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Broad-Spectrum Bactericidal Activity and Remarkable Selectivity of Main-Chain Sulfonium-Containing Polymers with Alternating Sequences
ACS Macro Letters ( IF 5.8 ) Pub Date : 2021-07-15 , DOI: 10.1021/acsmacrolett.1c00340
Yongjin Hu 1, 2 , Jinghua Zhao 1 , Jingyan Zhang 2 , Zhiyuan Zhu 3 , Jingyi Rao 1
Affiliation  

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 Staphylococcus aureus, 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.

中文翻译:

具有交替序列的主链含锍聚合物的广谱杀菌活性和显着选择性

将阳离子基团结合到聚合物中是制备抗菌材料最广泛使用的策略之一。锍作为一种典型的阳离子部分,以小分子的形式显示出强大的抗菌功效,然而,长期以来在聚合物体系中表现不佳。在这里,我们开发了一系列交替的聚锍,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节。对广泛的临床相关细菌具有出色的抗菌活性,包括耐甲氧西林金黄色葡萄球菌, 可以在最佳组合物中获得,最小杀菌浓度在 1.25-10 μg/mL 范围内,在聚合物浓度甚至高达 10000 μg/mL 时溶血作用可忽略不计。由于抗菌作用可能是膜破坏机制,细菌不容易对聚锍产生抗性。这项工作表明具有明确序列的锍基聚合物可以作为对抗耐药细菌感染的有希望的候选者。
更新日期:2021-08-17
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