In vitro antileishmanial activity of diphyllin isolated from Haplophyllum bucharicum.
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.
Di Giorgio
Carole
C
Laboratoire de Parasitologie Hygiène et Zoologie, Faculté de Pharmacie, Marseille, France. Carole.Digiorgio@Pharmacie.univ-mrs.fr
Delmas
Florence
F
Akhmedjanova
Valentina
V
Ollivier
Evelyne
E
Bessonova
Iraida
I
Riad
Elias
E
Timon-David
Pierre
P
D000818:Animals; D000981:Antiprotozoal Agents / Q000008:administration & dosage / Q000494:pharmacology* / Q000627:therapeutic use; D052117:Benzodioxoles; D002453:Cell Cycle / Q000187:drug effects; D004148:Dioxolanes / Q000008:administration & dosage / Q000494:pharmacology / Q000627:therapeutic use; D007891:Leishmania / Q000187:drug effects*; D007896:Leishmaniasis / Q000188:drug therapy; D017705:Lignans / Q000008:administration & dosage / Q000494:pharmacology / Q000627:therapeutic use; D008264:Macrophages / Q000469:parasitology; D021261:Parasitic Sensitivity Tests; D008517:Phytotherapy; D035261:Plant Components, Aerial; D010936:Plant Extracts / Q000008:administration & dosage / Q000494:pharmacology* / Q000627:therapeutic use; D027821:Rutaceae
D000981:Antiprotozoal Agents; D052117:Benzodioxoles; D004148:Dioxolanes; D017705:Lignans; D010936:Plant Extracts; C010130:diphyllin