In vitro antileishmanial properties of new flavonoids against Leishmania donovani

This study focuses on the in vitro antileishmanial evaluation of twenty original flavones which differ in substituent of the A-ring, mainly at C-7, and in substitution pattern of the lateral B-ring against Leishmania donovani. Flavonoids were evaluated in vitro against L. donovani promastigotes wild-type and drug-resistant lines using the MTT test and against intramacrophage amastigotes using a reporter gene luciferase assay. Cytotoxicity was evaluated on KB cell line. The most active compounds 7, 11 and 14, showed IC50 values on the intramacrophage amastigotes in a range from 1.7 to 3.6 μM with a selective index 29.9 for compound 14. Compound 14 being about 6-fold more active than miltefosine on this L. donovani intramacrophage amastigote model, it is proposed for a further in vivo evaluation.