摘要
介绍近年来通过对水飞蓟宾进行结构修饰以改进其溶解性和生物活性的研究进展。水飞蓟宾具有抗脂质过氧化、清除自由基、保护肝细胞、抗肝纤维化和免疫调节等作用,但因溶解性差、生物利用度低,其临床应用受到一定限制。故以水飞蓟宾为先导化合物合成相关衍生物,并从中筛选专一性强和活性高的化合物,已成为广受关注的研究热点。
Recent advances in the studies which is to improve its solubility and biological have revealed that silybin exhibited significant tion, cleaning up free radical, anti-hepatotoxic ever, its clinical use is limited because of the on the structure modification of silybin, the objective of activity, were reviewed in this article. The previous studies biological properties such as inhibiting of lipid peroxidaactivity, anti-hepatic fibrosis and immunoregulation. Howpoor solubility and low bioavailability. Therefore, it has become an interesting subject for researchers to use silybin as lead compound to synthesize the related derivatives for screening the new drugs which are more specific and more active for clinic applications.
出处
《药学进展》
CAS
2009年第8期360-364,共5页
Progress in Pharmaceutical Sciences
关键词
水飞蓟宾
衍生物
合成
药理活性
新药开发
silybin
derivatives
synthesis
pharmacological activity
drug development
