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Reversal of fluconazole resistance by sulfated sterols from the marine sponge Topsentia sp.

ABSTRACT: Bioassay-guided fractionation of the extract of Topsentia sp. led to the identification of two new sulfated sterols, geodisterol-3-O-sulfite (1) and 29-demethylgeodisterol-3-O-sulfite (2), the active constituents reversing efflux pump-mediated fluconazole resistance. Both compounds enhanced the activity of fluconazole in a Saccharomyces cerevisiae strain overexpressing the Candida albicans efflux pump MDR1, as well as in a fluconazole-resistant Candida albicans clinical isolate known to overexpress MDR1. These results provide insight into the clinical utility of combining efflux pump inhibitors with current antifungals to combat the resistance associated with opportunistic fungal infections caused by C. albicans.

SUBMITTER: Digirolamo JA

PROVIDER: S-EPMC3697152 | biostudies-literature | 2009 Aug

REPOSITORIES: biostudies-literature

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Reversal of fluconazole resistance by sulfated sterols from the marine sponge Topsentia sp.

Digirolamo Jessica A JA Li Xing-Cong XC Jacob Melissa R MR Clark Alice M AM Ferreira Daneel D

Journal of natural products 20090801 8

Bioassay-guided fractionation of the extract of Topsentia sp. led to the identification of two new sulfated sterols, geodisterol-3-O-sulfite (1) and 29-demethylgeodisterol-3-O-sulfite (2), the active constituents reversing efflux pump-mediated fluconazole resistance. Both compounds enhanced the activity of fluconazole in a Saccharomyces cerevisiae strain overexpressing the Candida albicans efflux pump MDR1, as well as in a fluconazole-resistant Candida albicans clinical isolate known to overexpr ...[more]

PMID: 19653640

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