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SINGH, B. UPRETI, D. SINGH, B. PANDEY, G. VERMA, S. ROY, S. NAQVI, A. RAWAT, A.
Original Title
Quercetin Sensitizes Fluconazole-Resistant Candida albicans To Induce Apoptotic Cell Death by Modulating Quorum Sensing
Type
journal article in Web of Science
Language
English
Original Abstract
Quorum sensing (QS) regulates group behaviors of Candida albicans such as biofilm, hyphal growth, and virulence factors. The sesquiterpene alcohol farnesol, a QS molecule produced by C. albicans, is known to regulate the expression of virulence weapons of this fungus. Fluconazole (FCZ) is a broad-spectrum antifungal drug that is used for the treatment of C. albicans infections. While FCZ can be cytotoxic at high concentrations, our results show that at much lower concentrations, quercetin (QC), a dietary flavonoid isolated from an edible lichen (Usnealongissima), can be implemented as a sensitizing agent for FCZ-resistant C. albicans NBC099, enhancing the efficacy of FCZ. QC enhanced FCZ-mediated cell killing of NBC099 and also induced cell death. These experiments indicated that the combined application of both drugs was FCZ dose dependent rather than QC dose dependent. In addition, we found that QC strongly suppressed the production of virulence weapons-biofilm formation, hyphal development, phospholipase, proteinase, esterase, and hemolytic activity. Treatment with QC also increased FCZ-mediated cell death in NBC099 biofilms. Interestingly, we also found that QC enhances the anticandidal activity of FCZ by inducing apoptotic cell death. We have also established that this sensitization is reliant on the farnesol response generated by QC. Molecular docking studies also support this conclusion and suggest that QC can form hydrogen bonds with Gln969, Thr1105, Ser1108, Arg1109, Asn1110, and Gly1061 in the ATP binding pocket of adenylate cyclase. Thus, this QS-mediated combined sensitizer (QC)-anticandidal agent (FCZ) strategy may be a novel way to enhance the efficacy of FCZ-based therapy of C. albicans infections.
Keywords
Quercetin; Fluconazole; Sensitization; Candida albicans; Cell death; Quorum sensing
Authors
SINGH, B.; UPRETI, D.; SINGH, B.; PANDEY, G.; VERMA, S.; ROY, S.; NAQVI, A.; RAWAT, A.
RIV year
2015
Released
1. 3. 2015
Publisher
ASM
Location
US
ISBN
0066-4804
Periodical
ANTIMICROBIAL AGENTS AND CHEMOTHERAPY
Year of study
59
Number
4
State
United States of America
Pages from
599
Pages to
614
Pages count
15
BibTex
@article{BUT115005, author="B.N. {Singh} and D.K. {Upreti} and B.R. {Singh} and G. {Pandey} and S. {Verma} and Sudeep {Roy} and A.H. {Naqvi} and A.K.S. {Rawat}", title="Quercetin Sensitizes Fluconazole-Resistant Candida albicans To Induce Apoptotic Cell Death by Modulating Quorum Sensing", journal="ANTIMICROBIAL AGENTS AND CHEMOTHERAPY", year="2015", volume="59", number="4", pages="599--614", doi="10.1128/AAC.03599-14", issn="0066-4804" }