Natural products, including plants, animals and minerals have been the basis of treatment of human diseases. History of medicine dates back practically to the existence of human civilization. The current accepted modern medicine or allopathy has gradually developed over the years by scientific and observational efforts of scientists. However, the basis of its development remains rooted in traditional medicine and therapies. The history of medicine includes many ludicrous therapies. Nevertheless, ancient wisdom has been the basis of modern medicine and will remain as one important source of future medicine and therapeutics. The future of natural products drug discovery will be more holistic, personalized and involve wise use of ancient and modern therapeutic skills in a complementary manner so that maximum benefits can be accrued to the patients and the community
2. Quotation
“Within the infant rind of this small flower
Poison hath residence and medicine power:
For this, being smelt, with that part cheers each part;
Being tasted, slays all senses with the heart….”
(Romeo & Juliet Act II Scene III.)
3. Introduction
• Powerful ingredients.
• Only 15% of estimated plant species on earth have
been investigated for possible Medicinal uses.
• No magic, diets high in fruits, grains, legumes reduce
the risk of a various number of diseases
• More than 95 % of the population in the least
developing countries use herbs for health and other
purposes.
4. History
• History of traditional medicine in eastern culture
– Ayurveda medicine
– Chinese medicine
• History of traditional medicine in western culture
– European history
The Greco-Roman Period
The Dark ages
19th Century
The 20th Century
– American history
• Breakthrough in pharmaceutical chemistry came when
Serturner isolated morphine from opium poppy in 1806
6. Ayurveda
The aim of Ayurveda is
proper maintenance of
metabolic equilibrium of the
human psychosomatic
material and the restoration of
the same to the normal when
disturbed
7. Contd…
• Ayurveda utilizes herbs and
product from natural resources for
healing
• Herbs like Neem , Aloe vera,
Turmeric, Tulsi ( Holy basil),
Babool, Garlic etc.
8. Chinese
• The Chinese believe that all
things in creation possess
the qualities of yin and
yang, the opposing forces
of nature
• When the balance between
these two is lost, disease is
manifest.
• Diagnosis is performed
primarily through the pulse
and tongue.
9. Unani
• Unani tibb meaning ‘Ionian’
or ‘Greek’ medicine
• based on the Greek tradition
of four humours – blood,
phlegm, black and yellow
bile
10. Japanese
• Ancient Japanese
medical practices
involved exorcism, ritual
bathing and herbal
therapy
• kampo, using fewer
and smaller quantities of
herbs, often ground into
granules to be taken in
tea.
11. Aromatherapy
• It is the art of using the pure
essence extract to promote the
health and well-being of body
and mind.
• Relies primarily on the use of essential oils
• Common oils- lavender, eucalyptus, tea tree oil,
neem, tulsi and cinnamon etc
13. Neem (Azadirachta indica)
Plant family: Meliaceae
Plant used: Entire plant
Origin culture: Native to East India
and Burma
Common uses: Antiviral, antifungal, antibacterial,
antimalarial, antifertility, antiulcerogenic,
antihypersensitive and antihyperglycaemic,
antidermatophytic, orodontal, hepatoprotective and
anticancer activity.
Active constituents:
Diterpenoids, triterpenoids
(Azadirachtin), vilasinin type of
compounds, limonoids and its derivatives.
14. Jungli amla (Phyllanthus amarus)
Plant Family: Euphorbiaceae
Parts used: Entire plant
Origin: South India
Common uses: Hepatitis, Gonorrhea, frequent
menstruation, and Diabetes, anti-viral effect,
skin for sores, swelling, and itchiness.
Active constituents: Phyllanthin D,
hypophyllanthine and five flavonaoids
viz. quercertin, astralgin, quercertrin,
isoquercitrin and rutin.
15. Aloe vera
Plant family: Asphodelaceae
Part used: Leaf pulp
Origin culture: Sub-Saharan
African and Coptic traditional
medicine
Common uses: Treatment of burns, skin
blemishes, topical irritations,
antibacterial, digestive aid.
Active constituents:
Anthroquinones, anthrols,
anthrones, chrysophanic acid.
16. Garlic (Allium sativum)
Plant family: Alliaceae
Part used: Leaves & stem (together
. called the bulb)
Origin culture: Chinese, Coptic, Farsi,
Mediterranean, and Semitic traditional
medicine
Common uses: Immunostimulation and
augmented circulation, triglyceride and
cholesterol level reduction,
hypertension control.
Active constituents: Allicin, and
allyl sulfides.
17. Ginger (Zingiber officinale)
Plant family: Zingiberaceae
Part used: Rhizome
.
Origin culture: Chinese and
Indian traditional medicine.
Common uses: Digestive aid,
carminative, nausea/vomiting remedy,
anti-inflammatory.
