一组基于Histatin5阳离子抗菌肽的设计、合成及抗菌活性  

Designing, Synthesis and Antimicrobial Activity of Cationic Antimicrobial Peptides Based on Histatin5

作　　者：路建光[1] 东圆珍[1] 朱裕辉[1] 张喜全[2] 冯军[1] 

机构地区：[1]中国医药工业研究总院上海医药工业研究院,创新药物与制药工艺国家重点实验室,上海200040 [2]江苏正大天晴药业股份有限公司,江苏南京210038

出　　处：《中国医药工业杂志》2013年第12期1210-1214,共5页Chinese Journal of Pharmaceuticals

基　　金：国家"重大新药创制"科技重大专项(2012ZX9301002-003)

摘　　要：Histatin5是人类唾液腺分泌的一种阳离子抗菌肽。本文以Histatin5及其类似物Dhvar4和Dhvar5为模板,设计9个具有新颖序列的抗菌肽,并用固相合成法进行合成。采用肉汤稀释法测定了抗菌肽的抗菌谱和最低抑菌浓度,结果显示有6个抗菌肽活性得到提高,呈现对细菌和真菌的广谱抗菌活性,并对临床常见耐药菌有效,值得进一步研究。本文还初步讨论了抗菌肽的抗菌活性与?-螺旋度、电荷、疏水性和两亲性的关系。Nine cationic antimicrobial peptides（CAMPs） were designed and synthesized based on Histatin5 and its analogues Dhvar4 and Dhvar5 and six of them exhibited higher in vitro activities against both standard and drug-resistant strains including bacteria and fungi by broth dilution method. The relationship between the antimicrobial activities of CAMPs and α-helicity, net positive charges, hydrophobicity as well as amphipathicity was discussed.

关 键 词：阳离子抗菌肽 多肽合成 最低抑菌浓度 

分 类 号：R978.16[医药卫生—药品]