Beijing National Laboratory for Molecular Sciences, Key Laboratory of Polymer Chemistry and Physics of Ministry of Education, Center for Soft Matter Science and Engineering, College of Chemistry & Molecular Engineering, Peking University, Beijing 100871, China.
CAS Key Laboratory for Biomedical Effects of Nanomaterials and Nanosafety, CAS Center for Excellence in Nanoscience, National Center for Nanoscience and Technology (NCNST), Beijing, 100190, China.
J Mater Chem B. 2024 Feb 7;12(6):1569-1578. doi: 10.1039/d3tb02578k.
Antimicrobial peptide-mimicking antibacterial polymers represent a practical strategy to conquer the ever-growing threat of antimicrobial resistance. Herein, we report the syntheses and antibacterial performance of degradable amphiphilic cationic polyesters containing pendent quaternary ammonium motifs and hydrophobic alkyl or fluoroalkyl groups. These polyesters were conveniently prepared from poly(3-methylene-1,5-dioxepan-2-one) highly efficient one-pot successive thiol-Michael addition reactions. The antibacterial activity of these polyesters against and and their hemolytic activity toward red blood cells were evaluated; some of them showed moderate antibacterial activity and selectivity against Gram-positive . The membrane disruption mechanism of these cationic polyesters was briefly explored by monitoring the bacteria killing kinetics and SEM observations. Moreover, the effects of cationic/hydrophobic ratio and the incorporation of fluoroalkyl groups on the antibacterial activity and selectivity of the polyesters were demonstrated.
抗菌肽模拟抗菌聚合物代表了一种实用的策略,可以克服日益严重的抗菌耐药性威胁。本文报道了一系列含有季铵盐侧基和疏水烷基或氟烷基的可降解两亲性阳离子聚酯的合成及抗菌性能。这些聚酯可通过聚(3-亚甲基-1,5-二氧戊环-2-酮)与巯基化合物的高效一锅法连续硫醇-Michael 加成反应方便地制备。评估了这些聚酯对 和 以及对红细胞的溶血活性的抗菌活性;其中一些对革兰氏阳性菌具有中等的抗菌活性和选择性。通过监测细菌杀伤动力学和 SEM 观察,简要探讨了这些阳离子聚酯的膜破坏机制。此外,还研究了阳离子/疏水性比以及氟烷基的引入对聚酯抗菌活性和选择性的影响。