Yu Jingyi, Rao Lulin, Zhan Lingling, Zhou Yan, Guo Yinjuan, Wu Xiaocui, Song Zengqiang, Yu Fangyou
Department of Laboratory Medicine, The First Affiliated Hospital of Wenzhou Medical University, Wenzhou, China.
School of Pharmaceutical Sciences, Wenzhou Medical University, Wenzhou, China.
Front Microbiol. 2021 Feb 3;12:618922. doi: 10.3389/fmicb.2021.618922. eCollection 2021.
is the most important pathogenic bacteria in humans. As the resistance of to existing antibiotics is increasing, there is an urgent need for new anti-infective drugs. biofilms cause persistent infections and resist complete eradication with antibiotic therapy. The present study investigated the inhibitory effect of the novel small-molecule ZY-214-4 (C H BrNO) on biofilm formation. At a subinhibitory concentration (4 μg/ml), ZY-214-4 had no effect on the growth of strains and also showed no cytotoxicity in human normal bronchial epithelial cells (Bease-2B). The results of a semi-quantitative biofilm test showed that ZY-214-4 prevented biofilm formation, which was confirmed by scanning electron microscopy and confocal laser scanning microscopy. ZY-214-4 significantly suppressed the production of polysaccharide intercellular adhesion and prevented cell aggregation, and also inhibited the mRNA expression of and other biofilm-related genes (, , , , , α, and β) in clinical isolates. Thus, at a subinhibitory concentration, ZY-214-4 inhibits biofilm formation by preventing cell aggregation, highlighting its clinical potential for preventing or treating infections.
是人类最重要的病原菌。随着其对现有抗生素的耐药性不断增加,迫切需要新型抗感染药物。生物膜会导致持续性感染,且抗生素治疗难以将其完全根除。本研究调查了新型小分子ZY-214-4(C₁₈H₁₉BrNO)对生物膜形成的抑制作用。在亚抑菌浓度(4μg/ml)下,ZY-214-4对菌株生长无影响,且在人正常支气管上皮细胞(Beas-2B)中也未显示出细胞毒性。半定量生物膜试验结果表明,ZY-214-4可阻止生物膜形成,扫描电子显微镜和共聚焦激光扫描显微镜证实了这一点。ZY-214-4显著抑制细胞间多糖黏附的产生并阻止细胞聚集,还抑制临床分离株中及其他生物膜相关基因(、、、、、α和β)的mRNA表达。因此,在亚抑菌浓度下,ZY-214-4通过阻止细胞聚集来抑制生物膜形成,凸显了其在预防或治疗感染方面的临床潜力。