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DOI: 10.1055/s-2000-8661
Leishmanicidal, Antiplasmodial and Cytotoxic Activity of Indole Alkaloids from Corynanthe pachyceras
Publication History
Publication Date:
31 December 2000 (online)
Abstract
Five indole alkaloids, corynantheidine, corynantheine, dihydrocorynantheine, α-yohimbine and corynanthine were isolated from bark of Corynanthe pachyceras K. Schum. (Rubiaceae). The structures were established by spectroscopic methods, inlcuding previously unreported assignment of all 1H-NMR resonances by COSY and NOESY experiments. These and related alkaloids showed pronounced activity against Leishmania major promastigotes (IC50 at the micromolar level) but no significant in vitro antiplasmodial activity (against chloroquine-sensitive Plasmodium falciparum). Cytotoxicity assessed with drug sensitive KB-3-1 and multidrug-resistant KB-V1 cell lines was low; the alkaloids are apparently not substrates for the P-glycoprotein (P-170) efflux pump.
Key words
Indole alkaloids - Plasmodium - Leishmania - multi-drug resistance - NMR
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Prof. Jerzy W. Jaroszewski
Department of Medicinal Chemistry The Royal Danish School of Pharmacy
Universitetsparken 2
DK-2100 Copenhagen
Denmark
Email: jj@dfh.dk
Phone: +45 3530 6040