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鲍曼不动杆菌生物膜抑制剂的设计合成及其活性测试

Design Synthesis and Evaluation of Biofilm Inhibitor Against Acinetobacter Baumannii
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摘要 国内外临床实践和研究结果均证明细菌的耐药性、慢性感染疾病难以治愈和反复发作都与细菌的生物膜密切相关。生物膜顽固的黏附性和致密性对游离细菌的保护,使得细菌对抗生素的耐药性增加10~1000倍。基于群体行为控制的生物膜抑制剂开发有望提供解决思路,为此合成出9个具有生物膜抑制作用的化合物,并测试其生物膜抑制活性。研究发现在20μmol的抑制剂条件下,其中8个化合物均显示鲍曼不动杆菌的生物膜抑制活性,其中2个化合物在20μmol条件下生物膜抑制率超过60%,并且通过扫描电镜观察研究细菌在硅胶片表面的生长情况,在添加化合物6的硅胶片表面并未形成生物膜群落,而在未添加化合物的硅胶片表面形成了生物膜群落,进一步说明了合成化合物对生物膜的抑制作用。 The clinical practice and research results have proved that the drug resistance and chronic infection of bacteria,the persistent and recurrently attack are closely related to bacterial biofilm The compactness and adhesion of biofilm provide protection for bacteria,biofilm can make bacteria resistance to antibiotics increased by10~1000folds.Development of biofilm inhibitors based on quorum sensing is expected to provide solutions Therefore,9compounds were synthesized and tested their inhibitory activity The results showed that at the concentration of20μmol,8of the synthesized compound showed biofilm inhibition activity and2of them can decrease60%of the biofilm at20μmol.Besides,the study of bacteria growth on silicon film surface by scanning electron microscopy was conducted,the silicon film surface did not form a biofilm community when cultured with compound6,and the formation of the biofilm community was observed on the silicon film surface without the addition of compounds,this result further illustrated the inhibitory effect of synthetic compounds.
作者 杨元勇 杨果 程铖 张林 汤磊 李春 周顺 Yang Yuanyong;Yang Guo;Cheng Cheng;Zhang Lin;Tang Lei;Li Chun;Zhou Shun(School of pharmacy, Guizhou Medical University1, Guiyang 550025,P R China;College of Chemistry and Molecular Sciences, Wuhan University2, Wuhan 430000,P R China)
出处 《科学技术与工程》 北大核心 2017年第33期1-5,共5页 Science Technology and Engineering
基金 国家自然科学基金(81660348) 贵州省科技厅联合基金([2015]7343) 贵阳市科技局基金([20151001]06) 贵州医科大学基金(院博合J字[2014]015) 贵州省普通高等学校药物化学工程研究中心(黔教合KY字[2014]219) 贵州省药物化学合成药物研发利用工程技术研究中心(黔科合[2016]平台人才5402)资助
关键词 鲍曼不动杆菌 生物膜抑制剂 群体感应 Acinetobacter baumannii biofilm inhibitor quorum sensing
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