In vitro activity of Triclisia patens and some bisbenzylisoquinoline alkaloids against Leishmania donovani and Trypanosoma brucei brucei.
In the search for antiprotozoal compounds from natural sources, Triclisia patens displayed activity against L. donovani promastigotes (IC(50) = 1.5 microg/mL) and T. b. brucei blood stream trypomastigote forms (IC(50) = 31.25 microg/mL). In addition, a total of 20 bisbenzylisoquinoline alkaloids were screened for antileishmanial and antitrypanosomal activity in vitro. Fangchinoline (IC(50) = 0.39 microM) was found to be as active as the standard pentamidine against Leishmania donovani promastigotes. Phaeanthine was three-fold more active (IC(50) = 2.41 microM; 1.5 microg/mL) than the standard drug Pentostam against L. donovani amastigotes, but at this concentration was toxic to murine macrophages. In contrast, cocsoline (IC(50) = 12.3 microM; 6.76 microg/mL) was as active as Pentostam, and was not toxic to macrophages at this concentration. Thalisopidine showed the strongest activity (IC(50) = 1.14 microM) against Trypanosoma brucei brucei blood stream form trypomastigotes, but was less active than pentamidine.
Centre for Pharmacognosy and Phytotherapy, The School of Pharmacy, University of London, 29-39 Brunswick Square, London WC 1N 1AX, UK.
Maria
M
del Rayo Camacho
J David
JD
Phillipson
Simon L
SL
Croft
Peter
P
Rock
Sarah J
SJ
Marshall
Paul L
PL
Schiff
D000470:Alkaloids / Q000009:adverse effects / Q000737:chemistry* / Q000494:pharmacology*; D000818:Animals; D000981:Antiprotozoal Agents / Q000009:adverse effects / Q000737:chemistry* / Q000494:pharmacology*; D002470:Cell Survival / Q000187:drug effects; D020128:Inhibitory Concentration 50; D007893:Leishmania donovani / Q000187:drug effects*; D008264:Macrophages / Q000166:cytology / Q000187:drug effects; D029583:Menispermaceae / Q000737:chemistry*; D051379:Mice; D015394:Molecular Structure; D010936:Plant Extracts / Q000737:chemistry; D018515:Plant Leaves / Q000737:chemistry; D014344:Trypanocidal Agents / Q000009:adverse effects / Q000737:chemistry / Q000494:pharmacology; D014346:Trypanosoma brucei brucei / Q000187:drug effects*
D000470:Alkaloids; D000981:Antiprotozoal Agents; D010936:Plant Extracts; D014344:Trypanocidal Agents