抗菌肽分子结构对其活性的影响

The influence of molecular structure on antimicrobial peptides' activity

抗菌肽是一种广泛存在于生物界的抵抗病原微生物入侵的小分子多肽,是生物先天免疫的重要组成部分,具有广谱抗菌活性和抗肿瘤、抗病毒、抗真菌、抗寄生虫及免疫调节等生物活性,其区别于传统抗生素的独特作用机理,使其不易产生耐药性,是一类极具潜力的肽类抗生素。抗菌肽多样的分子结构是其产生生物活性的基础,研究表明抗菌肽的正电荷数、水脂两亲结构、保守序列、α-螺旋、二硫键、铰链结构和氨基酸构型对抗菌肽的活性至关重要。围绕以上几个方面对抗菌肽进行分子设计和改造,人们有望更加有效地提高抗菌肽的抗菌活性,获得到更加高效、低毒的抗菌肽产品。现就抗菌肽的分子结构以及结构对活性的影响等方面做一综述。

Antimicrobial peptides are ubiquitous in nature where they play important roles in host defense and microbial control.More than 1,500 naturally occurring peptides have been described so far and shown to have broad spectrum antimicrobial activity,able to kill most strains of bacteria as well as some fungi,viruses,protozoa,and in addition,many types of tumor cells.The mechanism of action which is not easy to cause drug resistance is different from that of conventional antibiotics.As the foundation of antimicrobial activity,structural properties of antimicrobial peptides are numerous.In general,the number of the net cationic charge,amphipathic structures,conserved sequence,α-helix,disulfide bond,hinge region and L-or D-Protein are significant to antimicrobial peptides＇ activity.Research on structure-activity relationship has contributed to the design of more efficient and less poisonous antimicrobial peptides.Recent studies about the relationship among peptide structure,function and molecule design are reviewed in this paper.