4-hydroxylonchocarpin and Leishmaniasis--Visceral

Antileishmanial activities of thirty-five synthetic chalcones have been examined. Among them, ten compounds (4, 6, 16, 22, 23, 24, 25, 29, 35 and 37) exhibited potent in vitro activity (IC50 range from 1.70 to 8 μM) against extracellular promastigotes and intracellular amastigotes form of Leishmania donovani. Two promising compounds 22 and 37 were tested in vivo in L. donovani/hamster model. Chalcone 37 showed 83.32% parasite inhibition at a dose of 50 mg/kg for 10 days whereas, 75.89% parasite inhibition at 100 mg/kg dose for 5 days by intraperitoneal route at day 7 post-treatment.

Topics: Animals; Cell Line; Chalcones; Chlorocebus aethiops; Cricetinae; Disease Models, Animal; Dose-Response Relationship, Drug; Injections, Intraperitoneal; Leishmania donovani; Leishmaniasis, Visceral; Macrophages; Mice; Molecular Structure; Parasitic Sensitivity Tests; Structure-Activity Relationship; Trypanocidal Agents; Vero Cells