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 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 anti-biofilm activity, especially 3o exhibited promising biofilm inhibitory activity with biofilm inhibition ratio of 49.50 ± 1.35% at 50 μM. 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.

机会病原体铜绿假单胞菌中生物膜的形成和毒力因子的分泌对于建立慢性和复发性感染至关重要，这由群体感应系统调节。在这项研究中，设计和合成了一组卡南斯汀二苯甲酸类似物，并研究了它们抑制QS和生物膜形成的能力。在所有化合物中，化合物3g，3m和3o显示出有效的抗生物膜活性，尤其是3o在50μM时显示出有前途的生物膜抑制活性，生物膜抑制比为49.50±1.35％。构建了三种lacZ报告基因菌株以鉴定化合物3o的作用在不同的QS系统上。化合物3o对lasB-lacZ和pqsA-lacZ的表达以及相应毒力因子的产生均具有抑制作用。因此，预期产生化合物3o作为先导化合物，其抑制铜绿假单胞菌的生物膜形成和QS 。