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筛选和匹配两亲性阳离子聚合物以实现高效抗菌。

Screening and Matching Amphiphilic Cationic Polymers for Efficient Antibiosis.

机构信息

Department of Polymer Science and Technology, Key Laboratory of Systems Bioengineering of the Ministry of Education, School of Chemical Engineering and Technology, Tianjin University, Tianjin 300072, China.

Collaborative Innovation Center of Chemical Science and Engineering (Tianjin), Tianjin 300072, China.

出版信息

Biomacromolecules. 2020 Dec 14;21(12):5269-5281. doi: 10.1021/acs.biomac.0c01330. Epub 2020 Nov 23.

Abstract

The amphiphilic cationic polymers that mimic antimicrobial peptides have received increasing attention due to their excellent antibacterial activity. However, the relationship between the structure of cationic polymers and its antibacterial effect remains unclear. In our current work, a series of PEG blocked amphiphilic cationic polymers composed of hydrophobic alkyl-modified and quaternary ammonium salt (QAS) moieties have been prepared. The structure-antibacterial activity relationship of these cationic polymers was investigated against and , including PEGylation, random structure, molecular weights, and the content and lengths of the hydrophobic alkyl side chains. The results indicated that PEGylated random amphiphilic cationic copolymer (mPB/T) showed stronger antibacterial activity and better biocompatibility than the random copolymer without PEG (PB/T). Furthermore, mPB/T with appropriate mole fraction of alkyl side chains ( = 0.38), degree of polymerization (DP = 92), and four-carbon hydrophobic alkyl moieties was found to have the optimal structure that revealed the best antibacterial activities against both (MIC = 8 μg/mL, selectivity > 250) and (MIC = 4 μg/mL, selectivity > 500). More importantly, mPB/T could effectively eradicate biofilms by killing the bacteria embedded in the biofilms. Therefore, the structure of mPB/T provided valuable information for improving the antibacterial activity of cationic polymers.

摘要

由于具有优异的抗菌活性,模拟抗菌肽的两亲性阳离子聚合物受到了越来越多的关注。然而,阳离子聚合物的结构与其抗菌效果之间的关系尚不清楚。在我们目前的工作中,制备了一系列由疏水烷基修饰和季铵盐(QAS)部分组成的 PEG 封端的两亲性阳离子聚合物。研究了这些阳离子聚合物的结构-抗菌活性关系,包括 PEG 化、无规结构、分子量以及疏水烷基侧链的含量和长度对 和 的影响。结果表明,与没有 PEG 的无规共聚物(PB/T)相比,PEG 化的无规两亲性阳离子共聚物(mPB/T)具有更强的抗菌活性和更好的生物相容性。此外,发现具有适当烷基侧链摩尔分数( = 0.38)、聚合度(DP = 92)和四个碳疏水烷基部分的 mPB/T 具有最佳结构,对 和 均表现出最佳的抗菌活性(MIC = 8 μg/mL,选择性 > 250)和 (MIC = 4 μg/mL,选择性 > 500)。更重要的是,mPB/T 可以通过杀死嵌入生物膜中的细菌来有效清除 生物膜。因此,mPB/T 的结构为提高阳离子聚合物的抗菌活性提供了有价值的信息。

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