新型阳离子抗菌肽的合成及其抗菌活性  

Synthesis of New Cationic Antimicrobial Peptides and Their Antimicrobial Activities

作　　者：夏江华[1] 赵伟 王岩[1] 张喜全 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201203 [2]正大天晴药业集团股份有限公司,江苏南京210038

出　　处：《中国医药工业杂志》2016年第3期277-281,共5页Chinese Journal of Pharmaceuticals

基　　金：国家“重大新药创制”科技重大专项(2014ZX09507009-024)

摘　　要：本研究以抗菌肽Pep05（1）为模板,通过截短肽链和氨基酸替换设计了13条具有新型结构的抗菌肽（2~14）,用固相合成法合成,以反相高效液相色谱法分离纯化,并用微量肉汤稀释法测定抗菌活性。改造后得到的抗菌肽2、3、7、8、10的抗菌活性比1有所提高,抗大肠杆菌和铜绿假单胞菌的最低抑菌浓度（MIC）均为4μg/ml,比1增强2倍。同时还探讨了肽链长度、电荷数及疏水性与抗菌活性之间的关系。Thirteen cationic antimicrobial peptides （2--14） were designed based on Pep05 （1） by tnmcating and replacing amino acids. These antimicrobial peptides were synthesized with solid phase method and purified by RP- HPLC. Their antimicrobial activities were determined by broth microdilution method. The antimicrobial activities of peptides 2, 3, 7, 8 and 10 were all two times higher than that of 1, whose minimal inhibitory concentration （MICs） against Escherichia coli and Pseudomonas aeruginosa were 4 ktg/ml. Meanwhile, the relationships between lengths, charges and hydrophobicity of these peptides and their antimicrobial activities were also investigated.

关 键 词：阳离子抗菌肽 固相合成 抗菌活性 最低抑菌浓度 

分 类 号：R978.16[医药卫生—药品]