作者：Peng Liu, Gang Xu, Dicky Pranantyo, Li Qun Xu , Koon-Gee Neoh , and En-Tang Kang*
关键字：antimicrobial; biocompatible; charge-convertible; pH-sensitive; targeting; zwitterionic polymer
论文来源：期刊
具体来源：http://pubs.acs.org/doi/abs/10.1021/acsbiomaterials.7b00723
发表时间：2017年
It is highly desirable to develop new and more potent biocompatible antimicrobial agents to reduce the increasing risk of bacterial infection worldwide. To address this problem, we prepared a smart pH-sensitive polymer, poly(N′-citraconyl-2-(3-aminopropyl-N,N-dimethylammonium)ethyl methacrylate), or P(CitAPDMAEMA), which can undergo change in functionality from a biocompatible zwitterionic polymer to an antimicrobial cationic polymer at acidic bacterial infection sites. The precursor polymer, poly(2-(3-aminopropyl-N,N-dimethylammonium)ethyl methacrylate) (P(APDMAEMA)), was first prepared by reversible addition–fragmentation chain transfer (RAFT) polymerization, and then modified with citraconic anhydride to obtain the zwitterionic P(CitAPDMAEMA). P(CitAPDMAEMA) is zwitterionic at physiological pH and exhibits low hemotoxicity and good biocompatibility. However, P(CitAPDMAEMA) can change from neutral to cationic with decreasing pH because of the hydrolysis of citraconic amide under low pH conditions. This switch leads to pronounced bacteria binding of cationic P(CitAPDMAEMA) under acidic conditions of the infection sites and significantly inhibits the growth of Escherichia coli (E. coli) and Staphylococcus aureus (S. aureus). These results indicate that P(CitAPDMAEMA) is potentially a new on-demand antimicrobial agent.