灰毡毛忍冬抑制CRPA群体感应系统的活性成分筛选研究  

Study on screening of active components from Lonicera macranthoides to inhibit carbapenem-resistant Pseudomonas aeruginosa quorum sensing system

作　　者：唐霄 浦智婷 尹铁球 Tang Xiao;Pu Zhiting;Yin Tieqiu(Guilin Medical College,School of Laboratory Medicine,Guilin 541004)

机构地区：[1]桂林医学院医学检验学院,桂林541004

出　　处：《中国抗生素杂志》2024年第12期1321-1328,共8页Chinese Journal of Antibiotics

基　　金：广西科技基地和人才专项(No.AD22035034);基于产教融合的医学检验技术研究生联合培养模式研究(No.JGY2022203)。

摘　　要：目的通过筛选灰毡毛忍冬抑制碳青霉烯类耐药铜绿假单胞菌群体感应系统的主要活性成分,并研究其抑制作用。方法通过Discovery Studio的两种对接模块模拟分子间作用虚拟筛选抑菌成分,分析其结合模式,并检测其对碳青霉烯类耐药铜绿假单胞菌生长活性、生物膜的抑制作用,构建秀丽隐杆线虫感染模型,评估药物治疗效果。结果3种小分子均能不同程度抑制碳青霉烯类铜绿假单胞菌生长及生物膜形成,且显著提高线虫感染后存活率。结论3种灰毡毛忍冬小分子药物对碳青霉烯类铜绿假单胞菌的生长具有显著抑制作用,有望成为新型作用于QS系统的CRPA抑制剂。Objective To screen and identify the major active components of Lonicera macranthoides that inhibit the quorum sensing(QS)system of carbapenem-resistant Pseudomonas aeruginosa and investigate the inhibitory effects of these components.Methods Virtual screening of antibacterial components was conducted using two docking modules in Discovery Studio to simulate molecular interactions and analyze their binding modes.The inhibitory effects of the screened components on the growth activity and biofilm formation of carbapenem-resistant Pseudomonas aeruginosa were determined.A Caenorhabditis elegans infection model was established to evaluate the therapeutic effects of the drugs.Results All three small molecules exhibited varying degrees of growth inhibition and biofilm formation reduction in carbapenem-resistant Pseudomonas aeruginosa.Furthermore,all three small-molecule drugs significantly improved the survival rate of Caenorhabditis elegans after infection.Conclusion The three small molecule drugs derived from Lonicera macranthoides demonstrated significant inhibitory effects on the growth of carbapenem-resistant Pseudomonas aeruginosa,highlighting their potential as novel CRPA inhibitors targeting the QS system.

关 键 词：灰毡毛忍冬 碳青霉烯类耐药铜绿假单胞菌 群体感应系统 分子对接 

分 类 号：R978.1[医药卫生—药品]