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作为富含色氨酸的阳离子肽模拟物合成的抗菌聚甲基丙烯酸酯。

Antimicrobial Polymethacrylates Synthesized as Mimics of Tryptophan-Rich Cationic Peptides.

作者信息

Locock Katherine E S, Michl Thomas D, Stevens Natalie, Hayball John D, Vasilev Krasimir, Postma Almar, Griesser Hans J, Meagher Laurence, Haeussler Matthias

机构信息

CSIRO Materials Science and Engineering, Bayview Avenue, Clayton, Victoria 3168, Australia.

Ian Wark Research Institute, University of South Australia, Mawson Lakes, South Australia 5095, Australia.

出版信息

ACS Macro Lett. 2014 Apr 15;3(4):319-323. doi: 10.1021/mz5001527. Epub 2014 Mar 19.

Abstract

This study describes a facile and high yielding route to two series of polymethacrylates inspired by the naturally occurring, tryptophan-rich cationic antimicrobial polymers. Appropriate optimization of indole content within each gave rise to polymers with high potency against (e.g., PGI-3 minimum inhibitory concentration (MIC) = 12 μg/mL) and the methicillin-resistant strain of (e.g., PGI-3 MIC = 47 μg/mL) with minimal toxicity toward human red blood cells. Future work will be directed toward understanding the cooperative roles that the cationic and indole pendant groups have for the mechanism of these polymers.

摘要

本研究描述了一种简便且高产率的方法,用于合成受天然存在的富含色氨酸的阳离子抗菌聚合物启发的两个系列的聚甲基丙烯酸酯。对每个系列中吲哚含量进行适当优化,得到了对金黄色葡萄球菌(例如,PGI - 3最低抑菌浓度(MIC)= 12μg/mL)和耐甲氧西林金黄色葡萄球菌菌株(例如,PGI - 3 MIC = 47μg/mL)具有高效力且对人红细胞毒性最小的聚合物。未来的工作将致力于了解阳离子和吲哚侧基在这些聚合物作用机制中的协同作用。

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