Liu Yue, Li Jun-Jian, Li Hong-Yuan, Deng Shi-Ming, Jia Ai-Qun
School of Pharmaceutical Sciences, Key Laboratory of Ministry of Education for Advanced Materials in Tropical Island Resources, Hainan University, Haikou, 570228, China.
Synth Syst Biotechnol. 2021 Nov 1;6(4):360-368. doi: 10.1016/j.synbio.2021.09.010. eCollection 2021 Dec.
Quorum sensing (QS) plays an essential role in virulence factor production, biofilm formation, and antimicrobial resistance. As a potent QS inhibitor, hordenine can inhibit both QS and biofilm formation in and . In this work, we tested the QS inhibitory potential of 27 hordenine analogs against QS and biofilm formation in and Among the tested analogs, seven (12, 28, 27, 26, 2, 23, and 7) exhibited strong QS inhibitory activity against , five of which (12, 28, 27, 26, and 2) showed better inhibitory activity than hordenine. In addition, seven analogs (28, 12, 23, 7, 26, 2, and 27) exhibited better biofilm inhibition against than hordenine. Four analogs (7, 28, 2, and 12) showed QS inhibitory activity against , two of which (7 and 28) demonstrated better inhibitory activity than hordenine. Furthermore, analog 7 showed similar biofilm inhibition against as hordenine. Structure-activity relationship (SAR) analysis indicated that the inhibitory activities of the analogs were related to four factors, i.e., carbon chain length, presence or absence of an α,β-C[bond, double bond]C bond, amino group with/without lipophilic group, such as methyl group, and hydroxyl group in benzene ring.
群体感应（QS）在毒力因子产生、生物膜形成和抗菌耐药性中起着至关重要的作用。作为一种有效的群体感应抑制剂，去甲乌药碱可以抑制铜绿假单胞菌和金黄色葡萄球菌中的群体感应及生物膜形成。在本研究中，我们测试了27种去甲乌药碱类似物对铜绿假单胞菌和金黄色葡萄球菌群体感应及生物膜形成的抑制潜力。在所测试的类似物中，七种（12、28、27、26、2、23和7）对铜绿假单胞菌表现出较强的群体感应抑制活性，其中五种（12、28、27、26和2）显示出比去甲乌药碱更好的抑制活性。此外，七种类似物（28、12、23、7、26、2和27）对金黄色葡萄球菌的生物膜抑制作用比去甲乌药碱更好。四种类似物（7、28、2和12）对金黄色葡萄球菌表现出群体感应抑制活性，其中两种（7和28）的抑制活性比去甲乌药碱更好。此外，类似物7对金黄色葡萄球菌的生物膜抑制作用与去甲乌药碱相似。构效关系（SAR）分析表明，类似物的抑制活性与四个因素有关，即碳链长度、α,β-C=C键的有无、带有/不带有亲脂性基团（如甲基）的氨基以及苯环上的羟基。
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