Understanding the evolution of macrolides resistance: A mini review

IF 3.7 3区 医学 Q2 INFECTIOUS DISEASES
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Abstract

Background

Macrolides inhibit the growth of bacterial cells by preventing the elongation of polypeptides during protein biosynthesis and include natural, synthetic, and semi-synthetic products. Elongation prevention occurs by blocking the passage of the polypeptide chain as the macrolides bind at the nascent peptide exit tunnel.

Objective

Recent data of ribosome profiling via ribo-seq further proves that, other than blocking the polypeptide chain, macrolides are also able to affect the synthesis of individual proteins. Thus, this shows that the mode of action of macrolides is more complex than we initially thought. Since the discovery of macrolides in the 1950s, they have been widely used in veterinary practice, agriculture, and medicine. Due to misuse and overuse of antibiotics, bacteria have acquired resistance against them. Hence, it is of utmost importance for us to fully understand the mode of action of macrolides as well as the mechanisms of resistance against macrolides in order to mitigate antibiotic-resistance issues.

Results

Chemical modifications can be performed to improve macrolide potency if we have a better understanding of their mode of action. Furthermore, a complete and detailed understanding of the mode of action of macrolides has remained vague, as new findings have challenged theories that are already in existence—due to this obscurity, research into macrolide modes of action continues to this day.

Conclusion

In this review, we present an overview of macrolide antibiotics, with an emphasis on the latest knowledge regarding the mode of action of macrolides as well as the mechanisms of resistance employed by bacteria against macrolides.

了解大环内酯类药物耐药性的演变:微型综述。
背景:大环内酯类药物通过阻止蛋白质生物合成过程中多肽的伸长来抑制细菌细胞的生长,包括天然、合成和半合成产品。大环内酯类药物与新生肽出口隧道结合后,会阻止多肽链的通过:最近通过核糖体分析(ribo-seq)获得的数据进一步证明,除了阻断多肽链外,大环内酯类药物还能影响单个蛋白质的合成。由此可见,大环内酯类药物的作用模式比我们最初想象的要复杂得多。自 20 世纪 50 年代发现大环内酯类药物以来,它们已被广泛应用于兽医、农业和医药领域。由于滥用和过度使用抗生素,细菌已经对它们产生了抗药性。因此,我们必须充分了解大环内酯类药物的作用模式和耐药性机制,以减轻抗生素耐药性问题:内容:在更好地了解大环内酯类药物的作用模式后,可以对其进行化学修饰以提高药效。此外,由于新的发现对已有的理论提出了挑战,人们对大环内酯类药物作用模式的完整详细了解仍然模糊不清--由于这种模糊不清,对大环内酯类药物作用模式的研究一直持续到今天:在这篇综述中,我们概述了大环内酯类抗生素,重点介绍了有关大环内酯类药物作用模式和细菌对大环内酯类药物产生耐药性机制的最新知识。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
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来源期刊
Journal of global antimicrobial resistance
Journal of global antimicrobial resistance INFECTIOUS DISEASES-PHARMACOLOGY & PHARMACY
CiteScore
8.70
自引率
2.20%
发文量
285
审稿时长
34 weeks
期刊介绍: The Journal of Global Antimicrobial Resistance (JGAR) is a quarterly online journal run by an international Editorial Board that focuses on the global spread of antibiotic-resistant microbes. JGAR is a dedicated journal for all professionals working in research, health care, the environment and animal infection control, aiming to track the resistance threat worldwide and provides a single voice devoted to antimicrobial resistance (AMR). Featuring peer-reviewed and up to date research articles, reviews, short notes and hot topics JGAR covers the key topics related to antibacterial, antiviral, antifungal and antiparasitic resistance.
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