • 72. Uses Emetine and cephaeline have antitumour and antiviral activity, but are too toxic for therapeutic use. Emetine and psychotrine are mainly used as emetic drugs. The crude drug is used as expectorant (due to its saponin content) . Emetine HCl and Dehydroemetine (DHE) have an antiamoebic effect, and are used for the treatment of amoebic dysentry Ipeca alkaloids are diaphoretic, Dose :1 mg / kg of body weight,(IM or IV) Emetine and cephaeline have antitumour and antiviral activity, but are too toxic for therapeutic use. Emetine and psychotrine are mainly used as emetic drugs. The crude drug is used as expectorant (due to its saponin content) . Emetine HCl and Dehydroemetine (DHE) have an antiamoebic effect, and are used for the treatment of amoebic dysentry Ipeca alkaloids are diaphoretic, Dose :1 mg / kg of body weight,(IM or IV)
  • 73. OPIUM Biological Source: Opium or gum opium is the air dried milky exudates obtained by incising the unripe capsules of Papaver somniferum. family - Papaveraceae . History: In 1806 Serturner isolated the alkaloid morphine from Opium. The opium poppy is grown commercially now in many countries throughout the world. Cultivation and Collection: The cultivation of Opium poppy is controlled internationally by the International Narcotics Control Board of the United Nations. Synonym : Poppy Latex , Gum opium. Cultivation and Collection: The cultivation of Opium poppy is controlled internationally by the International Narcotics Control Board of the United Nations.
  • 74. The seeds of opium are cultivated in batches. This is to ensure that the entire crop is not affected by climatic conditions like frost or drought. The cultivation is done in the months between September and April. A gap of 25 cm should be maintained between two consecutive plants. Before sowing the seeds, they are mixed with sands properly. About five to six capsules appear on each plant and it flowers in the month of May-June. After the petals fall from the poppy, the pod, which is about the size of a golf ball, is lanced, and the opium latex is exuded. Poppies are lanced in the afternoon and the latex is scraped off the next morning. Pods ripen (soften) at different times in the field. Each pod can be lanced from 4 to 7 times. The seeds of opium are cultivated in batches. This is to ensure that the entire crop is not affected by climatic conditions like frost or drought. The cultivation is done in the months between September and April. A gap of 25 cm should be maintained between two consecutive plants. Before sowing the seeds, they are mixed with sands properly. About five to six capsules appear on each plant and it flowers in the month of May-June. After the petals fall from the poppy, the pod, which is about the size of a golf ball, is lanced, and the opium latex is exuded. Poppies are lanced in the afternoon and the latex is scraped off the next morning. Pods ripen (soften) at different times in the field. Each pod can be lanced from 4 to 7 times. Commercial varieties include Turkish, Persian, Indian & Yugoslavian opium.
  • 75. Macroscopic Character Odor: Strong , characteristic. Taste: Bitter. Color: Varies depending on the type of opium. For instance, Indian opium is dark brown while manipulated Turkish opium is chocolate brown in color.
  • 76. Chemical constituents Opium contains more than 19 alkaloids, some of which are combined with Meconic acid, others with sulfuric acid and some as free alkaloids. There are 3 main classes Phenanthrene.-----------------Morphine ,Thebeine , Codeine. Benzyl Isoquinoline. ------- Noscapine , Papaverine Phenyl alkyl amine --------- Narceine Chemical constituents Opium contains more than 19 alkaloids, some of which are combined with Meconic acid, others with sulfuric acid and some as free alkaloids. There are 3 main classes Phenanthrene.-----------------Morphine ,Thebeine , Codeine. Benzyl Isoquinoline. ------- Noscapine , Papaverine Phenyl alkyl amine --------- Narceine
  • 77. Extraction from Opium Powdered Opium Shaken with Calcium chloride solution and filteredShaken with Calcium chloride solution and filtered Filtrate concentrated+10% NaOH solution Precipitate (Narcotine, Papaverine, Thebaine) Filtrate (Morphine, Codeine,)
  • 78. 1.Opium is dissolved in water and then ferric chloride solution is added. It results in reddish purple color. The change in color occurs due to presence of Meconic acid in opium. 2.When opium is treated with small amount of nitric acid, orange red color is produced. This test occurs due to the presence of morphine in opium CHEMICAL TESTS 1.Opium is dissolved in water and then ferric chloride solution is added. It results in reddish purple color. The change in color occurs due to presence of Meconic acid in opium. 2.When opium is treated with small amount of nitric acid, orange red color is produced. This test occurs due to the presence of morphine in opium
  • 79. Morphine 1. Most powerful analgesic used in cases of severe pain as post operative pain, bone fractures, cancer patients & in cases of angina. 2. Remedy in convulsions. 3. Precede the use of anesthetics to increase their efficacy 4. Used as an antagonists for poisonous effects of other alkaloids as strychnine, atropine, phytostigmine. USESMorphine 1. Most powerful analgesic used in cases of severe pain as post operative pain, bone fractures, cancer patients & in cases of angina. 2. Remedy in convulsions. 3. Precede the use of anesthetics to increase their efficacy 4. Used as an antagonists for poisonous effects of other alkaloids as strychnine, atropine, phytostigmine. Dose: Morphine Sulfate parentrally is 10mg 6 / day.
