Trypanocidal and leishmanicidal activity of six limonoids

AbstractSix limonoids [kotschyienone A and B (1,2), 7-deacetylgedunin (3), 7-deacetyl-7-oxogedunin (4), andirobin (5) and methyl angolensate (6)] were investigated for their trypanocidal and leishmanicidal activities using bloodstream forms ofTrypanosoma brucei and promastigotes ofLeishmania major. Whereas all compounds showed anti-trypanosomal activity, only compounds1 –4 displayed anti-leishmanial activity. The 50% growth inhibition (GI50) values for the trypanocidal and leishmanicidal activity of the compounds ranged between 2.5 and 14.9  μM. Kotschyienone A (1) was found to be the most active compound with a minimal inhibition concentration (MIC) value of 10  μM and GI50 values between 2.5 and 2.9  μM. Only compounds1 and3 showed moderate cytotoxicity against HL-60 cells with MIC and GI50 values of 100  μM and 31.5–46.2 μM, respectively. Compound1 was also found to show activity against intracellular amastigotes ofL. major with a GI50 value of 1.5  μM. The results suggest that limonoids have potential as drug candidates for the development of new treatments against trypanosomiasis and leishmaniasis.
Source: Journal of Natural Medicines - Category: Drugs & Pharmacology Source Type: research