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基于新型抗菌策略——抗菌肽大分子偶联物的制备及抗菌性能研究

Synthesis and antibacterial property of an antibacterial peptide-chitosan coupling copolymer——based on a novel antibacterial strategy

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【作者】 韩永萍; 贾新宇; 何江川;

【Author】 HAN Yong-ping;JIA Xin-yu;HE Jiang-chuan;College of Bio-chemical Engineering, Beijing Union University;

【通讯作者】 何江川;

【机构】 北京联合大学生物化学工程学院;

【摘要】 以羧基和叠氮基进行端基修饰的聚乙二醇为连接臂,先通过酰胺化反应将聚乙二醇与壳聚糖接枝,再在硫酸铜的催化下与通过模拟天然抗菌性多肽结构设计的端基被炔化抗菌性多肽(WW11)进行点击化学反应,得到抗菌肽大分子偶联物CS-PEG-WW11。该偶联物的1H-MNR谱证实WW11的接枝率为11%;TEM照片显示其在水溶液中自组装成直径约为100 nm的纳米微球;对金黄色葡萄球菌和痤疮丙酸杆菌的抑菌实验表明其抗菌性能和抗生物膜性能都比未偶联的WW11显著提升;SEM和TEM照片显示其抗菌机制是对细菌细胞膜的破坏作用;红细胞溶血实验结果表明,该偶联物在实验浓度范围内几乎不溶血,具有很好的细胞安全性。

【Abstract】 A copolymer conjugate(CS-PEG-WW11)was prepared by grafting of an azide(polyethylene glycol)Carboxylic acid to chitosan through amidation reaction firstly, and then coupling of an alkynyl-ended antibacterial peptide(WW11)with the grafted chitosan through click reaction, the antibacterial peptide with a simulating structure of natural antibacterial peptides. 1H-MNR results showed the grafting ratio of WW11 was 11%;TEM photographs showed the self-assembly structure of hydrophilic nanoparticles(at about 100 nm grain size)when the conjugate was dispersed in aqueous solution; results of antibacterial tests against the bacterium of Staphylococcus aureus and Propionibacterium acnes showed that the antibacterial property and the anti-biofilm property of the conjugate were obviously improved, compared with WW11;morphology characterization via SEM&TEM showed its antibacterial mechanism through destroying cell membrane of the bacterium; erythrocyte hemolysis test results showed its excellent cell safety.

【关键词】 抗菌肽; 壳聚糖; 偶联; 生物膜; 抗菌性;
【Key words】 Antibacterial peptide; chitosan; coupling; biofilm; antibacterial property;
  • 【文献出处】 化学研究与应用 ,Chemical Research and Application , 编辑部邮箱 ,2022年10期
  • 【分类号】R318.08;O629.72
  • 【下载频次】86
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