  • 80. Codeine 1. is weaker in intensity than morphine. 2. produces less tendencies to addiction. 3. Codeine depresses the cough center in the brain. 4. Causes constipation & hypnosis. Dose: Usual doses of codeine phosphate and Codeine sulfate are As analgesic: 15-60 mg every 4 hrs. As antitussive:10-20 mg every 4-6 hrs. Dose: Usual doses of codeine phosphate and Codeine sulfate are As analgesic: 15-60 mg every 4 hrs. As antitussive:10-20 mg every 4-6 hrs.
  • 81. Heroin 1. It is the synthetic diacetyl derivative of morphine. 2. It is 5 X more potent as morphine. Papaverine Occurs naturally in opium to the extent of about 1%.Used as Smooth muscle relaxant and an anti-tussive in combination with Codeine sulfate. Dose: Orally 150 mg, IM 30 mg. • As antitussive 15mg.
  • 82. Synosym: Belladonna leaf, Deadly night shade Biological source: Belladonna herb consists of dried leafs and other aerial parts of Atropa belladonna, belonging to the family Solanaceae Macroscopy Colour: leaves are green to brownish Flowers are purple to yellowish Fruits are green to brown Odour : slight and characteristic Taste : Bitter acrid Size : Leaves-5 to 25 cm long,2.5 to 12 cm wide Flowers –corolla 3 cm long 2 cm wide Fruits- 10 cm diameter Shape : leaves are ovate , lanceolate , acuminate Flowers : campanulate , small Fruits : Berries , subglobular , BELLADONNA Colour: leaves are green to brownish Flowers are purple to yellowish Fruits are green to brown Odour : slight and characteristic Taste : Bitter acrid Size : Leaves-5 to 25 cm long,2.5 to 12 cm wide Flowers –corolla 3 cm long 2 cm wide Fruits- 10 cm diameter Shape : leaves are ovate , lanceolate , acuminate Flowers : campanulate , small Fruits : Berries , subglobular ,
  • 83. Microscopy Epidermal cells are slightly anticlinical Anisocytic stomata is present, uniserrate , covering trichomes also present Palisade ration is 5-7 Chemical constituents : l- Hyoscyamine , Belladonine ,Scopolamine. Uses :Parasympatholytic , Anti- cholenergic , reduces sweat , saliva , Gastric juice , spasm , also used as Antidote Dose : 0.6 - 1 ml Belladonna tincture 4 times / day. Epidermal cells are slightly anticlinical Anisocytic stomata is present, uniserrate , covering trichomes also present Palisade ration is 5-7 Chemical constituents : l- Hyoscyamine , Belladonine ,Scopolamine. Uses :Parasympatholytic , Anti- cholenergic , reduces sweat , saliva , Gastric juice , spasm , also used as Antidote Dose : 0.6 - 1 ml Belladonna tincture 4 times / day. S.NO PLANT NAME IDENTIFICATION 1 Plytolacca americanna ( leaves ) Presence of Idioblasts 2 Solanum nigrum Presence Thick lamina , Anomocytic stomata 3 Ailanthus glandulosa Presence cluster of calcium oxalate crystals Adulterants
  • 84. Synosym: Periwinkle , Vinca Biological source: Dried whole plant of Catharanthus roses , belonging to the family Apocynaceae. Macroscopy VINCA Colour: leaves are green , pale grey , flowers are violet , pink , white , carmine red. Odour : Bitter and characteristic Taste : Bitter Shape : leaves are ovate , petiolate , oblong , unicostate , reticulate , acute , apex , entire , brittle , glossy in appearance , Flowers : Bracteates , pedicellate , complex , hermaphodite , 2-3 cm cymose. Colour: leaves are green , pale grey , flowers are violet , pink , white , carmine red. Odour : Bitter and characteristic Taste : Bitter Shape : leaves are ovate , petiolate , oblong , unicostate , reticulate , acute , apex , entire , brittle , glossy in appearance , Flowers : Bracteates , pedicellate , complex , hermaphodite , 2-3 cm cymose.
