Cajaninstilbene acid analogues as novel quorum sensing and biofilm inhibitors of Pseudomonas aeruginosa
Cajaninstilbene acid analogues as novel quorum sensing and biofilm inhibitors of Pseudomonas aeruginosa
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木豆芪酸类似物作为铜绿假单胞菌的新型群体感应和生物膜抑制剂
DOI：
10.1016/j.micpath.2020.104414
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发表时间：
2020-11-01
影响因子：
3.8
通讯作者：
Chen, Wei-Min
中科院分区：
文献类型：
--
作者：
Huang, Zhi-Xing;Yu, Jia-Hui;Chen, Wei-Min
条件致病菌铜绿假单胞菌的生物膜形成和毒力因子分泌是其慢性和反复感染的关键，受群体感应系统（quorum sensing，QS）的调控。本研究设计并合成了一系列木豆烯酸类似物，并考察了它们抑制QS和生物膜形成的能力。在所有化合物中，化合物3g、3 m和3 o显示出有效的生物膜抑制活性，特别是3 o显示出有希望的生物膜抑制活性，在50 μ M下生物膜抑制率为49.50 +/- 1.35%。构建了三种lacZ报告菌株以鉴定化合物3 o对不同QS系统的影响。化合物30显示对lasB-lacZ和pqsA-lacZ的表达以及对它们相应的毒力因子的产生的抑制。因此，预期化合物3 o作为具有生物膜形成抑制和铜绿假单胞菌QS的先导化合物产生。
Biofilm formation and virulence factor secretion in opportunistic pathogen Pseudomonas aeruginosa are essential for establishment of chronic and recurrent infection, which are regulated by quorum sensing (QS) system. In this study, a set of cajaninstilbene acid analogues were designed and synthesized, and their abilities to inhibit QS and biofilm formation were investigated. Among all the compounds, compounds 3g, 3m and 3o showed potent antibiofilm activity, especially 3o exhibited promising biofilm inhibitory activity with biofilm inhibition ratio of 49.50 +/- 1.35% at 50 mu M. Three lacZ reporter strains were constructed to identify the effects of compound 3o on different QS systems. Compound 3o showed the suppression on the expression of lasB-lacZ and pqsA-lacZ as well as on the production of their corresponding virulence factors. Therefore, compound 3o is expected to be generated as a lead compound with inhibition of biofilm formation and QS of Pseudomonas aeruginosa.