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目的为了改善绿原酸的溶解性、脂水分配系数等性质,设计合成系列绿原酸酰胺衍生物进行生物活性评价。方法以绿原酸为原料,先对邻二醇结构保护,再与胺发生缩合反应,然后脱保护,最后得到目标化合物。分别采用MTT法与DPPH法对目标物进行体外抗肿瘤增殖活性与抗氧化活性评价。结果合成了8个绿原酸酰胺衍生物,通过IR、NMR进行了结构确定。活性测试表明,目标物有体外对肿瘤细胞抗增殖活性,部分化合物的活性略高于绿原酸;同时目标物抗氧化活性与绿原酸相当。结论修饰后的绿原酸酰胺衍生物仍有抗肿瘤与抗氧化活性。
In order to improve the solubility of chlorogenic acid, lipid-water partition coefficient and other properties, a series of chlorogenic acid amide derivatives were designed and synthesized for bioactivity evaluation. Methods Starting from chlorogenic acid, the structure of vicinal diol was first protected and then condensed with amine, then deprotected. Finally, the target compound was obtained. The anti-tumor activity and anti-oxidative activity of the target substance in vitro were evaluated by MTT assay and DPPH assay respectively. Results Eight chlorogenic acid amide derivatives were synthesized and their structures were confirmed by IR and NMR. Activity tests showed that the target anti-proliferative activity of tumor cells in vitro, some compounds activity slightly higher than the chlorogenic acid; the same time, the target antioxidant activity and chlorogenic acid equivalent. Conclusion The modified chlorogenic acid amide derivatives still have anti-tumor and anti-oxidation activities.