Zhang Long, Zhang Yongkang, Zhao Gang, Yang Han, Wang Xiaoqian, Yu Rutong, Liu Hongmei, Li Shanshan
Insititute of Nervous System Diseases, Xuzhou Medical University, Xuzhou 221002, P. R. China.
Department of Neurosurgery, Affiliated Hospital of Xuzhou Medical University, Xuzhou 221002, P. R. China.
ACS Omega. 2020 Sep 1;5(36):23053-23061. doi: 10.1021/acsomega.0c02774. eCollection 2020 Sep 15.
Bacterial infections are the most common type of clinical infection. The abuse of clinical antibiotics has led to the frequent appearance of drug-resistant strains and even some super bacteria. In this study, we synthesized Poly(MTZ) -(DMAEMA) polymer micelles with cations on the surface. The synthesis of this novel polymer comes in two steps. First, Poly(MTZ) was synthesized with metronidazole (MTZ) referred as the macromolecular chain transfer agent and v-501 as the initiator for initiating the polymerization of 4-cyanopentanoic acid dithiobenzoate. Then, novel polymer micelles were synthesized with Poly(MTZ) referred as the macromolecular chain transfer agent and v-501 as the initiator for initiating the polymerization of the monomer 2-(dimethylamino) ethyl methacrylate, which could adsorb to the negatively charged bacterial surface via electrostatic interaction and enhance bactericidal activity. Scanning electron microscopy showed that the micelles could be accurately targeted to the surface of bacteria, and the zone of inhibition assay confirmed that the micelles could enhance the sensitivity of bacteria to drugs. Hence, Poly(MTZ) -(DMAEMA) polymer micelles will have potential use for the clinical treatment of anaerobic infections in the future.
细菌感染是临床感染中最常见的类型。临床抗生素的滥用导致耐药菌株甚至一些超级细菌频繁出现。在本研究中,我们合成了表面带阳离子的聚(甲硝唑)-(甲基丙烯酸二甲氨基乙酯)聚合物胶束。这种新型聚合物的合成分两步进行。首先,以甲硝唑(MTZ)作为大分子链转移剂,以V-501作为引发剂引发4-氰基戊酸二硫代苯甲酸酯的聚合反应,合成聚(MTZ)。然后,以聚(MTZ)作为大分子链转移剂,以V-501作为引发剂引发单体甲基丙烯酸2-(二甲氨基)乙酯的聚合反应,合成新型聚合物胶束,该聚合物胶束可通过静电相互作用吸附到带负电荷的细菌表面并增强杀菌活性。扫描电子显微镜显示胶束可精确靶向细菌表面,抑菌圈试验证实胶束可增强细菌对药物的敏感性。因此,聚(MTZ)-(甲基丙烯酸二甲氨基乙酯)聚合物胶束在未来临床治疗厌氧菌感染方面将具有潜在用途。