Thoma Laura M, Boles Blaise R, Kuroda Kenichi
Department of Chemistry, University of Michigan , Ann Arbor, Michigan 48109, United States.
Biomacromolecules. 2014 Aug 11;15(8):2933-43. doi: 10.1021/bm500557d. Epub 2014 Jul 22.
The in vitro and in vivo antimicrobial activity of primary ammonium ethyl methacrylate homopolymers (AEMPs) was investigated. AEMPs with different degrees of polymerization (DP = 7.7-12) were prepared by reversible addition-fragmentation chain-transfer (RAFT) polymerization. The AEMPs showed higher inhibitory effects against Gram-positive bacteria, including methicillin-resistant Staphylococcus aureus (MRSA), than Gram-negative bacteria. The AEMPs also showed potent anti-S. aureus activity in the presence of fetal bovine serum, whereas the activity of the antibiotic mupirocin was reduced under the same conditions. The AEMPs showed very little or no hemolytic activity. The cytotoxicity of AEMPs against mammalian cells HEp-2 and COS-7 was concentration-dependent, and the cell viability significantly decreased at higher polymer concentrations. The AEMPs significantly reduced the number of viable S. aureus cells in the nasal environment of cotton rats when compared to that of the control. This study demonstrates that AEMPs have potential for use in treating topical S. aureus infections.
研究了甲基丙烯酸乙酯伯铵均聚物(AEMPs)的体外和体内抗菌活性。通过可逆加成-断裂链转移(RAFT)聚合制备了不同聚合度(DP = 7.7 - 12)的AEMPs。与革兰氏阴性菌相比,AEMPs对革兰氏阳性菌,包括耐甲氧西林金黄色葡萄球菌(MRSA),表现出更高的抑制作用。在胎牛血清存在的情况下,AEMPs也表现出强大的抗金黄色葡萄球菌活性,而在相同条件下抗生素莫匹罗星的活性降低。AEMPs表现出极少或无溶血活性。AEMPs对哺乳动物细胞HEp - 2和COS - 7的细胞毒性呈浓度依赖性,在较高聚合物浓度下细胞活力显著降低。与对照组相比,AEMPs显著减少了棉鼠鼻腔环境中活的金黄色葡萄球菌细胞数量。本研究表明,AEMPs有用于治疗局部金黄色葡萄球菌感染的潜力。