Varella Coelho Marcus Lívio, de Souza Duarte Andreza Freitas, do Carmo de Freire Bastos Maria
Departamento de Microbiologia Geral, Instituto de Microbiologia Paulo de Góes, UFRJ, Rio de Janeiro, Brazil.
Curr Top Med Chem. 2017;17(10):1177-1198. doi: 10.2174/1568026616666160930144809.
One of the biggest challenges faced presently by clinicians is the emergence of multidrug -resistant pathogens that can infect humans and animals. To control the infections caused by such pathogens the development of new drugs is required. Bacteria are a rich source of ribosomally -synthesized antimicrobial peptides known as bacteriocins, which are characterized by the presence of a self-defense immunity system. Labionin-containing lantibiotics and sactibiotics are posttranslationally modified bacteriocins with peculiar features. Labionin-containing peptides belong to subclass Ic lantibiotics in which the carbacyclic triamino triacid labionin, a structural variant of lanthionine, and a methyl-substitute labionin derivative are found, giving the molecule a labyrinthine structure. Sactibiotics are circular or linear peptides belonging to a distinct bacteriocin class (class V) which is characterized by the presence of cross-linkages formed by the thiol group of cysteine residues and the α-carbon of acceptor amino acids. A few examples of these bacteriocins have been described in the literature to date, although putative gene clusters with the potential to encode such peptides can be found in the genome of many bacterial species. Some peptides already under study exhibit potential biotechnological applications because of their remarkable antibacterial or antiviral activities, as well as their analgesic activity. Therefore, in this review, the main findings concerning these peptides will be addressed and discussed, with an emphasis on their potential use in clinical settings.
临床医生目前面临的最大挑战之一是出现了可感染人类和动物的多重耐药病原体。为了控制此类病原体引起的感染,需要开发新药。细菌是核糖体合成的抗菌肽(即细菌素)的丰富来源,其特点是存在自我防御免疫系统。含拉比宁的羊毛硫抗生素和硫肽抗生素是具有独特特征的翻译后修饰细菌素。含拉比宁的肽属于Ic类羊毛硫抗生素,其中发现了碳环三氨基三酸拉比宁(羊毛硫氨酸的结构变体)和甲基取代的拉比宁衍生物,赋予分子迷宫般的结构。硫肽抗生素是属于不同细菌素类别(V类)的环状或线性肽,其特点是存在由半胱氨酸残基的巯基与受体氨基酸的α-碳形成的交联。迄今为止,文献中已描述了这些细菌素的一些实例,尽管在许多细菌物种的基因组中可以找到有可能编码此类肽的推定基因簇。一些正在研究的肽由于其显著的抗菌或抗病毒活性以及镇痛活性而展现出潜在的生物技术应用。因此,在本综述中,将阐述和讨论有关这些肽的主要研究结果,重点是它们在临床环境中的潜在用途。