绿原酸缀合物HA-CGA的抗菌活性研究

Study on antibacterial activity of chlorogenic acid conjugate HA-CGA

目的合成透明质酸(HA)-绿原酸(CGA)的水溶性缀合物HA-CGA并对其结构进行表征,并比较该缀合物与单体药物CGA的抗菌活性。方法将HA溶于水中,用1-乙基-(3-二甲基氨基丙基)碳二亚胺盐酸盐(EDC·HCl)将其活化,然后加入溶于DMF的CGA进行酯化反应,最后将反应溶液在水中透析除杂,冻干,得到缀合物HA-CGA,并采用核磁共振氢谱法、红外光谱法对HA-CGA结构进行表征;采用平板计数法来比较CGA和HA-CGA对大肠埃希菌、金黄色葡萄球菌等2种细菌的抑制作用。结果CGA和HA-CGA对2种细菌均有不同程度的抑制作用,其中HA-CGA抗菌活性强于CGA。结论通过HA对CGA的结构进行修饰,增加了CGA的水溶性,进一步提高了CGA的抗菌性能。

Objective To synthesize and characterize the water-soluble conjugate of hyaluronic acid(HA)-chlorogenic acid(CGA)(HA-CGA),and to compare the antibacterial activity of the conjugate with that of the free drug CGA.Methods HA was dissolved in water,activated by 1-ethyl-(3-dimethylaminopropyl)carbodiimide hydrochloride(EDC·HCl),and followed by the addition of a solution of CGA dissolved in DMF for esterification reaction.Finally,the reaction solution was dialyzed in water to remove impurities and then lyophilized to obtain the conjugate HA-CGA.The structure of HA-CGA was characterized by nuclear magnetic resonance spectroscopy(1H NMR)and infrared spectroscopy(FT-IR).The inhibitory effects of CGA and HA-CGA on Escherichia coli and Staphylococcus aureus were compared by the plate counting method.Results CGA and HA-CGA had different inhibitory effects on the two bacteria,and the antibacterial activity of HA-CGA was stronger than that of CGA.Conclusion By modifying the structure of CGA with HA,the water solubility of CGA was increased and its antibacterial activity was further improved.