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Altered sterol profile induced in Leishmania amazonensis by a natural dihydroxymethoxylated chalcone.
Title | Altered sterol profile induced in Leishmania amazonensis by a natural dihydroxymethoxylated chalcone. |
Publication Type | Journal Article |
Year of Publication | 2009 |
Authors | Torres-Santos, ECaio, Sampaio-Santos, MIsabel, Buckner, FS, Yokoyama, K, Gelb, M, Urbina, JA, Rossi-Bergmann, B |
Journal | J Antimicrob Chemother |
Volume | 63 |
Issue | 3 |
Pagination | 469-72 |
Date Published | 2009 Mar |
ISSN | 1460-2091 |
Keywords | Animals, Antiprotozoal Agents, Chalcone, Chromatography, Thin Layer, Enzyme Inhibitors, Gas Chromatography-Mass Spectrometry, Leishmania, Sterols |
Abstract | OBJECTIVES: The effects of the antileishmanial chalcone 2',6'-dihydroxy-4'-methoxychalcone (DMC) on Leishmania amazonensis sterol composition and biosynthesis were investigated to obtain information about the mechanism of growth inhibition by DMC on this parasite. METHODS: The interference of sterol biosynthesis by DMC was studied in drug-treated promastigotes by two different methods. (i) Newly synthesized sterols from parasites grown in the presence of [(3)H]mevalonate were analysed by thin layer chromatography (TLC)/fluorography. (ii) Total sterols extracted from the parasites grown with or without DMC were characterized by gas chromatography coupled to mass spectroscopy (GC/MS). RESULTS: TLC and GC/MS analyses of sterols extracted from DMC-treated promastigotes revealed the accumulation of early precursors and a reduction in the levels of C-14 demethylated and C-24 alkylated sterols, as well as a reduction in exogenous cholesterol uptake. CONCLUSIONS: This study demonstrates that the natural chalcone DMC alters the sterol composition of L. amazonensis and suggests that the parasite target is different from other known sterol inhibitors. |
DOI | 10.1093/jac/dkn546 |
Alternate Journal | J. Antimicrob. Chemother. |
PubMed ID | 19176591 |