Laboratory of Molecular Biology, State University of Paraiba, Joao Pessoa-PB, Brazil.
Laboratory of Synthesis and Drug Delivery, State University of Paraiba, Joao Pessoa-PB, Brazil.
Curr Top Med Chem. 2018;18(1):42-74. doi: 10.2174/1568026618666180206095224.
The ever increasing number of multidrug-resistant microorganism pathogens has become a great and global public health threat. Antibiotic mechanisms of action and the opposing mechanisms of resistance are intimately associated, but comprehension of the biochemical and molecular functions of such drugs is not a simple exercise. Both the environment, and genetic settings contribute to alterations in phenotypic resistance (natural bacterial evolution), and make it difficult to control the emergence and impacts of antibiotic resistance. Under such circumstances, comprehension of how bacteria develop and/or acquire antibiotic resistance genes (ARG) has a critical role in developing propositions to fight against these superbugs, and to search for new drugs. In this review, we present and discuss both general information and examples of common genetic and molecular mechanisms related to antibiotic resistance, as well as how the expression and interactions of ARGs are important to drug resistance. At the same time, we focus on the recent achievements in the search for antibiotic adjuvants, which help combat antibiotic resistance through deactivation of bacterial mechanisms of action such as β-lactamases. Recent advances involving the use of anti-resistance drugs such as: efflux pump inhibitors; anti-virulence drugs; drugs against quorum sensing; and against type II/III secretion systems are revealed. Such antibiotic adjuvants (as explored herein) collaborate against the problems of antibiotic resistance, and may restore or prolong the therapeutic activity of known antibiotics.
不断增加的多药耐药微生物病原体已成为一个巨大的全球公共卫生威胁。抗生素的作用机制和耐药的拮抗机制密切相关,但理解这些药物的生化和分子功能并不是一件简单的事情。环境和遗传背景都会导致表型耐药性(细菌自然进化)的改变,这使得控制抗生素耐药性的出现和影响变得困难。在这种情况下,了解细菌如何产生和/或获得抗生素耐药基因(ARG)对于提出对抗这些超级细菌的措施以及寻找新药具有关键作用。在这篇综述中,我们介绍和讨论了与抗生素耐药性相关的一般信息和常见遗传和分子机制的实例,以及 ARG 的表达和相互作用如何对抗生素耐药性很重要。同时,我们专注于寻找抗生素佐剂的最新进展,这些佐剂通过使细菌的作用机制失活(如β-内酰胺酶)来帮助对抗抗生素耐药性。本文还揭示了使用抗耐药药物(如:外排泵抑制剂;抗毒力药物;群体感应抑制剂;以及 II/III 型分泌系统抑制剂)的最新进展。这些抗生素佐剂(如本文所探讨的)共同对抗抗生素耐药性问题,并可能恢复或延长已知抗生素的治疗活性。