In Vitro Antileishmanial Activity of Diphyllin Isolated from Haplophyllum bucharicum

Abstract

Diphyllin isolated from Haplophyllum bucharicum Litv. (Rutaceae), an endemic plant of Uzbekistan, displayed a moderate antiproliferative activity towards human monocytes (IC₅₀ = 35.2 μM) and Leishmania promastigotes (IC₅₀ = 14.4 μM), by a mechanism of action that involved interaction with macromolecules and resulted in cell cycle arrest in the S-phase and inhibition of protein synthesis. In the intracellular amastigote form of the parasite, diphyllin exerted a strong specific inhibitory activity (IC₅₀ = 0.2 μM) resulting from the inhibition of parasite internalization within macrophages. This property was mainly due to modulation of macrophage phagocytosis and, to a lesser extent, it also involved interference with surface molecules of the promastigote membrane.

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