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

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.