  • 85. Microscopy Upper surface is single layered rectangular in shape Epidermis consists of unicellular ,  covering trichomes . Palisade is single layered 5- 8 layered Spongy parenchyma is present Mid rib consists of collenchyma , xylem , phloem present in centre Stomata is of cruciferous Lower epidermis contains Calcium oxalate crystals Upper surface is single layered rectangular in shape Epidermis consists of unicellular ,  covering trichomes . Palisade is single layered 5- 8 layered Spongy parenchyma is present Mid rib consists of collenchyma , xylem , phloem present in centre Stomata is of cruciferous Lower epidermis contains Calcium oxalate crystals Chemical constituents : mainly contains Indole group with oncocytic action like Vincristine , Vinblastine , ajmalicine , Dose : Vincristine-10 to 30 mg / body wt : Vinblastine 100 µg / body wt T.S of : Vinca
  • 86. Antineoplastic agents Vinblastine Arrests mitosis in metaphase Gives intravenously in acute leukemia in children Vincristine Arrests mitosis in metaphase Interferes amino acid metabolism treats Hodgkin's disease Hypertensive and anti diabetic Uses Antineoplastic agents Vinblastine Arrests mitosis in metaphase Gives intravenously in acute leukemia in children Vincristine Arrests mitosis in metaphase Interferes amino acid metabolism treats Hodgkin's disease Hypertensive and anti diabetic
  • 87. EPHEDRA Synosym: Ma-Huang Biological source: It consists of dried young stem of Ephedra gerardiana and Ephedra nebrodensis. Belonging in to the Family Gnetaceae (Ephedraceae). MACROSCOPY Ephedra is Gymnospermous bearing thin stem which are woody ,cylindrical in nature 5 mm in diameter. Ephedra consists of scaly leaves , The bases of the leaves are dark brown and they are joined on all sides of the node forming a sheath . Which bears a terminal bud, which is short , usually constricted at the base. The male spikes are solitary , ovate , sessile and crowded. “ma”=astringent, “huang”=yellow MACROSCOPY Ephedra is Gymnospermous bearing thin stem which are woody ,cylindrical in nature 5 mm in diameter. Ephedra consists of scaly leaves , The bases of the leaves are dark brown and they are joined on all sides of the node forming a sheath . Which bears a terminal bud, which is short , usually constricted at the base. The male spikes are solitary , ovate , sessile and crowded.
  • 88. MICROSCOPY Unicellular epidermis made up of quadrangular cells along with thick walled cuticle Vertical rows of sunken stomata and papillae on ridges Cortex is collenchymatous Hypodermal fibers are non-lignified Pericyclic fibres are lignified Calcium oxalate crystals are present in cortex Pith is of parenchymatous dark in color Unicellular epidermis made up of quadrangular cells along with thick walled cuticle Vertical rows of sunken stomata and papillae on ridges Cortex is collenchymatous Hypodermal fibers are non-lignified Pericyclic fibres are lignified Calcium oxalate crystals are present in cortex Pith is of parenchymatous dark in color T.S of : Ephedra
  • 89. Chemical constituents :It contains the amino alkaloids : Ephedrine, nor-ephedrine, n-methyl ephedrine, pseudo-ephedrine. Ephedrine Produced commercially by: Extraction of the plant material Chemical procedure involving a reductive condensation between L-1-phenyl-1- acetylcarbinol and methylamine Occurs as white, rosette or needle crystals, or as an unctuous mass Soluble in water, alcohol, chloroform, ether, and liquid petrolatum Melts between 33 and 400C, depending on its water content Chemical constituents :It contains the amino alkaloids : Ephedrine, nor-ephedrine, n-methyl ephedrine, pseudo-ephedrine. Ephedrine Produced commercially by: Extraction of the plant material Chemical procedure involving a reductive condensation between L-1-phenyl-1- acetylcarbinol and methylamine Occurs as white, rosette or needle crystals, or as an unctuous mass Soluble in water, alcohol, chloroform, ether, and liquid petrolatum Melts between 33 and 400C, depending on its water content Identification Test :-- Ephedrine is dissolved in water and dil.hcl ,then treated separately with copper sulphate and sodium hydroxide. The solution gives Violet colour. If shaken with ether the organic layer shows purple colour and aqueous layer shows blue colour.
