Methacrylamide based antibiotic polymers with no detectable bacterial resistance,Soft Matter

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Methacrylamide based antibiotic polymers with no detectable bacterial resistance
Soft Matter ( IF 2.9 ) Pub Date : 2021-2-9 , DOI: 10.1039/d0sm02176h
Anju Tyagi ₁ , Abhijit Mishra

Affiliation

The growing number of multidrug-resistant pathogens is a major healthcare concern. In search of alternatives to antibiotics, synthetic mimics of antimicrobial peptides (SMAMPs) in the form of antimicrobial polymers have gained tremendous attention. Here, we report the synthesis of a set of 7 amphiphilic water-soluble cationic copolymers using aminopropyl methacrylamide and benzyl methacrylamide repeat units that show significant antibacterial activity. The antibacterial activity was evaluated using a broth microdilution assay against S. aureus and E. coli, while toxicity to mammalian cells was quantified by hemolysis assay with human red blood cells (RBCs). We find that the antibacterial activity and selectivity of the polymers depends on the mole fraction of aromatic benzyl units (f_benzyl) and the average molecular weight (M_n). Polymers with f_benzyl of 0.10 and 0.19, named AB-10 and AB-19 respectively, exhibited the highest antibacterial efficacy without inducing hemolysis and were chosen for further study. Liposome dye leakage study and observations from confocal and scanning electron microscopy indicate that the AB polymers killed bacterial cells primarily by disrupting the cytoplasmic membrane. No resistant mutants of E. coli and S. aureus were obtained with AB-19 in a 30 day serial passage study.

中文翻译：

基于甲基丙烯酰胺的抗生素聚合物，无可检测的细菌抗性

越来越多的耐多药病原体是一个主要的医疗保健问题。在寻找抗生素的替代品时，以抗微生物聚合物形式存在的抗微生物肽（SMAMPs）的合成模拟物引起了极大的关注。在这里，我们报告了一组使用具有显着抗菌活性的氨丙基甲基丙烯酰胺和苄基甲基丙烯酰胺重复单元合成的7种两亲水溶性阳离子共聚物。使用肉汤微量稀释测定法对金黄色葡萄球菌和大肠杆菌的抗菌活性进行了评估，而对哺乳动物细胞的毒性通过用人红细胞（RBC）的溶血测定法进行了定量。我们发现聚合物的抗菌活性和选择性取决于芳族苄基单元的摩尔分数（f_苄基）和平均分子量（M _n）。f_苄基为0.10和0.19的聚合物，分别命名为AB-10和AB-19，在不引起溶血的情况下表现出最高的抗菌功效，因此被选择作进一步研究。脂质体染料泄漏的研究以及共聚焦和扫描电子显微镜的观察表明，AB聚合物主要通过破坏细胞质膜杀死细菌细胞。在30天的连续传代研究中，用AB-19未获得大肠杆菌和金黄色葡萄球菌的抗性突变体。

更新日期：2021-03-01

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