Deformylated Gramicidin A and Its Derivatives Showing High Antimicrobial Activity and Low Hemolytic Toxicity  

作　　者：Wei-Wei Haoyang Min Zhang Jun-Li Hou 

机构地区：[1]Department of Chemistry,Fudan University,220 Handan Road,Shanghai 200433,China

出　　处：《Chinese Journal of Chemistry》2019年第1期25-29,共5页中国化学（英文版）

基　　金：the National Natural Science Foundation of China (21725202,21572035);the National R&D Program of China (2017YFA0206901);STCSM (18XD1400800,18JC1411600)for financial support.

摘　　要：Summary of main observation and conclusion Gramicidin A is a natural peptide,which shows high antimicrobial activity to Gram-positive bacteria. However,the hemolytic toxicity prevents its therapeutic usage.We demonstrated that by simply removing the formyl group at the N terminus,the hemolytic toxicity of the peptide could be obviously decreased.The deformylated gramicidin A (1)could efficiently insert into the lipid bilayer to form transmembrane channels.The peptide can also selectively insert into the membrane of Gram-positive bacteria but not that of erythrocytes,leading to its high antimicrobial activity and very low hemolytic toxicity.The derivation of 1 could be achieved by decoration at the terminal NH2 group,which also produced peptides showing high activity and low hemolytic toxicity.This derivation method provided us with an efficient strategy to build a library for future activity and cytotoxicity screening in vitro and in vivo.

关 键 词：PEPTIDE BUILD GROUP 

分 类 号：O6[理学—化学]