| Antifungal canthin-6-one series accumulate in lipid droplets and affect fatty acid metabolism in Saccharomyces cerevisiae. | |
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MedLine Citation:
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PMID: 17888617 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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The mechanism of action of antifungal canthin-6-one series was investigated in Saccharomyces cerevisiae. After a rapid uptake, a preferential accumulation of the drug within lipid droplets was observed. The antifungal action of canthin-6-one was found as reversible. Canthin-6-one did not exhibit affinity for sterols, and membrane ergosterol was not necessary for the antifungal activity since the MICs were similar on an ergosterol-deleted and the wild-type S. cerevisiae clones. Relative amount of unsaturated alkyl chain fatty acids was significantly enhanced suggesting a stimulation of desaturase enzyme systems. No synergistic effect was observed between canthin-6-one and amphotericin B, ketoconazole and caspofungine. Canthin-6-one should now be evaluated in vivo against fungal pathogens. |
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Authors:
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D Lagoutte; V Nicolas; E Poupon; A Fournet; R Hocquemiller; D Libong; P Chaminade; P M Loiseau |
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Publication Detail:
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Type: Comparative Study; Journal Article Date: 2007-08-23 |
Journal Detail:
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Title: Biomedicine & pharmacotherapy = Biomédecine & pharmacothérapie Volume: 62 ISSN: 0753-3322 ISO Abbreviation: Biomed. Pharmacother. Publication Date: 2008 Feb |
Date Detail:
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Created Date: 2008-02-15 Completed Date: 2008-06-02 Revised Date: 2009-11-19 |
Medline Journal Info:
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Nlm Unique ID: 8213295 Medline TA: Biomed Pharmacother Country: France |
Other Details:
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Languages: eng Pagination: 99-103 Citation Subset: IM |
Affiliation:
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Laboratoire de Pharmacognosie et Chimiothérapie Antiparasitaire, UMR 8076 CNRS, Faculté de Pharmacie, Univ Paris-Sud, 92290 Châtenay-Malabry, France. |
Export Citation:
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| MeSH Terms | |
Descriptor/Qualifier:
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Amphotericin B
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pharmacology Antifungal Agents / isolation & purification, pharmacokinetics, pharmacology* Drug Synergism Fatty Acid Desaturases / drug effects, metabolism Fatty Acids / metabolism Indoles / isolation & purification, pharmacology* Ketoconazole / pharmacology Microbial Sensitivity Tests Naphthyridines / isolation & purification, pharmacology* Saccharomyces cerevisiae |
| Chemical | |
Reg. No./Substance:
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0/Antifungal Agents; 0/Fatty Acids; 0/Indoles; 0/Naphthyridines; 0/canthin-6-one; 1397-89-3/Amphotericin B; 65277-42-1/Ketoconazole; EC 1.14.19.-/Fatty Acid Desaturases |
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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