Department of Medical Laboratory, Weifang Medical University, Weifang, Shandong, 261053, P.R. China.
Institutional Key Laboratory of Clinical Laboratory Diagnostics, 12th 5-Year Project of Shandong Province, Weifang Medical University, Weifang, Shandong, 261053, P.R. China.
Protein Pept Lett. 2023;30(4):280-294. doi: 10.2174/0929866530666230315113624.
The high global burden of tuberculosis (TB) and the increasing emergence of the drugresistant (DR) strain of Mycobacterium tuberculosis () emphasize the urgent need for novel antimycobacterial agents. Antimicrobial peptides (AMPs) are small peptides widely existing in a variety of organisms and usually have amphiphilic cationic structures, which have a selective affinity to the negatively charged bacterial cell wall. Besides direct bactericidal mechanisms, including interacting with the bacterial cell membrane and interfering with the biosynthesis of the cell wall, DNA, or protein, some AMPs are involved in the host's innate immunity. AMPs are promising alternative or complementary agents for the treatment of DR-TB, given their various antibacterial mechanisms and low cytotoxicity. A large number of AMPs, synthetic or natural, from human to bacteriophage sources, have displayed potent anti-mycobacterial activity in vitro and in vivo. In this review, we summarized the features, antimycobacterial activity, and mechanisms of action of the AMPs according to their sources. Although AMPs have not yet met the expectations for clinical application due to their low bioavailabilities, high cost, and difficulties in large-scale production, their potent antimycobacterial activity and action mechanisms, which are different from conventional antibiotics, make them promising antibacterial agents against DR- in the future.
全球结核病（TB）负担沉重，结核分枝杆菌（）耐药菌株不断出现，这强调了急需新型抗分枝杆菌药物。抗菌肽（AMPs）是广泛存在于多种生物体中的小肽，通常具有两亲性阳离子结构，对带负电荷的细菌细胞壁具有选择性亲和力。除了直接杀菌机制，包括与细菌细胞膜相互作用以及干扰细胞壁、DNA 或蛋白质的生物合成外，一些 AMPs 还参与宿主的先天免疫。鉴于其多种抗菌机制和低细胞毒性，AMP 是治疗耐多药结核病（DR-TB）的有前途的替代或补充药物。大量来自人类到噬菌体来源的 AMPs，无论是天然的还是合成的，在体外和体内都显示出很强的抗分枝杆菌活性。在这篇综述中，我们根据 AMP 的来源总结了它们的特征、抗分枝杆菌活性和作用机制。尽管由于生物利用度低、成本高和大规模生产困难，AMP 尚未达到临床应用的期望，但它们强大的抗分枝杆菌活性和不同于传统抗生素的作用机制，使它们有望成为未来治疗耐多药的抗菌药物。
