水飞蓟宾类黄酮木质素衍生物的研究进展

Silybin-derived flavonolignans and their structure-activity relationships:research advances

水飞蓟是多国药典收载的天然药物,具有抗氧化、抗纤维化、抗炎、免疫调节以及肝细胞再生作用,临床用于治疗肝炎、脂肪肝、肝硬化、缺血性损伤、辐射损伤等。近期随着水飞蓟宾以抗肿瘤新药进入Ⅱ期临床试验,对其衍生物、构效关系以及抗氧化机制等的研究进入加速阶段。本文综述了近年来水飞蓟宾和脱氢水飞蓟宾的近百种衍生物及其活性研究结果 ,并对该类黄酮木质素类化合物今后的发展和设计研究状况做一概述。

Silybum marianum （L.） Gaertn. is recorded by the pharmacopoeias of many countries to have such bioactivities as antioxidant,anti-hepatocirrhosis,anti-inflammation,immunomodulation and liver regeneration. It has been used clinically to treat hepatitis,fatty liver,liver cirrhosis,ischemic damage,radiation injury,etc. With silybin entering the phase Ⅱ clinical trial as an anti-cancer drug,its correlative investigations including derivatives preparation,structure-activity relationship （SAR） detection,and the detailed action mechanisms have been developing rapidly. Recently,the new synthetic stra-tegy of silybin and dehydrosilybin （DHS） along with their anti-HSV （herpes simple virus） activity has also been reported. This paper reviews about one hundred preparative derivatives of silybin and DHS which appeared in recent years,with the emphasis on their pharmacological activity and the results of their SAR. The future development direction of structural modification of silybin and DHS is also discussed and predicted.