In vitro and in vivo effects of the antimycotic drug ketoconazole on sterol synthesis
Author(s) -
H. Van den Bossche,
G. Willemsens,
W Cools,
Frans W. Cornelissen,
W. Lauwers,
J.M. Van Cutsem
Publication year - 1980
Publication title -
antimicrobial agents and chemotherapy
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 2.07
H-Index - 259
eISSN - 1070-6283
pISSN - 0066-4804
DOI - 10.1128/aac.17.6.922
Subject(s) - ketoconazole , lanosterol , ergosterol , in vivo , candida albicans , sterol , mycelium , in vitro , pharmacology , drug , corpus albicans , biology , microbiology and biotechnology , chemistry , biochemistry , cholesterol , antifungal , botany
Ketoconazole, an orally active antimycotic drug, is a potent inhibitor of ergosterol biosynthesis in Candida albicans when added to culture media which support yeast or mycelial growth or to cultures containing outgrown mycelium. This inhibition coincides with accumulation of sterols with a methyl group at C-14 and can thus be attributed to an interference with one of the reactions involved in the removal of the 14 alpha-methyl group of lanosterol. When administered to rats infected with C. albicans, ketocanazole also inhibits fungal synthesis of ergosterol. A six-times-higher dose is required to effect cholesterol synthesis by rat liver.
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