Study on hypoglycemic activity of 9-substituted berberine derivatives in vitro
10.16438/j.0513-4870.2017-0040
- VernacularTitle:9-取代小檗碱类似物的体外降糖活性研究
- Author:
Gang REN
1
;
Ming-rui ZHANG
2
;
Dan-qing SONG
1
;
Jian-dong JIANG
1
;
Ying-hong LI
1
Author Information
1. Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China
2. School of Life Science, Liaoning Normal University, Dalian 116081, China
- Publication Type:ORIGINAL ARTICLES
- Keywords:
berberine analogues;
glucose consumption;
synthesis
- From:
Acta Pharmaceutica Sinica
2017;52(8):1282-1286
- CountryChina
- Language:Chinese
-
Abstract:
The glucose consumption activity of 9-substitued analogues of berberine was evaluated in L6 myotubes. It was found that the introduction of an ethoxy group on the 9-position of berberine was beneficial for the activity. 9-Ethoxy berberine analogue 2a exhibited superior activity to berberine in multiple dose levels, and the activity of 2a was 5.4 times as high as that of berberine at the dose of 1.25 μmol·L-1. At the meantime, the potency on AMPK activation of 2a was 2.8 times of that of berberine at the dose of 10 μmol·L-1. Therefore, the compound 2a is a promising scaffold for further modification.
