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首页> 外文期刊>ACS Macro Letters >Convenient Preparation of Bactericidal Hydrogels by Covalent Attachment of Stabilized Antimicrobial Peptides Using Thiol-ene Click Chemistry
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Convenient Preparation of Bactericidal Hydrogels by Covalent Attachment of Stabilized Antimicrobial Peptides Using Thiol-ene Click Chemistry

机译:使用硫醇-烯点击化学法通过稳定的抗菌肽共价连接方便地制备杀菌水凝胶

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摘要

This report describes the design and synthesis of a bactericidal poly(ethylene glycol)-based (PEG) hydrogel coating with covalently attached antimicrobial peptides (AMP) stabilized against proteolytic degradation. As such, mimics of the highly active AMP HHC10 (H-KRWWKWIRW-NH2) were designed for optimal stability in human serum while retaining strong antimicrobial activity against Staphylococcus aureus and Staphylococcus epidermidis, the major causative agents of biomaterial associated infection. In order to investigate the selectivity of the AMPs, their hemolytic activity was determined. A N-terminal cysteine facilitated thiol-ene chemistry for a fast, single-step immobilization/photopolymerization strategy. The antimicrobial activity of the resulting thin layer hydrogel coating on a PET surface was established using the Japanese Industrial Standard (JIS) Z2801 assay, showing complete killing (>99.9%) of inocula of S. aureus ATCC 49230, S. epidermidis ATCC 35984, and E. coli ATCC 8739.
机译:该报告描述了具有抗蛋白水解降解作用的共价连接的抗菌肽(AMP)的基于杀菌性聚(乙二醇)的(PEG)水凝胶涂层的设计和合成。因此,高活性AMP HHC10(H-KRWWKWIRW-NH2)的模拟物旨在在人血清中达到最佳稳定性,同时保留对金黄色葡萄球菌和表皮葡萄球菌(生物材料相关感染的主要病因)的强力抗菌活性。为了研究AMPs的选择性,确定了它们的溶血活性。 N端半胱氨酸促进了硫醇-烯化学反应,实现了快速,一步固定/光聚合策略。使用日本工业标准(JIS)Z2801测定法确定了在PET表面上形成的薄层水凝胶涂层的抗菌活性,显示金黄色葡萄球菌ATCC 49230,表皮葡萄球菌ATCC 35984的接种物被完全杀死(> 99.9%)。和大肠杆菌ATCC 8739。

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