In vitro activity of Triclisia patens and some bisbenzylisoquinoline alkaloids against Leishmania donovani and Tryanosoma brucei brucei

被引:36
作者
Camacho, MD
Phillipson, JD
Croft, SL
Rock, P
Marshall, SJ
Schiff, PL
机构
[1] Univ London, Sch Pharm, Ctr Pharmacognosy & Phytotherapy, London WC1N 1AX, England
[2] Univ London London Sch Hyg & Trop Med, Dept Infect & Trop Dis, London WC1E 7HT, England
[3] Univ Pittsburgh, Sch Pharm, Dept Pharmaceut Sci, Pittsburgh, PA 15261 USA
关键词
Triclisia patens; menispermaceae; bisbenzylisoquinoline alkaloids; antileishmanial activity; antitrypanosomal activity; Leishmania donovani; Trypanosoma brucei;
D O I
10.1002/ptr.929
中图分类号
R914 [药物化学];
学科分类号
100701 [药物化学];
摘要
In the search for antiprotozoal compounds from natural sources, Triclisia patens displayed activity against L. donovani promastigotes (IC50 = 1.5 mug/mL) and T.b. brucei blood stream trypomastigote forms (IC50 = 31.25 mug/mL). In addition, a total of 20 bisbenzylisoquinoline alkaloids were screened for antileishmanial and antitrypanosomal activity in vitro. Fangchinoline (IC50 = 0.39 muM) was found to be as active as the standard pentamidine against Leishmania donovani promastigotes. Phaeanthine was threefold more active IC50 = 2.41 muM; 1.5 mug/mL) than the standard drug Pentostam against L. donovani amastigotes, but at this concentration was toxic to murine macrophages. In contrast, cocsoline IC50 = 12.3 muM; 6.76 mug/mL) was as active as Pentostam, and was not toxic to macrophages at this concentration. Thalisopidine showed the strongest activity (IC50) = 1.14 muM) against Trypanosoma brucei brucei blood stream form trypomastigotes, but was less active than pentamidine. Copyright (C) 2002 John Wiley Sons, Ltd.
引用
收藏
页码:432 / 436
页数:5
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