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Engineering a novel antibacterial agent with multifunction: Protocatechuic acid-grafted-quaternized chitosan
Carbohydrate Polymers ( IF 10.7 ) Pub Date : 2021-01-22 , DOI: 10.1016/j.carbpol.2021.117683
Chen Zhou , Hai-Yong Ao , Xiao Han , Wen-Wen Jiang , Zhi-Fei Yang , Le Ma , Xiao-Yan Deng , Yi-Zao Wan

As a mild cationic antibacterial agent, hydroxypropyltrimethyl ammonium chloride chitosan (HACC) could kill gram-positive bacteria and gram-positive drug-resistant bacteria without cytotoxicity. Nevertheless, it was not effective against gram-negative bacteria. Herein, protocatechuic acid (PA) with broad-spectrum antibacterial properties and pharmacological activities was grafted on HACC. PA-g-HACC showed favourable antioxidant capacity and anti-inflammatory properties. Most importantly, the results of antibacterial assay indicated that the antibacterial rates of all PA-g-HACC groups against Staphylococcus aureus (S. aureus) and methicillin-resistant Staphylococcus aureus (MRSA) were above 92 %, and the antibacterial rate of PA-g-HACC against E. coli was increased with the amount of grafted PA. Furthermore, the cytocompatibility of PA-g-HACC was improved by appropriate grafting ratio of PA, while excessive grafted PA can lead to toxicity. We believe that PA-g-HACC in optimum grafting ratio of PA with favorable antibacterial properties, pharmacological activities and cytocompatibility will be potential antibacterial agent for treating infections.



中文翻译:

设计具有多功能的新型抗菌剂:原儿茶酸接枝季铵化壳聚糖

羟丙基三甲基氯化铵壳聚糖(HACC)作为一种温和的阳离子抗菌剂,可以杀死革兰氏阳性菌和革兰氏阳性耐药菌而无细胞毒性。但是,它对革兰氏阴性菌无效。在此,将具有广谱抗菌特性和药理活性的原儿茶酸(PA)嫁接到HACC上。PA-g-HACC显示出良好的抗氧化能力和抗炎特性。最重要的是,抗菌测定的结果表明,所有PA-g-HACC组对金黄色葡萄球菌S. aureus)和耐甲氧西林的金黄色葡萄球菌MRSA)的抗菌率)大于92%,并且PA-g-HACC对大肠杆菌的抗菌率随PA含量的增加而增加。此外,通过适当的PA接枝率可以改善PA-g-HACC的细胞相容性,而过量的PA接枝会导致毒性。我们认为,以最佳的PA接枝率具有良好的抗菌性能,药理活性和细胞相容性的PA-g-HACC将成为治疗感染的潜在抗菌剂。

更新日期:2021-01-28
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