  • 90. USES: Sympathomimetic (stimulates α, β1, & β2 adrenergic receptors) Ephedrine Sulfate – crystals of the sulfate of Ephedrine Used to combat hypotensive states, for allergic disorders, and for nasal decongestion. bronchodilator in asthma. Usual dose is: 25-50mg, 6-8x a day as necessary (oral & parenteral) 0.1-0.15mL of a 1-3% solution, 2-3x a day (intranasal) USES: Sympathomimetic (stimulates α, β1, & β2 adrenergic receptors) Ephedrine Sulfate – crystals of the sulfate of Ephedrine Used to combat hypotensive states, for allergic disorders, and for nasal decongestion. bronchodilator in asthma. Usual dose is: 25-50mg, 6-8x a day as necessary (oral & parenteral) 0.1-0.15mL of a 1-3% solution, 2-3x a day (intranasal)
  • 91. Synonyms :Coffee bean, coffee seedCOFFEE Biological Source : It is the dried ripe seed of Coffea arabica. It belongs to family Rubiaceae. Coffee plant is an evergreen shrub which bears drupe type of fruit with an ellipsoidal or spheroidal shape. Each fruit has 2 locules, containing one seed in each chamber.  Each plant gives about 2 -3 kg of coffee seeds. The fruit are dried to separate the seeds. The seeds are separated by wetting them and mechanically separating, followed by drying in heaps, which causes fermentation. The separated seeds or beans are green in colour. They are roasted by which the colour and odour is effected. The seeds acquire dark brown colour and possess an agreeable odour and bitter taste. Coffee plant is an evergreen shrub which bears drupe type of fruit with an ellipsoidal or spheroidal shape. Each fruit has 2 locules, containing one seed in each chamber.  Each plant gives about 2 -3 kg of coffee seeds. The fruit are dried to separate the seeds. The seeds are separated by wetting them and mechanically separating, followed by drying in heaps, which causes fermentation. The separated seeds or beans are green in colour. They are roasted by which the colour and odour is effected. The seeds acquire dark brown colour and possess an agreeable odour and bitter taste.
  • 92. CHEMICAL CONSTITUENTS The main constituents of coffee bean are caffeine, tannin, fixed oil and proteins. It contains 2-3% caffeine, 3-5% tannins, 13% proteins, 10-15% fixed oils, Caffeine chlorogenic or caffeotannic acid and sugars in the form of dextrin, glucose, etc. in the seeds, caffeine is present as a salt of chlorogenic acid. During roasting process, the agreeable smell of coffee is developed which is due to an oil called caffeol composed of mainly furfural along with minor quantities of phenol, pyridine and valerianic acid. CHEMICAL CONSTITUENTS The main constituents of coffee bean are caffeine, tannin, fixed oil and proteins. It contains 2-3% caffeine, 3-5% tannins, 13% proteins, 10-15% fixed oils, Caffeine chlorogenic or caffeotannic acid and sugars in the form of dextrin, glucose, etc. in the seeds, caffeine is present as a salt of chlorogenic acid. During roasting process, the agreeable smell of coffee is developed which is due to an oil called caffeol composed of mainly furfural along with minor quantities of phenol, pyridine and valerianic acid.
