Vaara Martti
Northern Antibiotics Ltd, Eskolantie 1, POB 72, FI-00720 Helsinki, Finland.
Curr Opin Pharmacol. 2009 Oct;9(5):571-6. doi: 10.1016/j.coph.2009.08.002. Epub 2009 Sep 6.
The emergence and rapid spread of extremely multiresistant bacteria necessitates every effort to develop novel antibacterial agents. Host-derived antimicrobial peptides (AMPs) pexiganan (a magainin), omiganan (an indolicidin), and iseganan (a protegrin) have been in clinical phases for more than 10 years and provide little in combating against those bacteria. Even though some recent approaches may yield more effective and better-tolerated derivatives of host-derived AMPs, most novel derivatives suffer from weak activity, nonspecific cytotoxicity, and apparent susceptibility to proteolysis. Few have undergone any systematic toxicity and efficacy studies. Bacterial peptides and their derivatives, such as lantibiotics, the RTA-3 peptide, and novel polymyxins, as well as certain peptidomimetics, such as ceragenins, might be more useful.
具有极强多重耐药性的细菌的出现和迅速传播，使得人们必须竭尽全力研发新型抗菌剂。源自宿主的抗菌肽（AMPs），如派罗星（一种蛙皮素）、奥米加南（一种吲哚杀菌素）和伊西加南（一种防御素），已经处于临床阶段超过10年了，但在对抗这些细菌方面成效甚微。尽管最近的一些方法可能会产生更有效且耐受性更好的源自宿主的抗菌肽衍生物，但大多数新型衍生物都存在活性较弱、非特异性细胞毒性以及对蛋白水解明显敏感的问题。很少有进行过任何系统的毒性和疗效研究。细菌肽及其衍生物，如羊毛硫抗生素、RTA - 3肽和新型多粘菌素，以及某些肽模拟物，如杀菌肽，可能会更有用。
