4种达玛烷型人参皂苷元结构改造及生物活性研究进展

Research Progress on Structural Transformations and Biological Activities of Four Dammarane-type Ginsengenins

达玛烷型人参皂苷元是人参皂苷在机体内的活性代谢产物,在抗癌、抗菌、抗炎、保护心脑系统等方面均具有独特的药理作用,已被广泛作为结构改造的研究对象。通过结构改造,可以增强达玛烷型人参皂苷元的水溶性、提高生物利用度、增强生物活性和减少毒副作用,扩大临床应用范围。近年来,通过化学方法和生物转化法对达玛烷型人参皂苷元进行结构改造及生物活性的研究取得了重要进展。其中:化学方法主要是针对分子中的羟基进行结构改造,结构改造的方法主要有酯化、酰胺化、引入含氮官能团等;生物转化法的改造位点多样化,该法具有特异性强、转化率高、微生物来源丰富的特点。本文对4种达玛烷型皂苷元的结构改造及生物活性研究进行综述,以期为人参皂苷元衍生物的设计合成与进一步开发利用以及为云南省丰富的三七资源开发与利用提供参考。

Dammarane-type ginsengenins are active metabolites of ginsenosides in body,which have unique pharmacological effects of anti-tumor,antibacterial,anti-inflammatory,and protection of heart and brain system.Structural transformations of ginsengenins have been widely conducted in order to enhance their water solubility,bioavailability,and biological activity,reduce their side effects,and expand their clinical application.In recent years,some progress has been made in the structural transformations and biological activities of dammarane-type ginsengenins.In chemical methods,modification sites are mainly focused on hydroxyl groups of the molecule.Chemical methods included esterification,amidation,and introduction of nitrogen-containing group,etc.Biotransformation method has the characteristics of high specificity,high conversion,and abundant sources of microorganism.In this paper,structural transformations and biological activities of four dammarane-type ginsengenins were reviewed,in order to provide reference for the design,synthesis,further development,and utilization of ginsenogenin derivatives,and for the development and utilization of rich Panax notoginseng resources in Yunnan Province.