Scutellaria baicalensis , Baicalin , anticancer substance , medicinal plants ,

1. Scutellaria
baicalensis &
Baicalin

2. • Recent trends in medicinal plants research
show that while ethnobotanical surveys
continue, there is an appreciable increase
in research activity in the area of
bioactivity of natural products. As many as
84% of pediatric oncology patients, 50%
of breast cancer patients and 37% of
prostate cancer patients use
complementary and alternative medicine
(CAM), including predominantly herbal
approaches

3. Scutellaria
Scutellaria is a perennial,
herbaceous genus in the
Lamiaceae family with 350
- 400 species This genus is
well represented by about
90 species in the North
America.

4. Scientific classification
• Kingdom: Plantae
• Order: Lamiales
• Family: Lamiaceae
• Subfamily: Scutellarioideae
• Genus: Scutellaria

5. Species include :-
• Scutellaria baicalensis Georgi – Baikal skullcap, Chinese
skullcap
• Scutellaria californica A.Gray – California skullcap
• Scutellaria lateriflora L. – blue skullcap, Virginian
skullcap
• Scutellaria montana Chapm. – mountain skullcap,
large-flowered skullcap
• Scutellaria ovata Hill – heart-leaved skullcap
• Scutellaria racemosa – South American skullcap
• Scutellaria wrightii – Wright's skullcap
• Scutellaria texana – Texas skullcap

6. • The scullcap (skullcap) is a North American
perennial plant that grows in wet places in
Canada and the northern and eastern U.S.
• Successful micropropagation of many
Scutellaria species have been reported It
has been estimated that the annual
consumption of scullcap increased by 23%
between 2000 and 2001.

7. • The dollar value of the 2001 scullcap
harvest was between $185,000 and
$195,000, that was 3.5 times higher than
that of 1997 As the demand for medicinal
herb is increasing, there is renewed interest
in this genus to propagate clean plants
and biomass in large amount

8. Scutellaria baicalensis
S. baicalensis is the most extensively studied
species of Skullcap

9. Scutellaria baicalensis, Chinese
skullcap
has been widely used as a
medicinal plant in China for
thousands of years (2000) , as a
traditional medicine known as
(Huang-Qin)
,where the preparation from its
roots

10. • The most authoritative book on traditional
Chinese medicine, Bencao Gangmu , which
was first published in 1593, reported that
Scutellaria baicalensis had been used in the
treatment : -

11. diarrhea,
hypertension,
hemorrhaging, insomnia,
inflammation and
respiratory infections

12. • Flavones such as baicalin,
wogonoside and their
aglycones baicalein,
wogonin are the major
bioactive compounds
extracted from the root of
S. baicalensis.

14. • These flavones have been reported to have
various pharmacological functions, including
• anti-cancer,
• hepatoprotection,
• antibacterial and antiviral,
• antioxidant,
• and neuroprotective effects

15. • Huang-Qin was first recorded in
Shennong Bencaojing (The Classic of
Herbal Medicine), written between about
200 and 250 AD, for treatment of bitter,
cold, lung and liver problems
• Its author, Li Shizhen, reported successful
self-administration to treat a severe lung
infection when he was 20 years old

16. • As in traditional Chinese medicine, the roots
of S. amoena and S. likiangensis have been
used commonly as alternatives to S.
baicalensis

17. Pharmacology of
Huang-Qin

18. Antitumor effects :
Many studies have shown that S. baicalensis
extract is cytotoxic to a broad range of cancer
cells from humans, including :
• brain tumor cells
• prostate cancer cells
• HNSCC (head and neck squamous cell
carcinoma) cell lines

19. • Aqueous extracts of S. baicalensis roots
induced apoptosis and therefore
suppressed growth of lymphoma and
myeloma cell line
• Similarly, S. baicalensis extracts were
selectively toxic to several human lung
cancer cell lines, but not to normal human
lung fibroblasts
• Wogonoside has anticancer effects on
acute myeloid leukemia (AML) cell lines

20. Hepatoprotection
• Scutellaria baicalensis is the main component
in the herbal remedy used for liver problems
such as hepatitis, hepatic fibrosis and
carcinoma .
• Yang-GanWan (YGW) is another prescription
containing baicalin, which has long been
known for its protective effects on the liver

21. • Several studies have suggested that S.
baicalensis can effectively inhibit fibrosis
and lipid peroxidation in rat liver
• Consumption of the roots and shoots of S.
baicalensis inhibits mutagenisis caused by
the aflatoxin-B1 mycotoxin in rat liver cells

22. Antibacterial and antiviral activities
• Amongst 46 herb and spice extracts, S.
baicalensis extracts have shown substantial
antibacterial effects against
• Bacillus cereus,
• Escherichia coli,
• Listeria monocytogenes,
• Salmonella anatum
• Staphylococcus aureus

