水飞蓟宾及其类似物的化学修饰研究进展

Advances in Chemical Modification of Silybin and Its Analogues

以天然黄酮类化合物为活性先导物,研究其化学结构与生物活性的关系,进而进行化学修饰研究,是目前创新药物的一条重要思路。药用植物水飞蓟用来治疗肝胆疾病已有2000多年的历史,水飞蓟宾作为水飞蓟素的主要活性成分具有保肝、抗炎和抗癌等活性而备受人们关注,但由于水飞蓟宾极低的溶解性极大地限制了其生物利用度。为此,国内外学者通过化学和物理等方法对其进行修饰和改造,并取得了一定的成果。本文就近10年来水飞蓟宾及其类似物的化学修饰研究进行综述。

On the basis of flavonoid lead compounds with biological activity,studying the relationship between structures and bioavailability and modifying their structures is an important means of innovation of new drugs.Silybum marianum（L.） Gaertn.has been used for more than 2000 years to treat liver and gallbladder disorders.Silybin,derived from the milk thistle plant,has received considerable attention due to its hepatoprotective,anti-inflammatory and anticancer effects,however,the bioavailability and therapeutic efficiency of silybin is rather limited by its very low solubility.To solve this problem,silybin is modified or altered via various chemical and physical methods by domestic and foreign scholars,and have obtained a certain achievement.In this paper,the chemical modification of silybin and its analogues in recent years are reviewed.