Mangoni Maria Luisa, Luca Vincenzo, McDermott Alison M
Istituto Pasteur-Fondazione Cenci Bolognetti, Department of Biochemical Sciences "A. Rossi Fanelli", Sapienza University of Rome, Piazzale Aldo Moro, 5-00185 Rome, Italy.
Istituto Pasteur-Fondazione Cenci Bolognetti, Department of Biochemical Sciences "A. Rossi Fanelli", Sapienza University of Rome, Piazzale Aldo Moro, 5-00185 Rome, Italy.
Peptides. 2015 Sep;71:286-95. doi: 10.1016/j.peptides.2015.04.018. Epub 2015 May 8.
Due to the growing emergence of resistance to commercially available antibiotics/antimycotics in virtually all clinical microbial pathogens, the discovery of alternative anti-infective agents, is greatly needed. Gene-encoded antimicrobial peptides (AMPs) hold promise as novel therapeutics. In particular, amphibian skin is one of the richest storehouses of AMPs, especially that of the genus Rana, with esculentins-1 being among the longest (46 amino acids) AMPs found in nature to date. Here, we report on the recently discovered in vitro and in vivo activities and mechanism of action of two derivatives of the N-terminal part of esculentin-1a and -1b peptides, primarily against two relevant opportunistic microorganisms causing a large number of life-threatening infections worldwide; i.e. the Gram-negative bacterium Pseudomonas aeruginosa and the yeast Candida albicans. Because of distinct advantages compared to several mammalian AMPs, the two selected frog skin AMP-derivatives represent attractive candidates for the development of new antimicrobial compounds with expanded properties, for both human and veterinary medicine.
由于几乎所有临床微生物病原体对市售抗生素/抗真菌药的耐药性日益增加，因此迫切需要发现替代抗感染药物。基因编码的抗菌肽（AMPs）有望成为新型治疗药物。特别是，两栖动物皮肤是AMPs最丰富的储存库之一，尤其是林蛙属，其中埃斯库林-1是迄今为止自然界中发现的最长（46个氨基酸）的AMPs之一。在这里，我们报告了最近发现的埃斯库林-1a和-1b肽N端部分的两种衍生物的体外和体内活性及作用机制，主要针对两种在全球范围内引起大量危及生命感染的相关机会性微生物；即革兰氏阴性菌铜绿假单胞菌和酵母白色念珠菌。与几种哺乳动物AMPs相比，这两种选定的青蛙皮肤AMP衍生物具有明显优势，它们是开发具有扩展特性的新型抗菌化合物的有吸引力的候选物，可用于人类和兽医学。
