Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
5158247 | European Journal of Medicinal Chemistry | 2017 | 62 Pages |
Abstract
A series of novel berberine derivatives, as AMPK indirect activators, was designed, synthesized, and biologically evaluated for their anti-diabetic activity. Optimized compound 4bq stimulated glucose consumption (2.2-fold) in L6 myotubes, reduced hepatocytes gluconeogenesis (by 85%) and improved pharmacokinetic profiles (bioavailability 45%) compared to berberine. In a db/db mice model compound 4bq lowered fasting blood glucose at a dose of 120 mg/kg/day, and compound 4bq exhibited no obvious hERG inhibition (IC50 > 10 μM).159
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Authors
Shengbin Zhou, Yanan Duan, Jiang Wang, Jin Zhang, Haifeng Sun, Haowen Jiang, Zhanni Gu, Junhua Tong, Jingya Li, Jia Li, Hong Liu,