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用于治疗生物膜的适配体-氨苄青霉素偶联物的研发。

Development of an aptamer-ampicillin conjugate for treating biofilms.

作者信息

Lijuan Cheng, Xing Yan, Minxi Wu, Wenkai Li, Le Deng

机构信息

Department of Microbiology, College of Life Science, Hunan Normal University, Changsha, Hunan, 410081, China; Department of Biochemistry and Molecular Biology, Hunan University of Chinese Medicine, Changsha, Hunan, 410208, China.

Department of Microbiology, College of Life Science, Hunan Normal University, Changsha, Hunan, 410081, China.

出版信息

Biochem Biophys Res Commun. 2017 Feb 5;483(2):847-854. doi: 10.1016/j.bbrc.2017.01.016. Epub 2017 Jan 6.

Abstract

Biofilm formation involves the development of extracellular matrix and initially depends on adherence and tropism by flagellar movement. With the widespread development of antibiotic resistance and tolerance of biofilms, there is a growing need for novel anti-infective strategies. No currently approved medications specifically target biofilms. Aptamers are single-stranded nucleic acid molecules that may bind to their targets with high affinity and affect the target functions. We developed a bifunctional conjugate by linking an aptamer targeting bacterial flagella with ampicillin. We investigated its influence on biofilm prevention and dissolution by ultraviolet-visible spectrophotometry, inverted microscopy, and atomic force microscopy. This conjugate had distinctive antibacterial activity. Notably, the conjugate was more active than either component, and thus had a synergistic effect against biofilms.

摘要

生物膜形成涉及细胞外基质的发展,最初依赖于通过鞭毛运动的黏附和趋向性。随着抗生素耐药性和生物膜耐受性的广泛发展,对新型抗感染策略的需求日益增加。目前尚无获批专门针对生物膜的药物。适体是单链核酸分子,可与其靶标高亲和力结合并影响靶标功能。我们通过将靶向细菌鞭毛的适体与氨苄西林连接,开发了一种双功能缀合物。我们通过紫外可见分光光度法、倒置显微镜和原子力显微镜研究了其对生物膜预防和溶解的影响。这种缀合物具有独特的抗菌活性。值得注意的是,该缀合物比任何一种组分都更具活性,因此对生物膜具有协同作用。

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