AUTHOR=Łącka Izabela , Konieczny Marek T., Bułakowska Anita , Kodedova Marie , Gaskova Dana , Maurya Indresh K., Prasad Rajendra , Milewski Slawomir 

TITLE=Chemosensitization of multidrug resistant Candida albicans by the oxathiolone fused chalcone derivatives

JOURNAL=Frontiers in Microbiology

VOLUME=6

YEAR=2015

URL=https://www.frontiersin.org/journals/microbiology/articles/10.3389/fmicb.2015.00783

DOI=10.3389/fmicb.2015.00783

ISSN=1664-302X

ABSTRACT=<p>Three structurally related oxathiolone fused chalcone derivatives appeared effective chemosensitizers, able to restore in part sensitivity to fluconazole of multidrug-resistant <italic>C. albicans</italic> strains. Compound <bold>21</bold> effectively chemosensitized cells resistant due to the overexpression of the <italic>MDR1</italic> gene, compound <bold>6</bold> reduced resistance of cells overexpressing the ABC-type drug transporters <italic>CDR1/CDR2</italic> and derivative <bold>18</bold> partially reversed fluconazole resistance mediated by both types of yeast drug efflux pumps. The observed effect of sensitization of resistant strains of <italic>Candida albicans</italic> 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-C<sub>3</sub>(3).</p>