title: Chemosensitization of multidrug resistant Candida albicans by the oxathiolone fused chalcone derivatives.
abstract: Three structurally related oxathiolone fused chalcone derivatives appeared effective chemosensitizers, able to restore in part sensitivity to fluconazole of multidrug-resistant C. albicans strains. Compound 21 effectively chemosensitized cells resistant due to the overexpression of the MDR1 gene, compound 6 reduced resistance of cells overexpressing the ABC-type drug transporters CDR1/CDR2 and derivative 18 partially reversed fluconazole resistance mediated by both types of yeast drug efflux pumps. The observed effect of sensitization of resistant strains of Candida albicans to fluconazole activity in the presence of active compounds most likely resulted from inhibition of the pump-mediated efflux, as was revealed by the results of studies involving the fluorescent probes, Nile Red, Rhodamine 6G and diS-C3(3).
authors: Department of Pharmaceutical Technology and Biochemistry, Gdańsk University of Technology Gdańsk, Poland.
authors: Izabela
authors: I
authors: Ła̧cka
authors: Department of Organic Chemistry, Medical University of Gdańsk Gdańsk, Poland.
authors: Marek T
authors: MT
authors: Konieczny
authors: Department of Organic Chemistry, Medical University of Gdańsk Gdańsk, Poland.
authors: Anita
authors: A
authors: Bułakowska
authors: Faculty of Mathematics and Physics, Charles University in Prague Prague, Czech Republic.
authors: Marie
authors: M
authors: Kodedová
authors: Faculty of Mathematics and Physics, Charles University in Prague Prague, Czech Republic.
authors: Dana
authors: D
authors: Gašková
authors: Membrane Biology Laboratory, School of Life Sciences, Jawaharlal Nehru University New Delhi, India.
authors: Indresh K
authors: IK
authors: Maurya
authors: Membrane Biology Laboratory, School of Life Sciences, Jawaharlal Nehru University New Delhi, India.
authors: Rajendra
authors: R
authors: Prasad
authors: Department of Pharmaceutical Technology and Biochemistry, Gdańsk University of Technology Gdańsk, Poland.
authors: Sławomir
authors: S
authors: Milewski
keywords: Candida albicans; antifungals; chalcones; chemosensitization; multidrug resistance