天蚕素类抗菌肽分子设计研究进展

Advances in Research on Molecular Design of Cecropin-like Peptides

天蚕素是一类由31~39个氨基酸残基组成的阳离子型线性α螺旋抗菌肽,具有抗细菌、抗真菌、抗病毒以及抑制肿瘤细胞等生物活性。天蚕素与传统抗生素作用机制不同,具有不易产生耐药性的特点,因此成为解决传统抗生素多重耐药性问题的一个新突破口。然而,天蚕素在抗菌活性、选择性、毒性以及稳定性等方面还存在诸多问题,并且天然天蚕素提取工艺复杂,成本较高,不适合大规模生产,其对细菌的高毒性也限制了原核工程菌的使用。近年来多肽分子设计的研究方法颇受青睐,为解决多肽物质诸多问题开辟了新的途径。针对天蚕素类抗菌肽研究过程中面临的主要问题综述了其分子设计的研究进展。

Cecropins, a series of linear 31 - 39-residue cationic α-helical antimicrobial peptides, display extensive bioaetivities against bacteria, fungus, virus and neoplastic cells. The mechanism of cecropins which is different from traditional antibiotics gives them the advantage that they tend to be not easily develop drug resistance,which indicate that cecropins may be potential potent novel antimicrobial agents to resolve multi-drug resistence problems. However, several problems of cecropins concerning antimicrobial activity, selectivity, toxicity, and stability remain to be solved. Moreover, natural ceeropins are not suitable for mass production due to their complicated extraction process and huge costs as well as high toxicity to prokaryote limit the use of engineering bacteria. Molecular design methods to solve these problems are reviewed.