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DOI: 10.1055/s-2005-864106
In Vitro Antileishmanial Activity of Diphyllin Isolated from Haplophyllum bucharicum
Publication History
Received: July 15, 2004
Accepted: December 12, 2004
Publication Date:
27 April 2005 (online)
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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Carole Di Giorgio
Laboratoire de Parasitologie, Hygiène et Zoologie
Faculté de Pharmacie
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