丹参素结构中醇羟基的修饰与初步活性评价

目的设计合成系列在丹参素醇羟基部位修饰的新衍生物，初步探索醇羟基在丹参素生物活性中的作用。方法丹参素的酚羟基以及羧基经苄基保护后，其醇羟基与相应的基团在不同的催化剂下缩合生成醚键以及酯键化合物，然后脱除保护基得到醇羟基修饰的衍生物。通过体外的心肌细胞氧化损伤模型初步评价新衍生物的生物活性，分析其构效关系。结果合成了11个丹参素新衍生物，并进行了结构确证；活性实验显示，醇羟基上醚键与酯键修饰的衍生物活性均没有明显高于母药丹参素。结论裸露的醇羟基可能是丹参素发挥作用的必需基团。

Synthesis and preliminary evaluation of Danshensu derivatives modified at hydroxyl group

Objective To design and synthesize Danshensu derivatives to study the role of hydroxyl group in Danshensu＇s bio- activity. Methods The phenolic and carboxyl groups of Danshensu were protected by benzyl, and then the hydroxyl group underwent reaction with different catalysts to get hydroxyl modified derivatives through ether and ester bonds, then benzyl groups were removed to get target derivatives. These derivatives were evaluated in H9c2 cells against tea-butyl hydroperoxide induced injury to illustrate the structure-activity relationship. Results Eleven derivatives were synthesized, and their structures were confirmed by MS, NMR and el- emental analysis. Biological results showed that neither ether nor ester derivatives showed better anti-oxidative effects than Danshensu. Conclusion The free hydroxyl group may he necessary for Danshensu＇s activity.