Catharanthine Explained

Catharanthine is a terpene indole alkaloid produced by the medicinal plant Catharanthus roseus and Tabernaemontana divaricata. Catharanthine is derived from strictosidine, but the exact mechanism by which this happens is currently unknown. Catharanthine is one of the two precursors that form vinblastine, the other being vindoline.

Pharmacology

(+)-Catharanthine competitively inhibits α9α10 nAChRs with potencies higher than that at α3β4 and α4β2 nAChRs and directly blocks Ca_V2.2.^[1] Catharanthine alkaloids are non competitive antagonist of muscle type nAChRs and this is thought to be the case due to presence of catharanthine moiety in those compounds.^[2] In in vitro study, it increased the levels of cAMP by inhibiting cAMP phosphodiesterase in brain.^[3] It is a potent inhibitor of TRPM8, similar to BCTC.^[4] Structural analysis of catharanthine shows activity on TRPM8, TRPA1, and butyrylcholinesterase.^[5]

See also

• Akuammicine
• Conopharyngine
• Stemmadenine
• Tabersonine

External links

• 23532933 . 2013 . Jadhav . A. . Liang . W. . Papageorgiou . P. C. . Shoker . A. . Kanthan . S. C. . Balsevich . J. . Levy . A. S. . Heximer . S. . Backx . P. H. . Gopalakrishnan . V. . Catharanthine dilates small mesenteric arteries and decreases heart rate and cardiac contractility by inhibition of voltage-operated calcium channels on vascular smooth muscle cells and cardiomyocytes . The Journal of Pharmacology and Experimental Therapeutics . 345 . 3 . 383–392 . 10.1124/jpet.112.199661 . 206501362 .

Notes and References

1. Arias HR, Tae HS, Micheli L, Yousuf A, Ghelardini C, Adams DJ, Di Cesare Mannelli L . Coronaridine congeners decrease neuropathic pain in mice and inhibit α9α10 nicotinic acetylcholine receptors and CaV2.2 channels . . 175 . 108194 . September 2020 . 32540451 . 10.1016/j.neuropharm.2020.108194 . 2158/1213504 . 219705597 . free .
2. Arias HR, Feuerbach D, Targowska-Duda KM, Jozwiak K . Catharanthine alkaloids are noncompetitive antagonists of muscle-type nicotinic acetylcholine receptors . . 57 . 2 . 153–61 . September 2010 . 20493225 . 10.1016/j.neuint.2010.05.007 . 24594292 .
3. Web site: Ethnobotany and ethnopharmacology of Tabernaemontana divaricata.
4. Terada Y, Kitajima M, Taguchi F, Takayama H, Horie S, Watanabe T . Identification of Indole Alkaloid Structural Units Important for Stimulus-Selective TRPM8 Inhibition: SAR Study of Naturally Occurring Iboga Derivatives . . 77 . 8 . 1831–8 . August 2014 . 25052206 . 10.1021/np500235b .
5. Web site: Catharanthine . SwissTargetPrediction .