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目的:观察 Efaroxan 的促胰岛素分泌作用特点,并探讨其相关作用机制。方法应用放免法测定不同条件下Efaroxan 对大鼠胰岛素分泌的影响。cAMP 放射免疫试剂盒测定胰岛细胞内 cAMP 含量。结果Efaroxan 促进胰岛素分泌作用具有葡萄糖浓度依赖性,其特点是在高浓度葡萄糖条件下(8.3、11.1 mmol·L -1)增强胰岛素分泌,而在低浓度葡萄糖条件下(0、2.8 mmol·L -1)则没有作用。Efaroxan 的拮抗剂 KU14R 可明显抑制 Efaroxan 对胰岛素分泌的促进作用,并明显的抑制了 forskolin 和 IBMX 对胰岛素分泌的促进作用。胰岛 cAMP 含量检测发现,forskolin 和 IBMX 明显增加了胰岛细胞 cAMP 含量,但是 Efaroxan 和 KU14R 对胰岛cAMP 含量没有影响。结论Efaroxan 促进胰岛素分泌作用与激动 cAMP 下游信号通路有关,KU14R 通过阻断 cAMP 下游信号转导通路发挥抑制 Efaroxan、forskolin 和 IBMX 的促胰岛素分泌作用。“,”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.