Institute of Functional Nano and Soft Materials (FUNSOM), Collaborative Innovation Center of Suzhou Nano Science and Technology, Soochow University, Suzhou 215123, China.
ACS Macro Lett. 2022 Mar 15;11(3):387-393. doi: 10.1021/acsmacrolett.2c00017. Epub 2022 Mar 1.
Surface modification with cationic polymer coatings represented an important strategy to address the medical device-related infection issues. However, limited antibacterial activities and high cytotoxicity have hampered their development. Herein, we report a facile method to enhance the surface antibacterial activity by construction of an imidazolium-based polypeptide with fosfomycin counteranions (i.e., S-PIL-FS). The polypeptide coating displayed a synergistic antibacterial effect from the combination of membrane disruption and inhibition of initial cell wall synthesis, leading to higher in vitro and in vivo surface antibacterial activities than cationic polypeptide or fosfomycin sodium alone. S-PIL-FS also showed a decrease in the hemolytic ratio and cytotoxicity toward different mammalian cells. Moreover, we observed an interesting biofilm-responsive property of S-PIL-FS originating from the esterase-induced cleavages of side-chain ester bonds that enabled an antibiofilm property of the cationic polypeptide coating.
通过阳离子聚合物涂层的表面改性来解决与医疗器械相关的感染问题是一种重要策略。然而，有限的抗菌活性和高细胞毒性阻碍了它们的发展。在此，我们报告了一种通过构建带有膦霉素抗衡阴离子的咪唑啉基多肽（即 S-PIL-FS）来提高表面抗菌活性的简便方法。该多肽涂层通过破坏细胞膜和抑制初始细胞壁合成的协同作用显示出协同抗菌作用，导致体外和体内表面抗菌活性高于阳离子多肽或磷霉素钠单独使用。S-PIL-FS 还显示出血红蛋白比率降低和对不同哺乳动物细胞的细胞毒性降低。此外，我们观察到 S-PIL-FS 的一个有趣的生物膜响应特性，源于侧链酯键的酯酶诱导裂解，使阳离子多肽涂层具有抗生物膜特性。
