Document Detail

Antifungal canthin-6-one series accumulate in lipid droplets and affect fatty acid metabolism in Saccharomyces cerevisiae.
MedLine Citation:
PMID:  17888617     Owner:  NLM     Status:  MEDLINE    
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.
D Lagoutte; V Nicolas; E Poupon; A Fournet; R Hocquemiller; D Libong; P Chaminade; P M Loiseau
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Publication Detail:
Type:  Comparative Study; Journal Article     Date:  2007-08-23
Journal Detail:
Title:  Biomedicine & pharmacotherapy = Biomédecine & pharmacothérapie     Volume:  62     ISSN:  0753-3322     ISO Abbreviation:  Biomed. Pharmacother.     Publication Date:  2008 Feb 
Date Detail:
Created Date:  2008-02-15     Completed Date:  2008-06-02     Revised Date:  2009-11-19    
Medline Journal Info:
Nlm Unique ID:  8213295     Medline TA:  Biomed Pharmacother     Country:  France    
Other Details:
Languages:  eng     Pagination:  99-103     Citation Subset:  IM    
Laboratoire de Pharmacognosie et Chimiothérapie Antiparasitaire, UMR 8076 CNRS, Faculté de Pharmacie, Univ Paris-Sud, 92290 Châtenay-Malabry, France.
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MeSH Terms
Amphotericin B / 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
Reg. No./Substance:
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

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