  • 93. Chemical Test: 1. Murexide test: caffeine when heated with Hcl & potassium chlorate gives a residue which turns purple when exposed to ammonia vapours 2. Caffeine forms a white precipitate with tannin solution EXTRACTION OF CAFFEINE Caffeine is prepared either by synthesis or extracted from natural sources. Coffee bean is one of the major sources for it. For the extraction, coffee roasters are used in which caffeine sublimed during roasting is recovered. USES It is used as the source of caffeine. The main effects of coffee i.e. stimulant and diuretic actions are due to caffeine. Chemical Test: 1. Murexide test: caffeine when heated with Hcl & potassium chlorate gives a residue which turns purple when exposed to ammonia vapours 2. Caffeine forms a white precipitate with tannin solution
  • 94. COLCHICUM Synosym: meadow saffron seed , autumn crocus Biological source: It consists of dried ripe seeds of Colchicum luteum and Colchicum autumnale. Belonging in to the family Liliaceae. Character Colchicum seed Colchicum corms Color Very hard and reddish brown testa Yellowish brown Odour None None Taste Bitter acrid Bitter acrid Size 2 – 3 mm in diameter Slices are 2 – 5 mm thickSize 2 – 3 mm in diameter Slices are 2 – 5 mm thick Shape Projection at hilum Ovate ,sub- reniform Extra features Presence of Strophiole at hilum Fracture is short and cut surface , shows grayish points
  • 95. MICROSCOPY The section of seed shows parenchyma and endosperm. The parenchymatous cells are reddish brown with thick walls. The endodermic cells shows pitted walls and contains aleurone grains and fixed oils. The Strophiole portion contains starch. The corm has epidermis , parenchyma and vascular tissue . Parenchymatous cells shows presence of starch. Epidermis shows presence of circular stomata. Vascular bundles are present with spiral annular xylems. The section of seed shows parenchyma and endosperm. The parenchymatous cells are reddish brown with thick walls. The endodermic cells shows pitted walls and contains aleurone grains and fixed oils. The Strophiole portion contains starch. The corm has epidermis , parenchyma and vascular tissue . Parenchymatous cells shows presence of starch. Epidermis shows presence of circular stomata. Vascular bundles are present with spiral annular xylems. Chemical constituents : Colchicine and Demi-colchicine.(both the alkaloids contain Tropolone ring structure). Colchicine is freely soluble in alcohol and chloroform , soluble in 25 parts of water and in 220 parts of ether.
  • 96. Identification Test :-- - Colchicine + 70% H2SO4 gives Yellow colour. Colchicine + alcoholic solution + Fecl3 gives red color Uses :-- Specific drug for treatment of Gout and also having Anti-Tumor activity. Apart from medicinal also shows mutations in as a chemical agent in horticulture. Dose :500-650 µg , orally 1 – 3 times daily orally 500 µg to 1 mg , 1-2 times a day intravenously Allied drugs: 1.Dipadax 2.Bulbocodium 3. Gloriosa Uses :-- Specific drug for treatment of Gout and also having Anti-Tumor activity. Apart from medicinal also shows mutations in as a chemical agent in horticulture. Dose :500-650 µg , orally 1 – 3 times daily orally 500 µg to 1 mg , 1-2 times a day intravenously Allied drugs: 1.Dipadax 2.Bulbocodium 3. Gloriosa
  • 97. HYOSCYAMUS Synosym: Henbane , Hyoscyamus leaf Biological source: Dried leafs of Hyoscyamus Niger belonging to the family solanaceae , it consists of NLT 0.05 % Hyoscyamus , l- Hyoscyamine. MACROSCOPY Color :leaves are pale green in color Odor :characteristic Taste :bitter , acrid Size : Lamina is 25 cm long Shape :Ovate , Oblong , Triangular , with petiole , Leaf margins are irregular , dentate Apex is covered with hairs , shows pinnate venetation Flowers are funnel shaped MACROSCOPY Color :leaves are pale green in color Odor :characteristic Taste :bitter , acrid Size : Lamina is 25 cm long Shape :Ovate , Oblong , Triangular , with petiole , Leaf margins are irregular , dentate Apex is covered with hairs , shows pinnate venetation Flowers are funnel shaped
  • 98. MICROSCOPY Leaves are Dorsiventral Epidermis covered with smooth cuticle Numerous glandular trichomes are present Palisade cells are appear in single layer Idioblasts are also present Chemical constituents : Scopolamine , l- hyoscyamine. Atropine T.S of : Hyoscyamus leafChemical constituents : Scopolamine , l- hyoscyamine. Atropine Uses :--Purgative , Sedative , Expectorant , Anti-spasmodic , Anti-histamatic Scopolamine patch is used for: Preventing nausea and vomiting associated with motion sickness and recovery from anesthesia and surgery. Identification Test :-- vitali-Morin test is +ve alkaloids gives violet colour when treated with conc. nitric acid and alcoholic KOH.
