Nimmagadda Alekhya, Liu Xuan, Teng Peng, Su Ma, Li Yaqiong, Qiao Qiao, Khadka Nawal K, Sun Xiaoting, Pan Jianjun, Xu Hai, Li Qi, Cai Jianfeng
Department of Medical Oncology, Shuguang Hospital, Shanghai University of Traditional Chinese Medicine , Shanghai 201203, People's Republic of China.
College of Chemistry and Chemical Engineering, Central South University , Changsha, HN 410083, People's Republic of China.
Biomacromolecules. 2017 Jan 9;18(1):87-95. doi: 10.1021/acs.biomac.6b01385. Epub 2016 Dec 8.
The resistance developed by life-threatening bacteria toward conventional antibiotics has become a major concern in public health. To combat antibiotic resistance, there has been a significant interest in the development of antimicrobial cationic polymers due to the ease of synthesis and low manufacturing cost compared to host-defense peptides (HDPs). Herein, we report the design and synthesis of amphiphilic polycarbonates containing primary amino groups. These polymers exhibit potent antimicrobial activity and excellent selectivity to Gram-positive bacteria, including multidrug resistant pathogens. Fluorescence and TEM studies suggest that these polymers are likely to kill bacteria by disrupting bacterial membranes. These polymers also show low tendency to elicit resistance in bacteria. Their further development may lead to new antimicrobial agents combating drug-resistance.
危及生命的细菌对传统抗生素产生的耐药性已成为公共卫生领域的一个主要问题。为了对抗抗生素耐药性，与宿主防御肽（HDPs）相比，由于合成简便且制造成本低，抗菌阳离子聚合物的开发引起了人们极大的兴趣。在此，我们报告了含伯氨基的两亲性聚碳酸酯的设计与合成。这些聚合物表现出强大的抗菌活性以及对革兰氏阳性菌（包括多重耐药病原体）的优异选择性。荧光和透射电子显微镜研究表明，这些聚合物可能通过破坏细菌膜来杀死细菌。这些聚合物在细菌中引发耐药性的倾向也较低。它们的进一步开发可能会带来对抗耐药性的新型抗菌剂。
