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Apocynaceae.pptx
- 1. FAMILY APOCYNACEAE By Ms. Yamema Younatan Lecturer, Department of Pharmacy CECOS University, Peshawar
- 2. RAUWOLFIA
- 3. INTRODUCTION BOTANICAL NAME Rouwolfia serpentina SYNONYMS Sarpagandha, Chandrika; Indian snake root FAMILY/PART USED Apocynaceae/ Rhizome and roots DISTRIBUTION It is an erect, evergreen, small shrub native to the Orient and occurs from India to Sumatra. It is also found in Burma, Thailand, Philippines, Vietnam, Indonesia, Malaysia, Pakistan and Java.
- 4. • Leaves • Leaves of the plant are in whorls of three, elliptic to lanceolate or obovate, bright green above and below pale green and thin. • Flowers • White, pinkish or red, occurring in whorls PLANT MORPHOLOGY
- 5. • Fruit • fruit are tiny, oval, fleshy which turn a shiny purple-black when ripe. PLANT MORPHOLOGY
- 6. • Roots and rhizomes are almost identical in external characters • Cylindrical or slightly tapering, tortuous piece • Pieces of rhizome closely resemble the root but may be identified by a small central pith; they occasionally have attached to them small pieces of aerial stem • Outer surface is greyish-yellow, light brown or brown with slight wrinkles (young pieces) or longitudinal ridges (older pieces) • Recently dried drug has a slight odour PLANT MORPHOLOGY
- 7. CHEMICAL CONSTITUENTS 0.7 – 2.4% At least 40 alkaloids • Reserpine • Rescinamine • Ajmaline • Ajmalicine • Ajmalinine • Serpentine • Serpentinine
- 8. CULTIVATION AND COLLECTION Drug is collected mainly from wild plants, but cultivation of the drug will probably increase as wild plants become more scarce Collectors instructed to leave root for future growth Endangered species in India Potential for the regeneration of plants from cell cultures and the possible utilization of nodal culture
- 9. USES • Rauwolfia is used as hypnotic, sedative and antihypertensive. It is specific for insanity, reduces blood pressure and cures pain. It is given in labours to increase uterine contractions and in certain neuropsychiatric disorders • Reserpine is an adrenergic blocking agent and used an antihypertensive and tranquilizer • Rescinnamine is also used as an antihypertensive. • Ajmaline, which has pharmacological properties similar to those of quinidine, is marketed in Japan for the treatment of cardiac arrhythmias • An estimated 3500 kg of ajmalicine (δ-yohimbine, raubasine) is isolated annually from either Rauwolfia or Catharanthus spp. by pharmaceutical industries for the treatment of hypertension and circulatory diseases • Conflicting reports on the possible involvement of the rauwolfia alkaloids in breast cancer engendered a natural hesitation in their use.
- 10. VINCA
- 11. INTRODUCTION BOTANICAL SOURCE Vinca is the dried entire plant of Catharanthus roseus Linn COMMON NAME Vinca rosea, Catharanthus, Madagascar periwinkle Barmasi, Sadabahar, Ratanjot FAMILY/PART USED Apocynaceae/Entire plant DISTRIBUTION The plant is a native of Madagascar and is found in many tropical and subtropical countries especially in India, Pakistan, Australia, South Africa and North and South America.
- 12. INTRODUCTION • Genus Catharanthus is from Greek word ‘Katharos’ which means ‘pure perfect flower. • Species ‘roseus’ means ‘rose-like’.
- 13. • Leaves are simple, glossy dark green, oval in shape, opposite arrangement, measuring about 2.5 - 3.5 cm long. Leaves are decussate and subsessile. • Stem is erect with flexible long branches, purple or light green. If bruised or cut, stems secrete milky- white sap. • It has characteristic odour and bitter taste. PLANT MORPHOLOGY
- 14. PLANT MORPHOLOGY
- 15. CHEMICAL CONSTITUENTS Present in entire shrub but leaves and roots contain more alkaloids. Main alkaloids: • Vincristine (leurocristine) • Vinblastine (vincaleukoblastine) • Ajmalicine • Lochnerine • Serpentine
- 17. CHEMICAL CONSTITUENTS • Present only in small concentrations • Vincristine 0.0002% yield from the crude drug • Large quantity of plant required • More demand for vincristine, plant produces more vinblastine • Conversion of vinblastine to vincristine chemically or microbiologically • Cell cultures method being investigated for growth now
- 18. USES • Vinblastin is an antitumour alkaloid used in the treatment of Hodgkin and non-Hodgkin lymphomas • Vincristine is a cytotoxic compound and used to treat leukaemia in children. other applications for lymphomas, small-cell lung cancer, cervical and breast cancers • Vincristine has a superior antitumour activity compared to vinblastine, but is more neurotoxic • Semi-synthetic Vindesine is also used in the treatment of acute lymphoid leukaemia in children
Editor's Notes
- Rauwolfia contains at least 40 alkaloids, which total some 0.7–2.4%. In 1931 Salimuzzaman Siddiqui isolated ajmaline (rauwolfine), ajmalinine, ajmalicine, serpentine and serpentinine. Ajmaline is named after Hakim Ajmal Khan. The chief therapeutically important alkaloids are reserpine and rescinnamine.
- The drug is collected mainly from wild plants, but cultivation of the drug will probably increase as wild plants become more scarce; in parts of India collectors are required to leave some root from each plant in the ground for future growth. Nevertheless, and coupled with the low seed viability, the plant is regarded as an endangered species in India. Consequently, the potential for the regeneration of plants from cell cultures and the possible utilization of nodal culture has received some attention
- Present in entire shrub but leaves and roots contain more alkaloids. The important alkaloids in Catharanthus are Vinblastine and Vincristine and they possess definite anticancer activity. These compounds are bisindole in chemistry. Other alkaloids are Ajmalicine, Lochnerine and Serpentine. Bisindole natural products consist of two monomeric indole alkaloid units as their obligate constituents. Bisindoles are more potent with respect to their biological activity than their corresponding monomeric units.
- Vincristine is structurally similar to vinblastine, but has a formyl group rather than a methyl on the indole nitrogen in the vindoline-derived portion
- Because these alkaloids are only minor constituents of the plant (vincristine is obtained in about 0.0002% yield from the crude drug), large quantities of raw material are required and chromatographic fractionations are extensively employed in the isolation procedures. In addition, there is a growing demand for vincristine rather than vinblastine, but the plant produces a much higher proportion of vinblastine. Fortunately, it is now possible to convert vinblastine into vincristine either chemically, or via a microbiological N-demethylation using Streptomyces albogriseolus. In efforts to improve the production of alkaloids, cell cultures of C. roseus have received considerable attention. Success has been achieved in obtaining total alkaloid yields corresponding to 0.1–1.5% dry weight cultured cells, but cultures produced catharanthine and tabersonine, and not vindoline, so lacked one of the essential precursors for formation of the bisindole alkaloids. A similar problem arises with transformed root cultures although the feeding of loganin alone at the early stationary phase has been shown to increase the ajmalicine production 2.3-fold and the serpentine 1.8-fold when compared with control cultures; catharanthine levels are unaffected by a single feed of the precursor. Research is still necessary to find means of inducing the production of the useful alkaloids.