  • 99. DUBOISIA Biological source: Dried leafs of Duboisia myoporoides belonging to the family solanaceae . Synosym: Cork wood MACROSCOPY Duboisia is a perennial herb / surb 3.0 m Color :Brown to purple Odor :characteristic Taste :bitter , acrid Size : Leaves are 3- 10 cm ling Shape : Tapering ends with alternate arrangement MACROSCOPY Duboisia is a perennial herb / surb 3.0 m Color :Brown to purple Odor :characteristic Taste :bitter , acrid Size : Leaves are 3- 10 cm ling Shape : Tapering ends with alternate arrangement
  • 100. Chemical constituents : Scopolamine , l- hyoscyamine. Atropine , Valtropine Identification Test :-- vitali-Morin test is +ve alkaloids gives violet colour when treated with conc. nitric acid and alcoholic KOH. Uses :Parasympatholytic , Anti- cholenergic , reduces sweat , saliva , Gastric juice , spasm , also used as Antidote Identification Test :-- vitali-Morin test is +ve alkaloids gives violet colour when treated with conc. nitric acid and alcoholic KOH. Uses :Parasympatholytic , Anti- cholenergic , reduces sweat , saliva , Gastric juice , spasm , also used as Antidote
  • 101. NUX VOMICA Biological source: Nux vomica consists of dried ripe seeds of Strycnos nux vomica Linn, belonging to family Loganiaceae Strycnos=poison vomica =nut with vomiting effect Synonym: crow fig, strychni,Nux vomica seed MACROSCOPY Colour: Greenish –brown Odour: None Taste :Bitter Size: Seeds are 10 -30 mm in diameter 4-6 mm thickness Extra features: seeds are radial disc shaped, Endosperm, cotyledons seen in L.S of seed MACROSCOPY Colour: Greenish –brown Odour: None Taste :Bitter Size: Seeds are 10 -30 mm in diameter 4-6 mm thickness Extra features: seeds are radial disc shaped, Endosperm, cotyledons seen in L.S of seed
  • 102. MICROSCOPIC STUDY Epidermis contains thickened, lignified trichomes followed by layer of collapsed cells. Endo dermis contains thickened polyhedral un- lignified cells with plasma derma. Oil globules, calcium oxalate crystals, starch grains are absent Chemical constituents: Indole alkaloids –strychine,brucine ,strychnine Chemical tests: T.S of Nux vomica with ammonium vandate and sulphuric acid (manddin’s test) gives purple colour – Strychine T.S of Nux vomica with Con,nitic acid gives yellow color- Brucine. Uses:1.stomachic ,tonic due to bitter taste 2.CNS Stimulant , 3.Action on CVS increase blood pressure MICROSCOPIC STUDY Epidermis contains thickened, lignified trichomes followed by layer of collapsed cells. Endo dermis contains thickened polyhedral un- lignified cells with plasma derma. Oil globules, calcium oxalate crystals, starch grains are absent Chemical constituents: Indole alkaloids –strychine,brucine ,strychnine Chemical tests: T.S of Nux vomica with ammonium vandate and sulphuric acid (manddin’s test) gives purple colour – Strychine T.S of Nux vomica with Con,nitic acid gives yellow color- Brucine. Uses:1.stomachic ,tonic due to bitter taste 2.CNS Stimulant , 3.Action on CVS increase blood pressure
  • 103. WITHANIA Synonyms: Withania root, asgandh, winter cherry. Biological source: It consists of dried roots & stem bases of withania somnifera belonging to the family solanaceae. Macroscopy: Colour - Buff or grey yellow Odour - Similar to urine of horse Taste - Bitter Fracture- Smooth & powdery Extra features: The root has longitudinal wrinkles They are un-branched, straight, conical & some of them bear a crown. Root crown shows a number of bud scars Roots are bitter in taste , fresh root gives smell similar to horse urine Macroscopy: Colour - Buff or grey yellow Odour - Similar to urine of horse Taste - Bitter Fracture- Smooth & powdery Extra features: The root has longitudinal wrinkles They are un-branched, straight, conical & some of them bear a crown. Root crown shows a number of bud scars Roots are bitter in taste , fresh root gives smell similar to horse urine