23. • Aqueous extracts of S. baicalensis roots
have antimycotic properties against
• Aspergillus fumigatus,
• Candida albicans,
• Geotrichum candidum
• Rhodotorula rubra

24. • Extracts of S. baicalensis can also enhance
the antimicrobial activity of several
antibiotics such as
• ciprofloxacin,
• ceftriaxone,
• Gentamicin
• penicillin

25. • indicating an antiviral function of
Scutellaria extracts
• Scutellaria root extracts can inhibit the
replication of HCV-RNA .
• Baicalin has very good anti-HIV-1 activity
as a nonnucleoside reverse transcriptase
inhibitor

26. • Early in 1989, Ono et al. reported baicalein
could effectively inhibit reverse
transcriptase activity of human
immunodeficiency virus (HIV); 2 μg/mL
baicalein inhibiting 90 % of the activity of
HIV reverse transcriptases
• These effects of baicalein and baicalin on
HIV have attracted considerable attention

27. Biotechnology to enhance S. baicalensis synthesis
• Understanding the regulation of production of
bioactive flavones (baicalein, baibalin, wogonin and
wogonoside) and their biosynthesis in S.
baicalensis, and developing strategies to enhance
their production are important objectives.
However, like other members of the mint family,
stable genetic transformation and regeneration of
this plant are very difficul

28. • Agrobacterium rhizogenes mediated
production of hairy roots of S. baicalensis
• A. rhizogenes strain-dependant manner.
Among the four strains (A4GUS, R1000 LBA
9402 and ATCC11325) tested by Tiwari et
al.(2008), the A4 stain produced the most
hairy roots, with an efficiency of 42.6 %

29. Flavonoid metabolism
• Scutellaria baicalensis Georgi produces various
natural products including amino acids,
essential oils, flavonoids, phenylethanoids, and
sterols. More than 30 types of flavones can be
found in its roots including baicalin, baicalein,
chrysin, oroxylin A, oroxylin A 7-O-glucuronide,
wogonin and wogonoside.

30. • Flavones are synthesized by the flavonoid
pathway, which is part of phenylpropanoid
metabolism
• Naringenin is a central intermediate in
normal flavone biosynthesis exemplified by
the production of the flavones, scutellarin
and scutellarein, derived from naringenin in
the aerial parts (leaves and flowers) of
Scutellaria baicalensis

31. Baicalin
• The dried root of Baikal skullcap ( Scutellaria
baicalensis ) has been historically and widely used
in traditional Eastern medicine. Modern science
proved that baicalin is the major bioactive
• Baicalin, a flavonoid found in several species in the
genus Scutellaria , has been regarded as a potent
anticancer agent

32. • Cancer is a group of diseases involving
abnormal cell growth with the potential to
invade or spread to other parts of the
body. In 2016, 1,685,210 new cancer cases
and 595,690 cancer deaths are projected to
occur in the United States

33. • Surgery,
• radiation therapy,
• chemotherapy,
• and targeted therapy
are the most common types of cancer
treatment. However, they might cause
severe side effects in patients

34. • Fatigue, a common early and chronic side effect of
irradiation, was reported in up to 80% of patients
during radiation therapy and 30% of follow-up
.The incidence of chemotherapy-induced nausea
vomiting (CINV) in patients was 59.7% within 24
hours after treatment. And the incidence of
CINV was 22.9% in patients who experienced
vomiting nor nausea during the first 24 hours post-
chemotherapy. Thus, it is important to find an
alternative cancer treatment with fewer adverse
effects.

35. • Baicalin is a flavonoid found in the Chinese
herb Scutellaria baicalensis (also known as
Baikal skullcap). Baicalein is the aglycone of
baicalin. Baicalin has been applied in
pharmaceuticals, food and cosmetics industries.
Different extraction methods are employed to
isolate baicalin from Scutellaria baicalensis.

36. Extraction
• are two most widely used extraction
methods
• Different extraction methods are employed
to isolate baicalin from Scutellaria
baicalensis.
• heat reflux extraction (HRE)
• ultrasound-assisted extraction (UAE)

37. Heat reflux extraction (HRE)
• HRE is a conventional
extraction method which
is versatile but time
consuming

38. ultrasound-assisted extraction (UAE)
• Compared with HRE, UAE reduced the
extraction time, the extraction temperature,
and the solvent consumption
• UAE is considered as an economical
alternative to replace traditional extraction
methods

40. • Previous studies have revealed that UAE achieved
superior yields of baicalin and had the prospects to
be applied in the industrial production of baicalin
• One of the studies illustrated that the extraction of
baicalin was most efficient at temperatures of 60°C,
with ethanol concentration of 40% (v/v)

41. • Combinatorial use of HRE with UAE shows
higher yield rate and efficiency compared with
the use of HRE or UAE alone.
• Therefore, the combinatorial use of HRE with
UAE is also very promising for the
commercialized manufacture of natural
compounds in the future (e.g. baicalin)