Therapeutics values of plant    derived compounds                   Punyakishore Maibam
Quotation“Within the infant rind of this small flower      Poison hath residence and medicine power:For this, being smelt,...
Introduction• Powerful ingredients.• Only 15% of estimated plant species on earth have  been investigated for possible Med...
History•   History of traditional medicine in eastern culture     – Ayurveda medicine     – Chinese medicine•   History of...
Traditional Healing Systems
Ayurveda     The aim of Ayurveda isproper maintenance ofmetabolic equilibrium of thehuman psychosomaticmaterial and the re...
Contd…• Ayurveda utilizes herbs and  product from natural resources for  healing•   Herbs like Neem , Aloe vera,    Turmer...
Chinese• The Chinese believe that all  things in creation possess  the qualities of yin and  yang, the opposing forces  of...
Unani• Unani tibb meaning ‘Ionian’  or ‘Greek’ medicine• based on the Greek tradition  of four humours – blood,  phlegm, b...
Japanese• Ancient Japanese  medical practices  involved exorcism, ritual  bathing and herbal  therapy            • kampo, ...
Aromatherapy• It is the art of using the pure  essence extract to promote the  health and well-being of body  and mind.• R...
Common plants used with its   derived products
Neem (Azadirachta indica)Plant family: Meliaceae    Plant used: Entire plant          Origin culture: Native to East India...
Jungli amla (Phyllanthus amarus)Plant Family: Euphorbiaceae    Parts used: Entire plant           Origin: South India     ...
Aloe veraPlant family: Asphodelaceae      Part used: Leaf pulp               Origin culture: Sub-Saharan               Afr...
Garlic (Allium sativum)Plant family: Alliaceae       Part used: Leaves & stem (together.      called the bulb)            ...
Ginger (Zingiber officinale)Plant family: Zingiberaceae     Part used: Rhizome.            Origin culture: Chinese and    ...
Ginseng (Panax ginseng)Plant family: Araliaceae.      Part used: Roots/rhizomes                 Origin culture: Chinese,  ...
Feverfew (Tanacetum parthenium)Plant family: Asteraceae    Part used: Leaves           Origin culture: Mediterranean      ...
Ginkgo (Ginkgo biloba)Plant family: Ginkgoaceae.    Part used: Leaves          Origin culture: Chinese          traditiona...
Milk Thistle (Silybum marianum)Plant family: Asteraceae.       Part used: Seeds              Origin culture: Mediterranean...
St. Johns Wort          (Hypericum perforatum)Plant family: Clusiaceae    Part used: Flowers & upper    stems/leaves      ...
To make it more effective and     commercialized… Principal concepts of research on new medicines                         ...
New approach • Biotransformation:              The chemical conversion of an   exogenously supplied substance by living ce...
Production of digitoxin         • Cardiac glycosides from Digitalis species           for heart diseases         • Yeild f...
Drawbacks• Toxicities are not well defined in herbal medicine• Risk of overdose is higher• Too much believe in herbal ther...
Reported Adverse Effects of Some Common Herbs   (Winslow et al., 1998)
Case studies
Introduction• Two most dreadful diseases• Plants have formed the basis of sophisticated  traditional medicine systems that...
Plant- Derived Anti Cancer agents    First agents, vinca alkaloids (vinblastine and vincristine) from    the Madagascar pe...
Contd…•    The leaves of T. baccata are used in the traditional Asiatic    Indian (Ayurvedic) medicine system (Kapoor, 199...
Anti- HIV agents•   Michellamine B isolated from the leaves of the liana,    Ancistrocladus korupensis, (Boyd et al., 1994...
Introduction•   Aim of the study:         To study the production of cinnamyl alcohol glycosides by          biotransform...
Biosynthetic pathway of salidroside and cinnamyl               alcohol glycosides                   (A)                   ...
Materials and methods      Experimental material      Experiment with the precursors      Fresh and dry weight measurem...
Results and discussion•   Growth of the cultures•   Production of the cinnamyl alcohol glycosides       Addition of gluco...
Contd…     The content of rosin and rosavin in the callus cultivated with 2 mM cinnamyl alcohol in the original MS-Rh     ...
Pharmacological effects of the alcohol-aqueous extract of Rhodiola rosea                                                  ...
Conclusion• Production of rosin and rosavin can be increased by    biotransformation• Ultimately leads to satisfactory con...
Introduction• Aim of study    To study the anti-ulcer and ulcer-healing activity of OS.• OC leaves 0.7% volatile oil comp...
Materials and methods           •      Animals (rats/guinea pigs)                –    Anti-ulcer study(6 rats6            ...
Results   Effect of ethanolic extract of Ocimum sanctum andomeprazole at doses of 50, 100 and 10 mg/kg body weight,       ...
Histopathology of acetic acid-induced ulcers      C                       T                                               ...
Discussion and conclusion•   Report suggests that anti-stress and anti-oxidant activity of OS    which suggests the free r...
Conclusion
Doubts please !!!
Thank you
Therapeutics values of plant derived compounds
Therapeutics values of plant derived compounds
Therapeutics values of plant derived compounds
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Therapeutics values of plant derived compounds

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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

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Therapeutics values of plant derived compounds

  1. 1. Therapeutics values of plant derived compounds Punyakishore Maibam
  2. 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. 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. 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
  5. 5. Traditional Healing Systems
  6. 6. Ayurveda The aim of Ayurveda isproper maintenance ofmetabolic equilibrium of thehuman psychosomaticmaterial and the restoration ofthe same to the normal whendisturbed
  7. 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. 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. 9. Unani• Unani tibb meaning ‘Ionian’ or ‘Greek’ medicine• based on the Greek tradition of four humours – blood, phlegm, black and yellow bile
  10. 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. 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
  12. 12. Common plants used with its derived products
  13. 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. 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. 15. Aloe veraPlant 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. 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. 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. 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. 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. 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. 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. 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. 23. To make it more effective and commercialized… Principal concepts of research on new medicines (Kuo-Hsiung Lee, 2005)
  24. 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. 25. Production of digitoxin • Cardiac glycosides from Digitalis species for heart diseases • Yeild from D. lanuta & D. purpurea were low. • Progesterone added for yieldBiotransformation 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. 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.
  27. 27. Reported Adverse Effects of Some Common Herbs (Winslow et al., 1998)
  28. 28. Case studies
  29. 29. 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.
  30. 30. 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)
  31. 31. 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).
  32. 32. 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)
  33. 33. 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)
  34. 34. Biosynthetic pathway of salidroside and cinnamyl alcohol glycosides (A) (B) Biosynthetic pathway of A) rosin, rosavin, rosarin and B) salidroside.
  35. 35. Materials and methods  Experimental material  Experiment with the precursors  Fresh and dry weight measurements  Chemical analyses  high performance liquid chromatography with mass spectrometric detection
  36. 36. 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
  37. 37. 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)
  38. 38. Pharmacological effects of the alcohol-aqueous extract of Rhodiola rosea (Gyorgy et al., 2006)
  39. 39. Conclusion• Production of rosin and rosavin can be increased by biotransformation• Ultimately leads to satisfactory content of the pharmacologically interesting compounds
  40. 40. 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)
  41. 41. 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 scheduleControl: 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
  42. 42. Results Effect of ethanolic extract of Ocimum sanctum andomeprazole 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)
  43. 43. 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 fromrats 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)
  44. 44. 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).
  45. 45. Conclusion
  46. 46. Doubts please !!!
  47. 47. Thank you
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