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<i>In Vitro</i>Antileishmanial Activity of Diphyllin Isolated from<i>Haplophyllum bucharicum</i>

Carole Di GiorgioLaboratoire de Parasitologie Hygiène et Zoologie, Faculté de Pharmacie, Marseille, France. [email protected]F. DelmasValentina AkhmedjanovaLaboratory of the Chemistry of Alkaloids, S. Yu. Yunusov Institute of the Chemistry of Plant Substances, Tashkent, UzbekistanÉvelyne OllivierLaboratoire de Pharmacognosie, Faculté de Pharmacie, Marseille, FranceI. A. BessonovaLaboratory of the Chemistry of Alkaloids, S. Yu. Yunusov Institute of the Chemistry of Plant Substances, Tashkent, UzbekistanElias RiadLaboratoire de Pharmacognosie, Faculté de Pharmacie, Marseille, FranceP Timon-David
Planta Medicajournal2005en
ABI

Аннотация

Diphyllin isolated from Haplophyllum bucharicum Litv. (Rutaceae), an endemic plant of Uzbekistan, displayed a moderate antiproliferative activity towards human monocytes (IC50 = 35.2 microM) and Leishmania promastigotes (IC50 = 14.4 microM), 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 microM) 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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