Effects of efaroxan on insulin release from pancreatic βcells
10.3969/j.issn.1001-1978.2015.04.017
- VernacularTitle:Efaroxan对胰岛素分泌的调控机制研究
- Author:
Yi ZHANG
;
Yunfeng LIU
;
Jingying GAO
;
Yaqin DING
- Publication Type:Journal Article
- Keywords:
Efaroxan;
insulin;
cAMP;
KU1 4R;
signal transduction;
islet function
- From:
Chinese Pharmacological Bulletin
2015;(4):524-526,527
- CountryChina
- Language:Chinese
-
Abstract:
Aim To study the insulinotropic effects of Efaroxan and the underlying mechanism in rat βcells. Methods Pancreatic islets were isolated by college-nase p digestion.Radioimmunoassay was used to meas-ure insulin secretion and cAMP level in rat pancreatic islets.Results Efaroxan only potentiated insulin se-cretion at high glucose concentrations(8.3,1 1 .1 mmol ·L -1 )but not at low glucose concentrations.KU1 4R,an antagonist of Efaroxan,remarkably inhibited Efarox-an-potentiated insulin secretion;and similarly,KU1 4R significantly inhibited forskolin-induced and IBMX-in-duced insulin secretion.cAMP measurement showed that forskolin and IBMX significantly increased cAMP levels,but Efaroxan and KU1 4R had no effects on cAMP content in pancreatic islets.Conclusion The mechanism of Efaroxan-potentiated insulin secretion is related to downstream of cAMP signaling pathway, KU1 4R antagonized the downstream of cAMP signaling leading to its inhibitory effects on Efaroxan,forskolin and IBMX-induced insulin secretion.
