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In vitro and in vivo activity of benzocphenanthridines against Leishmania amazonensis

In vitro and in vivo activity of benzocphenanthridines against Leishmania amazonensis

Castillo Pareja, Denis Helan; Sauvain, Michel Henri Auguste; Rivaud, Marion; Jullian, Valérie
URI: https://hdl.handle.net/20.500.12866/8065
Date: 2014

Abstract:

Seven benzo[c]phenanthridines, synthetic or isolated from Zanthoxylum rhoifolium root bark, were evaluated against Leishmania amazonensis axenic amastigotes. Five of them were considered leishmanicidal, with IC50 values ranging from 0.03 to 0.54 microM, and were evaluated on intramacrophagic amastigotes of L. amazonensis. Chelerythrine displayed the best activity (IC50=0.5 microM), which was in the same range as the reference compound amphotericin B (IC50=0.4 microM). In vivo studies with chelerythrine, avicine, and fagaridine on a model of mice cutaneous leishmaniasis resulted in the identification of fagaridine as the most active compound. Fagaridine decreased the parasitic burden more than 50% at the 3rd and 6th weeks after the end of treatment.

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