Active constituents: Zingiberene,
gingerols/shogoals (volatile oils).
18. Ginseng (Panax ginseng)
Plant family: Araliaceae
. Part used: Roots/rhizomes
Origin culture: Chinese,
Korean, and Siberian
traditional medicine.
Common uses: Taken internally for
fatigue/endurance/stress, control high
and low blood pressure.
Active constituents:
Ginsenosides
19. Feverfew (Tanacetum parthenium)
Plant family: Asteraceae
Part used: Leaves
Origin culture: Mediterranean
traditional medicine.
Common uses: Migraine headaches,
fevers.
Active constituents: Parthenolide (a
sesquiterpene lactose), tanetin.
20. Ginkgo (Ginkgo biloba)
Plant family: Ginkgoaceae
. Part used: Leaves
Origin culture: Chinese
traditional medicine
Common uses: Improved memory,
Alzheimer’s disease, Parkinson’s
disease, improved circulation, post
stroke recovery.
Active constituents: Ginkgolides/
bilobalide and flavonoids
21. Milk Thistle (Silybum marianum)
Plant family: Asteraceae
.
Part used: Seeds
Origin culture: Mediterranean
traditional medicine.
Common uses: Hepatitis, liver diseases.
Active constituents: Silymarin,
silibinin, flavonoids.
22. St. Johns Wort
(Hypericum perforatum)
Plant family: Clusiaceae
Part used: Flowers & upper
stems/leaves
Origin culture: Greek traditional
medicine.
Common uses: Antidepressant,
Antiviral.
Active constituents: Volatile oil,
carotenes, taninnin, flavanoids
(inc. hypericin)
23. To make it more effective and
commercialized…
Principal concepts of research on new medicines
(Kuo-Hsiung Lee, 2005)
24. New approach
• Biotransformation:
The chemical conversion of an
exogenously supplied substance by living cell
cultures, permeabilzed cells or entrapped enzymes
derived from cell culture.( Yeoman et al., 1990)
• Single step or multiple step
• A method used to improve the product yield.
25. Production of digitoxin
• Cardiac glycosides from Digitalis species
for heart diseases
• Yeild from D. lanuta & D. purpurea were
low.
• Progesterone added for yield
Biotransformation of β-methyldigoxin by D. lanata cells in 201 bioreactor
over a period of 17 days
g%
β-Methyldigitoxin added 17.24 (100)
Unconverted β-methyldigitoxin 2.0 (11.8)
β-Methyldigoxin formed 14.36 (81.7)
By-product 0.28 (1.4)
Yield (94.90)
(Misawa, 1994)
26. Drawbacks
• Toxicities are not well defined in herbal medicine
• Risk of overdose is higher
• Too much believe in herbal therapy
• Herbs and other alternatives therapies are more likely
to abandon potentially beneficial conventional therapy
when faced with an illness.
30. Introduction
• Two most dreadful diseases
• Plants have formed the basis of sophisticated
traditional medicine systems that have been in
existence for thousands of years in countries, such
as China (Chang & But, 1986) and India (Kapoor,
1990).
• Plant-derived compounds have played an important
role in the development of several clinically
useful anti-cancer and anti-aids agents.
31. Plant- Derived Anti Cancer agents
First agents, vinca alkaloids (vinblastine and vincristine) from
the Madagascar periwinkle, Catharanthus roseus (Cragg et al.,
1994)
• Epipodophyllotoxin used as the active anti -tumour agent from
the genus Podophyllum (Cragg et al., 1994)
• Most recent additions are Paclitaxel (Taxus brevifolia),
campothecin (Camptotheca acuminata) homoharringtonine
(Cephalotaxus harringtonia var. Drupacea), elliptinium, a
derivative of ellipticine (Bleekeria vitensis), combretastatins,
(Combretum caffrum)
32. Contd…
• The leaves of T. baccata are used in the traditional Asiatic
Indian (Ayurvedic) medicine system (Kapoor, 1990), with one
reported use in the treatment of .cancer. (Hartwell, 1982)
• Homoharringtonine against various leukemias while elliptinium
for the treatment of breast cancer (Cragg et al., 1993b).
• The combretastatins (Combretum caffrum) which act as anti-
angiogenic agents, causing vascular shutdown in tumours
(Holwell et al., 2002).
33. Anti- HIV agents
• Michellamine B isolated from the leaves of the liana,
Ancistrocladus korupensis, (Boyd et al., 1994).
• Calophyllum lanigerum, yielded calanolide A which showed
significant anti-HIV activity (Kashman et al., 1992)
• Prostratin from Homalanthus nutans (Gustafson et al., 1992)
determined that prostratin is a potent activator of HIV
expression in latently infected T-cell lines
• Extracts of the Smokebush (Conospermum incurvum) yielded
conocurvone as the active agent (Decosterd et al., 1993)
34.
