交易激励
化学
区域选择性
葡萄糖激酶
兴奋剂
水飞蓟
药理学
立体化学
生物化学
酶
受体
生物
医学
转录因子
基因
传统医学
催化作用
作者
Zhipeng Zhang,Meng Yang,Wei Zhan,Mei Yu,Shite Gao,Yue-Jiao Wu,S. X. Du
出处
期刊:ACS omega
[American Chemical Society]
日期:2022-01-20
卷期号:7 (4): 3812-3822
被引量:1
标识
DOI:10.1021/acsomega.1c06778
摘要
Glucokinase (GK) and PPARγ are important targets for antidiabetic use. Silybin is one of the major active ingredients of Silybum marianum. The regioselective modification of the five hydroxyl groups in the silybin structure has always been a challenge. In this study, we found that silybin was an agonist of GK and PPARγ. A novel synthesis scheme of silybin derivatives was designed, and a series of novel silybin derivatives has been synthesized. The derivative 8d showed relatively strong activation activity for GK and PPARγ in enzyme activity and transactivation assays (GK activation fold: 1.86; PPARγ transactivation activation percentage: 90.32%). This research suggests that silybin and its derivatives could be used as novel GK and PPARγ dual-target agonists.
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