期刊
MOLECULES
卷 27, 期 8, 页码 -出版社
MDPI
DOI: 10.3390/molecules27082439
关键词
Pseudomonas aeruginosa; quorum sensing; las system; flavone derivative; inhibitor
资金
- National Natural Science Foundation of China [22077142, 22022706, 21837006, 91953117, 21877131]
- Natural Science Foundation of Guangdong Province, China [2019A1515011156]
Quorum sensing is a cell-to-cell communication process that controls bacterial collective behaviors. A phosphate ester derivative of chrysin has been identified as a potent quorum sensing inhibitor of the human pathogen Pseudomonas aeruginosa, with higher anti-virulence activity compared to the parent molecule.
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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