作者: Izabela Ła̧cka , Marek T. Konieczny , Anita Bułakowska , Marie Kodedová , Dana Gašková
关键词: Efflux 、 Multiple drug resistance 、 Chemosensitization 、 Candida albicans 、 Molecular biology 、 Corpus albicans 、 Biology 、 Chalcone 、 Fluconazole 、 Pharmacology 、 Nile red
摘要: Three structurally related oxathiolone fused chalcone derivatives appeared effective chemosensitizers, able to restore in part sensitivity fluconazole of multidrug-resistant C. albicans strains. Compound 21 effectively chemosensitized cells resistant due the overexpression MDR1 gene, compound 6 reduced resistance overexpressing ABC-type drug transporters CDR1/CDR2 and derivative 18 partially reversed mediated by both types yeast efflux pumps. The observed effect sensitization strains Candida activity presence active compounds most likely resulted from inhibition pump-mediated efflux, as was revealed results studies involving fluorescent probes, Nile Red, Rhodamine 6G diS-C3(3).