Yajima H, Komatsu M, Schermerhorn T, Aizawa T, Kaneko T, Nagai M, Sharp G W, Hashizume K
Department of Aging Medicine and Geriatrics, Shinshu University School of Medicine, Matsumoto, Japan.
Diabetes. 1999 May;48(5):1006-12. doi: 10.2337/diabetes.48.5.1006.
Cyclic AMP potentiates glucose-stimulated insulin release by actions predominantly at a site, or sites, distal to the elevation of the cytosolic free Ca2+ concentration ([Ca2+]i). Glucose also acts at a site, or sites, distal to the elevation of [Ca2+]i via the ATP-sensitive K+ channel (K+ATP channel)-independent signaling pathway. Accordingly, using rat pancreatic islets, we studied the location of the action of cAMP and its interaction with the glucose pathway. Forskolin, an activator of adenylyl cyclase, raised intracellular cAMP levels and enhanced KCl-induced (Ca2+ -stimulated) insulin release in the presence, but not in the absence, of glucose. Thus, cAMP has no direct effect on Ca2+ -stimulated insulin release. The interaction between cAMP and glucose occurs at a step distal to the elevation of [Ca2+]i because forskolin enhancement of KCl-induced insulin release, in the presence of glucose, was demonstrated in the islets treated with diazoxide, a K+ATP channel opener. The enhancement of insulin release was not associated with any increase in [Ca2+]i. Furthermore, the interaction between cAMP and glucose was unequivocally observed even under stringent Ca2+ -free conditions, indicating the Ca2+ -independent action of cAMP. This action of cAMP is physiologically relevant, because not only forskolin but also glucagon-like peptide 1, glucose-dependent insulinotropic polypeptide, and pituitary adenylyl cyclase activating polypeptide exerted similar actions. In conclusion, the cAMP/protein kinase A pathway has no direct effect on Ca2+ -stimulated insulin exocytosis. Rather, it strongly potentiates insulin release by increasing the effectiveness of the K+ATP channel-independent action of glucose.
环磷酸腺苷(cAMP)主要通过作用于胞质游离钙离子浓度([Ca2+]i)升高位点的远端来增强葡萄糖刺激的胰岛素释放。葡萄糖也通过不依赖于ATP敏感性钾通道(K+ATP通道)的信号通路作用于[Ca2+]i升高位点的远端。因此,我们使用大鼠胰岛研究了cAMP的作用位点及其与葡萄糖信号通路的相互作用。腺苷酸环化酶激活剂福斯可林在有葡萄糖存在而非无葡萄糖时,可提高细胞内cAMP水平并增强氯化钾诱导(钙离子刺激型)的胰岛素释放。因此,cAMP对钙离子刺激型胰岛素释放无直接作用效应。cAMP与葡萄糖之间的相互作用发生在[Ca2+]i升高位点的远端,因为在使用K+ATP通道开放剂二氮嗪处理的胰岛中,已证实福斯可林在有葡萄糖存在时可增强氯化钾诱导的胰岛素释放。胰岛素释放增强并未伴随[Ca2+]i的任何升高。此外即使在严格不含钙离子的条件下,也明确观察到了cAMP与葡萄糖之间的相互作用,这表明cAMP的作用不依赖于钙离子。cAMP的这一作用具有生理相关性,因为不仅福斯可林,胰高血糖素样肽1、葡萄糖依赖性促胰岛素多肽和垂体腺苷酸环化酶激活多肽也发挥了类似作用。总之,cAMP/蛋白激酶A信号通路对钙离子刺激型胰岛素胞吐作用无直接作用效应。相反,它通过提高葡萄糖不依赖于K+ATP通道作用的有效性来强烈增强胰岛素释放。