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FEMS Yeast Res ; 20(1)2020 Feb 01.
Artigo em Inglês | MEDLINE | ID: mdl-31942998

RESUMO

One strategy for overcoming infectious diseases caused by drug-resistant fungi involves combining drugs rendered inactive by resistance with agents targeting the drug resistance mechanism. The antifungal activity of n-dodecanol disappears as incubation time passes. In Saccharomyces cerevisiae, anethole, a principal component of anise oil, prolongs the transient antifungal effect of dodecanol by downregulating genes of multidrug efflux pumps, mainly PDR5. However, the detailed mechanisms of dodecanol's antifungal action and the anethole-induced prolonged antifungal action of dodecanol are unknown. Screening of S. cerevisiae strains lacking genes related to Ca2+ homeostasis and signaling identified a pmr1Δ strain lacking Golgi Ca2+-ATPase as more sensitive to dodecanol than the parental strain. Dodecanol and the dodecanol + anethole combination significantly increased intracellular Ca2+ levels in both strains, but the mutant failed to clear intracellular Ca2+ accumulation. Further, dodecanol and the drug combination reduced PMR1 expression and did not lead to specific localization of Pmr1p in the parental strain after 4-h treatment. By contrast with the parental strain, dodecanol did not stimulate PDR5 expression in pmr1Δ. Based on these observations, we propose that the antifungal activity of dodecanol is related to intracellular Ca2+ accumulation, possibly dependent on PMR1 function, with anethole enabling Ca2+ accumulation by restricting dodecanol efflux.


Assuntos
Anisóis/farmacologia , ATPases Transportadoras de Cálcio/genética , Cálcio/metabolismo , Dodecanol/farmacologia , Deleção de Genes , Chaperonas Moleculares/genética , Proteínas de Saccharomyces cerevisiae/genética , Saccharomyces cerevisiae/efeitos dos fármacos , Derivados de Alilbenzenos , Anisóis/química , Antifúngicos/química , Antifúngicos/farmacologia , ATPases Transportadoras de Cálcio/efeitos dos fármacos , ATPases Transportadoras de Cálcio/metabolismo , Dodecanol/química , Sinergismo Farmacológico , Citometria de Fluxo , Complexo de Golgi/enzimologia , Chaperonas Moleculares/efeitos dos fármacos , Chaperonas Moleculares/metabolismo , RNA Fúngico/química , RNA Fúngico/isolamento & purificação , Reação em Cadeia da Polimerase em Tempo Real , Saccharomyces cerevisiae/genética , Saccharomyces cerevisiae/metabolismo , Proteínas de Saccharomyces cerevisiae/efeitos dos fármacos , Proteínas de Saccharomyces cerevisiae/metabolismo , Transdução de Sinais/genética
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