Malaisse W J, Garcia-Morales P, Dufrane S P, Sener A, Valverde I
Endocrinology. 1984 Nov;115(5):2015-20. doi: 10.1210/endo-115-5-2015.
Forskolin activated adenylate cyclase in rat islet homogenates and stimulated cAMP production in intact islets incubated in the absence or presence of either D-glucose or Ca2+. Forskolin failed to affect D-[U-14C]glucose oxidation, glucose-stimulated net 45Ca uptake, or basal insulin release, but enhanced insulin secretion evoked by either nutrients (D-glucose, 2-ketoisocaproate, L-leucine alone or in combination with L-glutamine), or nonnutrient secretagogues (12-O-tetradecanoylphorbol-13-acetate, Ba2+ alone or in combination with theophylline). Forskolin stimulated insulin release from islets incubated in the presence of glucose but in the absence of Ca2+. These findings confirm that a marked increase in cAMP production is not sufficient to cause sustained insulin release. They also suggest that the enhancing action of endogenous cAMP upon insulin release does not depend on a facilitation of Ca2+ influx into islet cells.
福斯高林可激活大鼠胰岛匀浆中的腺苷酸环化酶,并在无或有D-葡萄糖或Ca2+存在的情况下刺激完整胰岛中cAMP的产生。福斯高林未能影响D-[U-14C]葡萄糖氧化、葡萄糖刺激的净45Ca摄取或基础胰岛素释放,但增强了由营养物质(D-葡萄糖、2-酮异己酸、单独或与L-谷氨酰胺联合的L-亮氨酸)或非营养性促分泌剂(12-O-十四烷酰佛波醇-13-乙酸酯、单独或与茶碱联合的Ba2+)引起的胰岛素分泌。福斯高林刺激了在有葡萄糖但无Ca2+存在的情况下孵育的胰岛释放胰岛素。这些发现证实,cAMP产生的显著增加不足以引起持续的胰岛素释放。它们还表明,内源性cAMP对胰岛素释放的增强作用不依赖于促进Ca2+流入胰岛细胞。