  • 104. Microscopic study The T.S of root shows presence of cork with non lignified cells of 2 – 4 layers It also shows presence of vascular tissue like cambium , phloem , sieve tubes Secondary xylem is hard in nature Starch grains are present in stem bases , it also shows tracheids. Chemical constituents: The main constituents are alkaloids & steroidal lactones. Withanine is the main constituent. The other alkaloids are somniferine, somnine, pseudo withanine. Steroidal lactones are also called withanolides. The drug also contains somnitol & somnirol. Uses: It has sedative & hypnotic effects. It has hypotensive, Respiratory, stimulant actions. It is an immunomodulatory agent. It is used in the treatment of rheumatism, gout & skin diseases. It is widely used as sex stimulant & rejuvenator. Also used against staphylococcus aureus Microscopic study The T.S of root shows presence of cork with non lignified cells of 2 – 4 layers It also shows presence of vascular tissue like cambium , phloem , sieve tubes Secondary xylem is hard in nature Starch grains are present in stem bases , it also shows tracheids. Chemical constituents: The main constituents are alkaloids & steroidal lactones. Withanine is the main constituent. The other alkaloids are somniferine, somnine, pseudo withanine. Steroidal lactones are also called withanolides. The drug also contains somnitol & somnirol. Uses: It has sedative & hypnotic effects. It has hypotensive, Respiratory, stimulant actions. It is an immunomodulatory agent. It is used in the treatment of rheumatism, gout & skin diseases. It is widely used as sex stimulant & rejuvenator. Also used against staphylococcus aureus
  • 105. Biological source: It is the dried stem bark of Holarrhena antidysentrica / Holarrhena pubescens belonging to the family Apocynacece. It is collected from 8 to 10 years old plant and freed from attached wood and peeled into small pieces. It should contain NLT 2% of total alkaloids of kurchi Macroscopy: Colour - Buff to pale brown on outer surface Slightly brownish on inner surface Odour - No odour Taste - Bitter and Acrid Macroscopy: Colour - Buff to pale brown on outer surface Slightly brownish on inner surface Odour - No odour Taste - Bitter and Acrid Extra features: Shape :- Longitudinally RECURVED pieces Size :- Variable Outer surface :-It is longitudinally wrinkled and bears horizontal lenticels Inner surface :- Brownish rough and with irregular transverse cracks Fracture :- Short and granular
  • 106. MICROSCOPIC STUDY CORK CELLS Thin walled few colorless and few are with yellowish brown matter STONE CELLS / SCLERIDS Rectangular to oval in shape, walls striated, pitted and lignified. surrounded by sheath of parenchymatous cells containing calcium oxalate crystals. MEDULLARY RAYS Phloem parenchyma traverse the medullary rays at right angles through such pieces are not seen many in number CALCIUM OXALATE CRYSTALS Present in the form of prisms scattered all over in the powder STARCH GRAINS Few in number, simple grains CORK CELLS Thin walled few colorless and few are with yellowish brown matter STONE CELLS / SCLERIDS Rectangular to oval in shape, walls striated, pitted and lignified. surrounded by sheath of parenchymatous cells containing calcium oxalate crystals. MEDULLARY RAYS Phloem parenchyma traverse the medullary rays at right angles through such pieces are not seen many in number CALCIUM OXALATE CRYSTALS Present in the form of prisms scattered all over in the powder STARCH GRAINS Few in number, simple grains
