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通过先臂法获得的阳离子星形聚合物——阳离子单元的臂数和位置对抗菌活性的影响

Cationic Star Polymers Obtained by the Arm-First Approach─Influence of Arm Number and Positioning of Cationic Units on Antimicrobial Activity.

作者信息

Laroque Sophie, Locock Katherine E S, Perrier Sébastien

机构信息

Department of Chemistry, University of Warwick, Gibbet Hill Road, Coventry CV4 7AL, U.K.

CSIRO Manufacturing, Clayton, Victoria 3168, Australia.

出版信息

Biomacromolecules. 2025 Jan 13;26(1):190-200. doi: 10.1021/acs.biomac.4c00882. Epub 2024 Dec 2.

Abstract

Recently, we published a study demonstrating the promising structure-activity relationship of 4-arm star polymers toward bacterial cells and biofilms. The aim of this study was to increase the number of arms to determine if this could further enhance activity via the arm-first approach, which enables access to star structures with a higher number of arms. A library of amphiphilic diblock and miktoarm star polymers was successfully synthesized, and their biological properties were assessed. The increased number of arms failed to increase activity for the diblock stars, possibly due to shielding of the cationic units located at the core from binding to the membrane, which was slightly improved for the miktoarm structures. However, the efficient synthesis of these structures shown herein could be used to synthesize star polymers with a higher cationic ratio or longer arms, thereby circumventing the limitation of reduced interaction of cationic units with the membrane.

摘要

最近,我们发表了一项研究,证明了四臂星形聚合物对细菌细胞和生物膜具有良好的构效关系。本研究的目的是增加臂的数量,以确定这是否可以通过“先臂法”进一步增强活性,该方法能够获得具有更多臂的星形结构。成功合成了一系列两亲性二嵌段和多臂星形聚合物,并评估了它们的生物学特性。对于二嵌段星形聚合物,臂数量的增加未能提高活性,这可能是由于位于核心的阳离子单元与膜结合受到屏蔽,而对于多臂结构,这种情况略有改善。然而,本文所示这些结构的高效合成可用于合成具有更高阳离子比例或更长臂的星形聚合物,从而规避阳离子单元与膜相互作用降低的限制。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3c41/11733951/29150eb964f4/bm4c00882_0001.jpg

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