35. Introduction
• Aim of the study:
To study the production of cinnamyl alcohol glycosides by
biotransformation
• Rhodiola rosea is only the species that produce he
cinamyl alcohol glycosides
• Various secondary metabolites are the cinnamyl
alcohol glycosides (rosin, rosavin, rosarinand) &
tyrosol and its glycoside salidroside
• Field cultivation takes several year so cell and
tissues cultures give a satisfactory results
• Apart other compounds 337, 481, 483, and 321 are
also reported (Tolonen et al., 2004)
36. Biosynthetic pathway of salidroside and cinnamyl
alcohol glycosides
(A) (B)
Biosynthetic pathway of A) rosin, rosavin, rosarin and B) salidroside.
37. Materials and methods
Experimental material
Experiment with the precursors
Fresh and dry weight measurements
Chemical analyses
high performance liquid chromatography
with mass spectrometric detection
38. Results and discussion
• Growth of the cultures
• Production of the cinnamyl alcohol glycosides
Addition of glucose was beneficial concerning
the production
Rosin production increased
Rosavin was not produced in the original
medium
• Production of salidroside
• Addition of glucose to the medium show any
positive effect
• Accumulation pattern was same in both cases
39. Contd…
The content of rosin and rosavin in the callus cultivated with 2 mM cinnamyl alcohol in the original MS-Rh
medium (containing only sucrose) or in the glucose containing medium, during 14 days.
The content of salidroside in the callus cultivated with 2 mM tyrosol in the original MS-Rh medium
(containing only sucrose) or in the glucose containing medium, during 14 days.
(Gyorgy et al., 2005)
41. Conclusion
• Production of rosin and rosavin can be increased by
biotransformation
• Ultimately leads to satisfactory content of the
pharmacologically interesting compounds
42.
43. Introduction
• Aim of study
To study the anti-ulcer and ulcer-healing activity of OS.
• OC leaves 0.7% volatile oil comprising about 71%
eugenol and 20% methyl eugenol.
• Additional components are carvacrol, sesquiterpine
hydrocarbon caryophyllene, apigenin,
luteolin,apigenin-7-O-glucuronide, orientin,
molludistin and ursolic acid (Gupta et al., 2002)
44. Materials and methods
• Animals (rats/guinea pigs)
– Anti-ulcer study(6 rats6
guinea pigs)
– Ulcer healing study (20 rats/
20 guinea pigs)-acetic acid-
induced ulcer model.
• Treatment schedule
Control: Treatment:
OS extract and standard anti- OS extract and OMZ
ulcer drug Omeprazole (OMZ) 3 days
Ulcerogens
• Cold restraint stress induced
ulcers (CRU)
• Aspirin-induced ulcers (ASP)
• Alcohol-induced ulcers (AL)
• Histamine- induced ulcers (HST)
• Pylorus ligation-induced ulcers
(PL)
• Evaluation of ulcer-healing activity- acetic acid- induced ulcer model
45. Results
Effect of ethanolic extract of Ocimum sanctum and
omeprazole at doses of 50, 100 and 10 mg/kg body weight,
respectively, on percentage
protection of ulcer index in different anti-ulcer models.
Effect of ethanolic extract of Ocimum sanctum and
omeprazole at doses of 100 and 10 mg/kg body weight
per day, respectively, on percentage
protection of ulcer index in acetic acid-induced ulcer
model in rats after 5, 10, 15 and 20 days of drug
treatment.
(Dharmani et al., 2004)
46. Histopathology of acetic acid-induced ulcers
C T
Sections of ulcerated stomach obtained from
rats of control groups and treated with Ocimum
sanctum in acetic acid-induced ulcer model in
rats
after 5 days of treatment
C T
Sections of ulcerated stomach obtained from
rats of control groups and treated with Ocimum
sanctum in acetic acid-induced ulcer model in
rats
after 10 days of treatment
C T
Sections of ulcerated stomach obtained from
rats of control groups and treated with Ocimum
sanctum in acetic acid-induced ulcer model in
rats
after 15 days of treatment
(Dharmani et al., 2004)
47. Discussion and conclusion
• Report suggests that anti-stress and anti-oxidant activity of OS
which suggests the free radical scavenging effect of OS (Sen et
al., 1992).
• Ethanol induced ulcers are due to direct necrotizing effect of
ethanol on gastric mucosa (Miller and Henagan, 1984) so OS
increases mucus secretion.
• In PL, ulcers are developed due to accumulation of gastric acid
and pepsin which leads to auto-digestion of gastric mucosa
(Goel and Bhattacharya, 1991).