Engineering Antibacterial Activities and Biocompatibility of Hyperbranched Lysine-based Random Copolymers  

作　　者：Hui Liu Xiao Liu Yuan-Qiao Cao Ming Liu Miao-Miao Han Sheng-Xiang Ji 

机构地区：[1]Key Laboratory of Polymer Ecomaterials,Changchun Institute of Applied Chemistry,Chinese Academy of Sciences,Changchun 130022,China [2]University of Science and Technology of China,Hefei 230026,China

出　　处：《Chinese Journal of Polymer Science》2023年第3期345-355,I0006,共12页高分子科学（英文版）

基　　金：financially supported by the National Natural Science Foundation of China(No.51973212);Department of Science and Technology of Jilin Province(Nos.20210203119SF and 20210203173SF)。

摘　　要：Antimicrobial peptides(AMPs)have been considered as an alternative to small molecule antibiotics since they are difficult to develop antimicrobial resistance.Hyperbranched polylysine(HPL),an AMP mimics,has gained attention due to its broad-spectrum antibacterial activities,but it also suffers from high toxicity.Here we report a facile strategy to engineer the toxicity of HPL by copolymerizing lysine(K)with a hydrophobic amino acid,e.g.,alanine(A),tryptophan(W)or phenylalanine(F),to afford hyperbranched random copolymers.These copolymers have comparable antibacterial activities to HPL while their cytotoxicities and in vivo toxicities are lowered when the type and content of hydrophobic amino acid and the size of copolymers are optimized.The G.mellonella infection model demonstrates that the copolymers are effective against the S.aureus infection in vivo.The copolymers kill the bacteria through the disruption of cell membranes and the bacteria do not develop resistance to the copolymers.

关 键 词：Hyperbranched random copolymers LYSINE Hydrophobic amino acid Antibacterial activity High selectivity 

分 类 号：TQ317[化学工程—高聚物工业] R318.08[医药卫生—生物医学工程]