Inhibition of Quorum-Sensing Regulator from <i>Pseudomonas aeruginosa</i> Using a Flavone Derivative
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 su...
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| Format: | Article |
| Language: | English |
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MDPI AG
2022-04-01
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| Series: | Molecules |
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| Online Access: | https://www.mdpi.com/1420-3049/27/8/2439 |
| _version_ | 1797409923540189184 |
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| author | Yanxuan Xie Jingxin Chen Bo Wang Ai-Yun Peng Zong-Wan Mao Wei Xia |
| author_facet | Yanxuan Xie Jingxin Chen Bo Wang Ai-Yun Peng Zong-Wan Mao Wei Xia |
| author_sort | Yanxuan Xie |
| collection | DOAJ |
| description | 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 <i>Pseudomonas aeruginosa</i> (<i>P. aeruginosa</i>) 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 <i>P. aeruginosa</i>. |
| first_indexed | 2024-03-09T04:22:31Z |
| format | Article |
| id | doaj.art-ff563e2d0a404efea68f345e8ea3be3c |
| institution | Directory Open Access Journal |
| issn | 1420-3049 |
| language | English |
| last_indexed | 2024-03-09T04:22:31Z |
| publishDate | 2022-04-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Molecules |
| spelling | doaj.art-ff563e2d0a404efea68f345e8ea3be3c2023-12-03T13:46:10ZengMDPI AGMolecules1420-30492022-04-01278243910.3390/molecules27082439Inhibition of Quorum-Sensing Regulator from <i>Pseudomonas aeruginosa</i> Using a Flavone DerivativeYanxuan Xie0Jingxin Chen1Bo Wang2Ai-Yun Peng3Zong-Wan Mao4Wei Xia5School of Chemistry, Sun Yat-Sen University, Guangzhou 510275, ChinaSchool of Chemistry, Sun Yat-Sen University, Guangzhou 510275, ChinaSchool of Chemistry, Sun Yat-Sen University, Guangzhou 510275, ChinaSchool of Chemistry, Sun Yat-Sen University, Guangzhou 510275, ChinaSchool of Chemistry, Sun Yat-Sen University, Guangzhou 510275, ChinaSchool of Chemistry, Sun Yat-Sen University, Guangzhou 510275, ChinaQuorum 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 <i>Pseudomonas aeruginosa</i> (<i>P. aeruginosa</i>) 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 <i>P. aeruginosa</i>.https://www.mdpi.com/1420-3049/27/8/2439<i>Pseudomonas aeruginosa</i>quorum sensing<i>las</i> systemflavone derivativeinhibitor |
| spellingShingle | Yanxuan Xie Jingxin Chen Bo Wang Ai-Yun Peng Zong-Wan Mao Wei Xia Inhibition of Quorum-Sensing Regulator from <i>Pseudomonas aeruginosa</i> Using a Flavone Derivative Molecules <i>Pseudomonas aeruginosa</i> quorum sensing <i>las</i> system flavone derivative inhibitor |
| title | Inhibition of Quorum-Sensing Regulator from <i>Pseudomonas aeruginosa</i> Using a Flavone Derivative |
| title_full | Inhibition of Quorum-Sensing Regulator from <i>Pseudomonas aeruginosa</i> Using a Flavone Derivative |
| title_fullStr | Inhibition of Quorum-Sensing Regulator from <i>Pseudomonas aeruginosa</i> Using a Flavone Derivative |
| title_full_unstemmed | Inhibition of Quorum-Sensing Regulator from <i>Pseudomonas aeruginosa</i> Using a Flavone Derivative |
| title_short | Inhibition of Quorum-Sensing Regulator from <i>Pseudomonas aeruginosa</i> Using a Flavone Derivative |
| title_sort | inhibition of quorum sensing regulator from i pseudomonas aeruginosa i using a flavone derivative |
| topic | <i>Pseudomonas aeruginosa</i> quorum sensing <i>las</i> system flavone derivative inhibitor |
| url | https://www.mdpi.com/1420-3049/27/8/2439 |
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