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用于根除细菌和真菌生物膜的具有可忽略溶血毒性的主链含锍均聚物。

Main-Chain Sulfonium-Containing Homopolymers with Negligible Hemolytic Toxicity for Eradication of Bacterial and Fungal Biofilms.

作者信息

Wang Xiao, Wang Guixian, Zhao Jinghua, Zhu Zhiyuan, Rao Jingyi

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.

Suzhou Jufeng Electrical Insulation System Co., Ltd., Suzhou, Jiangsu 215214, People's Republic of China.

出版信息

ACS Macro Lett. 2021 Dec 21;10(12):1643-1649. doi: 10.1021/acsmacrolett.1c00698. Epub 2021 Dec 10.

Abstract

Antimicrobials against planktonic cells and established biofilms at low doses are in increasing demand to tackle antibiotic-resistant biofilm infections. As a promising alternative to antibiotics, cationic polymers can effectively kill planktonic microbes but usually require high concentrations to eradicate the established biofilms. Herein, we developed a series of sulfonium-based homopolymers with cationic sulfoniums and alkane spacers in the main chain. These polysulfoniums presented effective activity against planktonic fungi () and bacteria ( and ) with minimum inhibition concentrations (MICs) of 0.5-32 μg/mL, and the optimal composition can provide an 80-90% reduction in biofilm mass and >99% killing of and cells in 3-day mature biofilms at 2 × MIC as well as steadily low hemolytic toxicity. The influence of amphiphilicity and charge density of polysulfonium homopolymers on their antimicrobial activity against planktonic microbes and mature biofilms was investigated to provide insights for effective antimicrobial polymer design.

摘要

为应对抗生素耐药性生物膜感染,低剂量下针对浮游细胞和已形成生物膜的抗菌剂需求日益增加。作为抗生素的一种有前景的替代品,阳离子聚合物可有效杀死浮游微生物,但通常需要高浓度才能根除已形成的生物膜。在此,我们开发了一系列主链中带有阳离子锍和烷烃间隔基的锍基均聚物。这些聚锍对浮游真菌()和细菌(和)具有有效活性,最低抑菌浓度(MIC)为0.5 - 32μg/mL,最佳组成在2×MIC时可使3天成熟生物膜中的生物膜量减少80 - 90%,并对和细胞的杀灭率>99%,且溶血毒性持续较低。研究了聚锍均聚物的两亲性和电荷密度对其针对浮游微生物和成熟生物膜的抗菌活性的影响,为有效的抗菌聚合物设计提供见解。

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