Inhibition of Quorum-Sensing Regulator from Pseudomonas aeruginosa Using a Flavone Derivative |
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| Authors: | Yanxuan Xie Jingxin Chen Bo Wang Ai-Yun Peng Zong-Wan Mao Wei Xia |
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| Institution: | 1.School of Chemistry, Sun Yat-Sen University, Guangzhou 510275, China; (Y.X.); (J.C.); (B.W.); (A.-Y.P.);2.MOE Key Laboratory of Bioinorganic and Synthetic Chemistry, Sun Yat-Sen University, Guangzhou 510275, China |
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| Abstract: | Quorum sensing (QS) is a cell-to-cell communication process that controls bacterial collective behaviors. The QS network regulates and coordinates bacterial virulence factor expression, antibiotic resistance and biofilm formation. Therefore, inhibition of the QS system is an effective strategy to suppress the bacterial virulence. Herein, we identify a phosphate ester derivative of chrysin as a potent QS inhibitor of the human pathogen Pseudomonas aeruginosa (P. aeruginosa) using a designed luciferase reporter assay. In vitro biochemical analysis shows that the chrysin derivative binds to the bacterial QS regulator LasR and abrogates its DNA-binding capability. In particular, the derivative exhibits higher anti-virulence activity compared to the parent molecule. All the results reveal the potential application of flavone derivative as an anti-virulence compound to combat the infectious diseases caused by P. aeruginosa. |
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| Keywords: | Pseudomonas aeruginosa quorum sensing las system flavone derivative inhibitor |
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