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首页> 外文期刊>Biomaterials Science >Development of mechanism-based antibacterial synergy between Fmoc-phenylalanine hydrogel and aztreonam
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Development of mechanism-based antibacterial synergy between Fmoc-phenylalanine hydrogel and aztreonam

机译：FMOC-苯丙氨酸水凝胶和阿兹特瓜胺型机理抗菌协同作用的研制

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摘要

Recently, fluorenylmethyloxycarbonyl (Fmoc) conjugated amino acids (Fmoc-AA), especially Fmoc-phenylalanine (Fmoc-F), have been discovered to have antimicrobial properties specific to Gram-positive bacteria including MRSA. Their weak antibacterial activity against Gram-negative bacteria is due to their inability to cross the bacterial membrane. Here in order to increase the antibacterial spectrum of Fmoc-F, we prepared a formulation of Fmoc-F with the Gram-negative specific antibiotic aztreonam (AZT). This formulation displayed antibacterial activity against both Gram-positive and Gram-negative bacteria and significantly reduced the bacterial load in a mouse wound infection model. The combination produced a synergistic effect and higher efficacy against P. aeruginosa due to the increased Fmoc-F permeability by AZT through the bacterial membrane. This combinatorial approach could be an effective strategy for other Fmoc-AA having a Gram-positive specific antibacterial effect for the better management of bacterial wound infections.
机译：最近，已发现芴基甲氧基羰基（FMOC）缀合的氨基酸（FMOC-AA），特别是FMOC-苯丙氨酸（FMOC-F）具有特异于包括MRSA的革氏阳性细菌的抗微生物性质。它们对革兰阴性细菌的弱抗菌活性是由于它们无法穿过细菌膜。这里为了增加FMOC-F的抗菌谱，我们制备了用革兰氏阴性特异性抗生素AztReonam（AZT）的FMOC-F的配方。该配方显示针对革兰氏阳性和革兰氏阴性细菌的抗菌活性，并显着降低了小鼠伤口感染模型中的细菌载荷。由于AZT通过细菌膜的FMOC-F渗透率增加，该组合产生了对铜绿假单胞菌的协同效应和更高的疗效。这种组合方法可以是具有革兰氏阳性特异性抗菌作用的其他FMOC-AA的有效策略，用于更好地管理细菌伤口感染。

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