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In vitro antileishmanial activity of diphyllin isolated from Haplophyllum bucharicum.

Title: In vitro antileishmanial activity of diphyllin isolated from Haplophyllum bucharicum.
Authors: Di Giorgio C; Laboratoire de Parasitologie Hygiène et Zoologie, Faculté de Pharmacie, Marseille, France. Carole.Digiorgio@Pharmacie.univ-mrs.fr; Delmas F; Akhmedjanova V; Ollivier E; Bessonova I; Riad E; Timon-David P
Source: Planta medica [Planta Med] 2005 Apr; Vol. 71 (4), pp. 366-9.
Publication Type: Journal Article
Language: English
Journal Info: Publisher: George Thieme Country of Publication: Germany NLM ID: 0066751 Publication Model: Print Cited Medium: Print ISSN: 0032-0943 (Print) Linking ISSN: 00320943 NLM ISO Abbreviation: Planta Med Subsets: MEDLINE
Imprint Name(s): Publication: Stuttgart ; New York : George Thieme; Original Publication: Stuttgart, Hippokrates Verlag.
MeSH Terms: Phytotherapy* ; Rutaceae*; Antiprotozoal Agents/*pharmacology ; Leishmania/*drug effects ; Plant Extracts/*pharmacology; Antiprotozoal Agents/administration & dosage ; Antiprotozoal Agents/therapeutic use ; Cell Cycle/drug effects ; Dioxolanes/administration & dosage ; Dioxolanes/pharmacology ; Dioxolanes/therapeutic use ; Leishmaniasis/drug therapy ; Lignans/administration & dosage ; Lignans/pharmacology ; Lignans/therapeutic use ; Macrophages/parasitology ; Plant Extracts/administration & dosage ; Plant Extracts/therapeutic use ; Animals ; Benzodioxoles ; Parasitic Sensitivity Tests ; Plant Components, Aerial
Abstract: 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.
Substance Nomenclature: 0 (Antiprotozoal Agents); 0 (Benzodioxoles); 0 (Dioxolanes); 0 (Lignans); 0 (Plant Extracts); W4PN5LDP26 (diphyllin)
Entry Date(s): Date Created: 20050428 Date Completed: 20050621 Latest Revision: 20210809
Update Code: 20260130
DOI: 10.1055/s-2005-864106
PMID: 15856417
Database: MEDLINE

Journal Article