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含交替序列主链季𬭸聚合物的广谱杀菌活性和显著选择性。

Broad-Spectrum Bactericidal Activity and Remarkable Selectivity of Main-Chain Sulfonium-Containing Polymers with Alternating Sequences.

机构信息

Hubei Key Laboratory of Material Chemistry and Service Failure, Hubei Engineering Research Center for Biomaterials and Medical Protective Materials, School of Chemistry and Chemical Engineering, Huazhong University of Science and Technology, Wuhan, Hubei 430074, People's Republic of China.

School of Materials and Chemical Engineering, Anhui Jianzhu University, Hefei, Anhui 230601, People's Republic of China.

出版信息

ACS Macro Lett. 2021 Aug 17;10(8):990-995. doi: 10.1021/acsmacrolett.1c00340. Epub 2021 Jul 15.

Abstract

Incorporation of cationic groups into polymers represents one of the most widely used strategies to prepare antibacterial materials. Sulfonium, as a typical cationic moiety, displays potent antibacterial efficacy in the form of small molecules, however, has long underperformed in polymeric systems. Herein, we developed a series of alternating polysulfoniums, where the hydrophobicity of each alternating unit can be accurately tuned by altering the monomer precursors. Excellent antibacterial activity against a broad spectrum of clinically relevant bacteria, including Methicillin-resistant , can be obtained in the optimal compositions with minimum bactericidal concentrations in the range of 1.25-10 μg/mL, as well as negligible hemolytic effect at polymer concentrations even up to 10000 μg/mL. Bacteria do not readily develop resistance to polysulfoniums due to the antibacterial action is possibly the membrane disrupting mechanism. This work demonstrates sulfonium-based polymers with well-defined sequences can function as a promising candidate to combat drug-resistant bacterial infection.

摘要

将阳离子基团引入聚合物是制备抗菌材料最广泛使用的策略之一。锍盐作为一种典型的阳离子部分,以小分子的形式表现出很强的抗菌效果,但在聚合物体系中的性能一直不佳。在此,我们开发了一系列交替的聚锍盐,其中每个交替单元的疏水性可以通过改变单体前体来精确调整。在最佳组成中,可以获得对广泛的临床相关细菌(包括耐甲氧西林的细菌)的优异抗菌活性,最小杀菌浓度范围为 1.25-10μg/mL,即使聚合物浓度高达 10000μg/mL,溶血作用也可以忽略不计。由于抗菌作用可能是膜破坏机制,因此细菌不易对聚锍盐产生耐药性。这项工作表明,具有明确序列的基于锍盐的聚合物可以作为对抗耐药性细菌感染的有前途的候选物。

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