South China Sea Fisheries Research Institute, Chinese Academy of Fishery Sciences, Guangzhou 510300, PR China.
State Key Laboratory for Biocontrol, School of Life Sciences, Zhongshan (Sun Yat-sen) University, Guangzhou 510275, PR China.
J Med Microbiol. 2011 Dec;60(Pt 12):1827-1834. doi: 10.1099/jmm.0.024166-0. Epub 2011 Aug 18.
The objective of this study was to screen for novel quorum-sensing inhibitors (QSIs) from traditional Chinese medicines (TCMs) that inhibit bacterial biofilm formation. Six of 46 active components found in TCMs were identified as putative QSIs based on molecular docking studies. Of these, three compounds inhibited biofilm formation by Pseudomonas aeruginosa and Stenotrophomonas maltophilia at a concentration of 200 µM. A fourth compound (emodin) significantly inhibited biofilm formation at 20 µM and induced proteolysis of the quorum-sensing signal receptor TraR in Escherichia coli at a concentration of 3-30 mM. Emodin also increased the activity of ampicillin against P. aeruginosa. Therefore, emodin might be suitable for development into an antivirulence and antibacterial agent.
本研究旨在从中药中筛选抑制细菌生物膜形成的新型群体感应抑制剂（QSIs）。根据分子对接研究，从 46 种中药中的 6 种活性成分中鉴定出 6 种可能的 QSIs。其中，三种化合物在 200μM 浓度下抑制铜绿假单胞菌和嗜麦芽寡养单胞菌的生物膜形成。第四种化合物（大黄素）在 20μM 浓度下显著抑制生物膜形成，并在 3-30mM 浓度下诱导大肠杆菌中群体感应信号受体 TraR 的蛋白水解。大黄素还增加了氨苄西林对铜绿假单胞菌的活性。因此，大黄素可能适合开发为一种抗毒力和抗菌剂。
