表没食子儿茶素没食子酸酯的化学修饰及生物活性研究进展

Research progress on chemical modification and biological activities of epigallocatechin gallate

中文关键词:  表没食子儿茶素没食子酸酯  结构修饰  衍生物  生物活性  功能性食品

英文关键词:epigallocatechin gallate  structural modification  derivatives  biological activity  functional food

中文摘要:

      表没食子儿茶素没食子酸酯(epigallocatechin gallate, EGCG)是茶叶中的一种重要儿茶素, 具有良好的生物活性, 但口服生物利用度低、脂溶性及稳定性差等缺点使其在功能性健康产品开发中的应用受到限制。研究发现, 通过醚化、酯化和糖苷化等化学修饰方法, 在EGCG结构中引入烷基、酰基、糖基等基团可得到不同EGCG衍生物, 显著改善EGCG的理化性质, 并特异性增强EGCG的抗氧化、抗炎、抗病毒、抗衰老、抗癌等生物活性。醚化修饰的操作简便, 但产物复杂、不利于后续的分离纯化; 酯化修饰的研究多集中在小分子试剂上; 糖苷化修饰的合成技术难度较高, 但是该修饰方法可定向制备目标产物。本文对近几年EGCG化学修饰的常见方法及EGCG衍生物的活性研究进行了系统的总结, 为EGCG的构效关系研究及开发EGCG类功能性健康产品提供参考。

英文摘要:

      Epigallocatechin gallate (EGCG) is an important catechin in tea, which has a wide range of biological activities. However, its application in functional health product development is limited due to its low oral bioavailability, poor lipid solubility and stability. It has found that different EGCG derivatives could be obtained by introducing alkyl, acyl and sugar groups into the structure of EGCG through chemical modification methods such as etherification, esterification and glycosidation, which can significantly improve the physical and chemical properties of EGCG and specifically enhance the antioxidant, anti-inflammatory, antiviral, anti-aging and anti-cancer biological activities of EGCG. The operation of etherification modification is simple, but the product is complex, which is not conducive to the subsequent separation and purification. The research of esterification modification is mainly focused on small molecule reagents. The synthesis of glycosidation modification is technically difficult, but the modification method can be directed to prepare the target products. This review summarized the common methods of EGCG chemical modification and the activities of EGCG derivatives, which provides a guideline for the studies of EGCG structure-activity relationship of and the development of related functional health products.