National Engineering Research Center for Healthcare Devices, Guangdong Institute of Medical Instruments, Guangzhou 510632, PR China; Biomedical Engineering Institute, Jinan University, Guangzhou 510632, PR China.
Department of Pharmacology, Utrecht Institute for Pharmaceutical Sciences, Utrecht University, 3568 CG Utrecht, the Netherlands.
Int J Biol Macromol. 2021 Jan 15;167:66-75. doi: 10.1016/j.ijbiomac.2020.11.143. Epub 2020 Nov 23.
Bacterial adhesion infection caused by medical materials in clinical application has become a serious threat, and it urgently needs new strategies to deal with these clinical challenges. The purpose of this study is to explore the effectiveness of surface-decorated aryl (β-amino) ethyl ketones (AAEK), a promising sorting enzyme A (SrtA) inhibitor of Staphylococcus aureus, to improve the anti-adhesion ability of biomaterials. AAEK was covalently grafted onto cellulose films (CF) via copper-catalyzed azide-alkyne 1, 3-dipolar cycloaddition click reaction. The data of contact angle measurements, ATR-FTIR and XPS proved the successful covalent attachment of AAEK-CF, and the antimicrobial efficacy of AAEK coating was assessed by CFUs, crystal violet staining, scanning electron microscopy and Living/Dead bacteria staining assay. The results illustrated that AAEK-CF exhibited excellent anti-adhesion ability to Staphylococcus aureus, and significantly reduced the number of bacteria adhering to the film. More importantly, AAEK-CF could hinder the formation of bacterial biofilm. Furthermore, AAEK-CF indicated no cytotoxicity to mammalian cells, and the cells could grow normally on the modified surface. Hence, our present work demonstrated that the grafting of the SrtA inhibitor-AAEK onto cellulose films enabled to combat bacterial biofilm formation in biomedical applications.
在临床应用中，医用材料引起的细菌黏附感染已成为严重威胁，因此急需新的策略来应对这些临床挑战。本研究旨在探索芳基（β-氨基）乙基酮（AAEK）表面修饰的效果，AAEK 是一种有前途的金黄色葡萄球菌分选酶 A（SrtA）抑制剂，可提高生物材料的抗黏附能力。通过铜催化的叠氮-炔基 1,3-偶极环加成点击反应，将 AAEK 共价接枝到纤维素膜（CF）上。接触角测量、ATR-FTIR 和 XPS 数据证明了 AAEK-CF 的成功共价结合，通过 CFU、结晶紫染色、扫描电子显微镜和活/死细菌染色实验评估了 AAEK 涂层的抗菌功效。结果表明，AAEK-CF 对金黄色葡萄球菌表现出优异的抗黏附能力，显著减少了黏附在薄膜上的细菌数量。更重要的是，AAEK-CF 可以阻止细菌生物膜的形成。此外，AAEK-CF 对哺乳动物细胞无细胞毒性，细胞可以在修饰后的表面上正常生长。因此，本研究表明，将 SrtA 抑制剂-AAEK 接枝到纤维素膜上，可以在生物医学应用中对抗细菌生物膜的形成。
