State Key Laboratory of Polymer Physics and Chemistry, Changchun Institute of Applied Chemistry, Chinese Academy of Sciences, Changchun 130022, P. R. China.
University of Science and Technology of China, Hefei 230026, P. R. China.
Biomater Sci. 2022 Feb 1;10(3):834-845. doi: 10.1039/d1bm01620b.
Antimicrobial peptides (AMPs) are attractive antimicrobial agents used to combat bacterial infections, and have been advanced to be one of the most promising alternatives to conventional antibiotics. They stand out for their attractive broad-spectrum activity, unmatched antibacterial mechanism that is not prone to develop drug resistance and diversified topologies, which can be fabricated with manifold amino acid blocks. In this study, using -hexylamine and amine-terminated polyamidoamine dendrimers (G-PAMAM, = 1-2) as initiators, a series of AMPs with linear and star-shaped topological structures were constructed the controllable ring-opening polymerization (ROP) of -carboxyanhydrides (NCAs). The antibacterial performances of the tailored linear and star-shaped AMPs were comprehensively evaluated in both solution states and surface-bonded states. The results indicated that the star-shaped AMPs exhibited enhanced bactericidal activity against Gram-negative and similar bactericidal activity against Gram-positive when compared with the linear AMPs. It is worth mentioning that star-shaped AMPs demonstrated a significantly faster bactericidal efficiency (completely killed bacteria within 5 min at a concentration of 2 × MIC for ) than their linear analogues (took 15 min to achieve the same effect). However, when the AMPs were immobilized to the surface, they similarly exhibited superior antibacterial activity and fast bactericidal efficiency towards and in the case of the same surface grafting amount. In addition, both the surfaces grafted with AMPs of different topologies demonstrated favorable biocompatibility .
抗菌肽（AMPs）是一种有吸引力的抗菌剂，用于对抗细菌感染，被认为是传统抗生素最有前途的替代品之一。它们具有广谱活性、独特的抗菌机制（不易产生耐药性）和多样化的拓扑结构的特点，这些拓扑结构可以用多种氨基酸块来构建。在这项研究中，我们使用 - 己胺和胺端聚酰胺胺树枝状大分子（G-PAMAM， = 1-2）作为引发剂，通过可控开环聚合（ROP） - 羧酸酐（NCAs）构建了一系列具有线性和星形拓扑结构的 AMPs。我们综合评估了定制的线性和星形 AMPs 在溶液状态和表面结合状态下的抗菌性能。结果表明，与线性 AMPs 相比，星形 AMPs 对革兰氏阴性菌表现出增强的杀菌活性，对革兰氏阳性菌表现出相似的杀菌活性。值得注意的是，星形 AMPs 表现出明显更快的杀菌效率（在浓度为 2×MIC 时，在 5 分钟内完全杀死细菌），而其线性类似物则需要 15 分钟才能达到相同的效果。然而，当 AMPs 固定到表面时，同样的，在相同的表面接枝量下，它们对 和 也表现出优异的抗菌活性和快速的杀菌效率。此外，具有不同拓扑结构的 AMPs 接枝的表面都表现出良好的生物相容性。