  • 107. Kurchi bark contains steroidal alkaloid up to about 1.8 to 4.5% They are C21 group of steroidal alkaloids The active alkaloids are conessine (kurchicine), norconessine, isoconessine, dioxyconessine, conessimine, holarrhimine, holarrhidine, Conessine is also present in root bark along with some other steroidal alkaloids In addition to alkaloids kurchi contains gums, resins, tannins, lupeal and beta- sitosterol Chemical constituents Kurchi bark contains steroidal alkaloid up to about 1.8 to 4.5% They are C21 group of steroidal alkaloids The active alkaloids are conessine (kurchicine), norconessine, isoconessine, dioxyconessine, conessimine, holarrhimine, holarrhidine, Conessine is also present in root bark along with some other steroidal alkaloids In addition to alkaloids kurchi contains gums, resins, tannins, lupeal and beta- sitosterol HOLARRHIDINECONESSINE
  • 108. CHEMICAL TESTSCHEMICAL TESTS SALKOWSKI REACTION:- To 20 ml of extract add 2ml of chloroform and 2ml of concentrated sulphuric acid shake well. chloroform layer appears red and acid layer shows greenish yellow fluorescence. Indicates the presence of steroidal moiety . LIBERMANN-BURCHARD REACTION:-Mix 2ml of extract with chloroform add 1-2ml of acetic anhydride and 2drops of concentrated sulphuric acid from sides of the test tube. First red then blue and finally green color appears. Indicates the presence of steroidal moiety. LIBERMANN’S REACTION:-Mix 3ml extract with 3ml acetic anhydride heat and cool, add few drops of concentrated sulphuric acid. Blue color appears. Indicates the presence of steroidal moiety . CHEMICAL TESTSCHEMICAL TESTS SALKOWSKI REACTION:- To 20 ml of extract add 2ml of chloroform and 2ml of concentrated sulphuric acid shake well. chloroform layer appears red and acid layer shows greenish yellow fluorescence. Indicates the presence of steroidal moiety . LIBERMANN-BURCHARD REACTION:-Mix 2ml of extract with chloroform add 1-2ml of acetic anhydride and 2drops of concentrated sulphuric acid from sides of the test tube. First red then blue and finally green color appears. Indicates the presence of steroidal moiety. LIBERMANN’S REACTION:-Mix 3ml extract with 3ml acetic anhydride heat and cool, add few drops of concentrated sulphuric acid. Blue color appears. Indicates the presence of steroidal moiety .
  • 109. THERAPEUTIC USESTHERAPEUTIC USES • Kurchi bark is antiprotozoal in activity and used to treat amoebic dysentery • Kurchi bark is considered to be stomachic, astringent, tonic, anti- dysenteric, febrifuge and anthelmintic • The dried bark is rubbed over the body in dropsy • Conessine is highly active against Entamoeba histolytica • A traditional preparation of kurchi bark i.e. “kutajarishta” is commonly used specially for chronic amoebiasis THERAPEUTIC USESTHERAPEUTIC USES • Kurchi bark is antiprotozoal in activity and used to treat amoebic dysentery • Kurchi bark is considered to be stomachic, astringent, tonic, anti- dysenteric, febrifuge and anthelmintic • The dried bark is rubbed over the body in dropsy • Conessine is highly active against Entamoeba histolytica • A traditional preparation of kurchi bark i.e. “kutajarishta” is commonly used specially for chronic amoebiasis
  • 110. DATURA Synonyms: hell’s bells, devil’s trumpet, Nightshade, Datura metal Biological source: Dried leaves & flowering tops of Datura stramonium , belonging to the family solanaceae , it consists of NLT 0.20 % alkaloids l-hyoscyamine Macroscopy Colour - Green Odour - Unpleasant and bitter Taste - Bitter Size - 9-18 cm length 8-13 cm width Leaves are entire , broken wrinkled , un equal bases , acute apex , flowers are funnel shaped ,seeds are brown in color , found in thorny capsules Macroscopy Colour - Green Odour - Unpleasant and bitter Taste - Bitter Size - 9-18 cm length 8-13 cm width Leaves are entire , broken wrinkled , un equal bases , acute apex , flowers are funnel shaped ,seeds are brown in color , found in thorny capsules
  • 111. Microscopic study Datura is a Dorsiventral leaf Collenchyma appears above & below the mid rib regions Unicellular covering & glandular trichomes are present Xylem is surrounded by phloem Presence of Anisocytic stomata