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工程化具有多功能的新型抗菌剂:原儿茶酸接枝季铵化壳聚糖。

Engineering a novel antibacterial agent with multifunction: Protocatechuic acid-grafted-quaternized chitosan.

机构信息

Jiangxi Key Laboratory of Nanobiomaterials & Institute of Advanced Materials, East China Jiaotong University, Nanchang 330000, China.

Jiangxi Key Laboratory of Nanobiomaterials & Institute of Advanced Materials, East China Jiaotong University, Nanchang 330000, China.

出版信息

Carbohydr Polym. 2021 Apr 15;258:117683. doi: 10.1016/j.carbpol.2021.117683. Epub 2021 Jan 22.

DOI:10.1016/j.carbpol.2021.117683
PMID:33593556
Abstract

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.

摘要

作为一种温和的阳离子型抗菌剂,羟丙基三甲基氯化铵壳聚糖(HACC)能够杀灭革兰氏阳性菌和革兰氏阳性耐药菌,同时无细胞毒性。然而,它对革兰氏阴性菌无效。在此,将具有广谱抗菌性能和药理活性的原儿茶酸(PA)接枝到 HACC 上。PA-g-HACC 表现出良好的抗氧化能力和抗炎性能。最重要的是,抗菌实验结果表明,所有 PA-g-HACC 组对金黄色葡萄球菌(S. aureus)和耐甲氧西林金黄色葡萄球菌(MRSA)的抑菌率均在 92%以上,且随着接枝 PA 量的增加,PA-g-HACC 对大肠杆菌的抑菌率也有所提高。此外,通过适当的 PA 接枝比,可以提高 PA-g-HACC 的细胞相容性,而过量的接枝 PA 会导致毒性。我们相信,具有最佳 PA 接枝比、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。

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