Zhang Lan, Tian Xiaoyuan, Sun Lei, Mi Kun, Wang Ru, Gong Fengying, Huang Lingli
College of Veterinary Medicine, Huazhong Agricultural University, Wuhan 430070, China.
National Reference Laboratory of Veterinary Drug Residues, Huazhong Agricultural University, Wuhan 430070, China.
Pharmaceutics. 2024 Jan 25;16(2):170. doi: 10.3390/pharmaceutics16020170.
Bacterial resistance is a growing problem worldwide, and the number of deaths due to drug resistance is increasing every year. We must pay great attention to bacterial resistance. Otherwise, we may go back to the pre-antibiotic era and have no drugs on which to rely. Bacterial resistance is the result of several causes, with efflux mechanisms widely recognised as a significant factor in the development of resistance to a variety of chemotherapeutic and antimicrobial medications. Efflux pump inhibitors, small molecules capable of restoring the effectiveness of existing antibiotics, are considered potential solutions to antibiotic resistance and have been an active area of research in recent years. This article provides a review of the efflux mechanisms of common clinical pathogenic bacteria and their efflux pump inhibitors and describes the effects of efflux pump inhibitors on biofilm formation, bacterial virulence, the formation of bacterial persister cells, the transfer of drug resistance among bacteria, and mismatch repair. Numerous efforts have been made in the past 20 years to find novel efflux pump inhibitors which are known to increase the effectiveness of medicines against multidrug-resistant strains. Therefore, the application of efflux pump inhibitors has excellent potential to address and reduce bacterial resistance.
细菌耐药性是一个在全球范围内日益严重的问题,因耐药性导致的死亡人数每年都在增加。我们必须高度重视细菌耐药性。否则,我们可能会回到抗生素出现之前的时代,没有药物可以依赖。细菌耐药性是由多种原因导致的,其中外排机制被广泛认为是对多种化疗药物和抗菌药物产生耐药性的一个重要因素。外排泵抑制剂是能够恢复现有抗生素效力的小分子,被认为是解决抗生素耐药性的潜在方案,并且近年来一直是一个活跃的研究领域。本文综述了常见临床病原菌的外排机制及其外排泵抑制剂,并描述了外排泵抑制剂对生物膜形成、细菌毒力、细菌持留细胞形成、细菌间耐药性转移以及错配修复的影响。在过去20年里,人们付出了诸多努力来寻找新型外排泵抑制剂,已知这些抑制剂可提高药物对多重耐药菌株的效力。因此,外排泵抑制剂的应用在应对和降低细菌耐药性方面具有巨大潜力。