Galas M C, Harden T K
Department of Pharmacology, School of Medicine, University of North Carolina, Chapel Hill 27599, USA.
Eur J Pharmacol. 1996 Oct 24;314(1-2):157-64. doi: 10.1016/s0014-2999(96)00524-9.
The interaction of the cyclic AMP and inositol lipid signalling systems was studied in turkey erythrocytes. Elevation of intracellular cyclic AMP concentrations by pretreatment of the cells with forskolin or 8-Br-cAMP resulted in a marked decrease in responsiveness of phospholipase C to G-protein activators in membranes prepared from treated cells. Decreases in responsiveness occurred with a t1/2 of approximately 5 min and were reversible after transfer of desensitized cells to drug-free medium. Pretreatment of the cells with forskolin inhibited inositol phosphate formation in a concentration-dependent manner and addition of the phosphodiesterase inhibitor IBMX 93-isobutyl-1-methylxanthine) during pretreatment increased the capacity of forskolin to desensitize phospholipase C activity. IBMX also produced a similar potentiation of forskolin-stimulated accumulation of cyclic AMP in turkey erythrocytes. Isoproterenol pretreatment of the cells induced, like forskolin, partial inhibition of inositol phosphate generation in response to G-protein activators and to P2y purinoceptor and beta-adrenoceptor agonists. The capacity of isoproterenol to induce desensitization of phospholipase C activity also was increased by the presence of IBMX during pretreatment of the cells. H8 (N-[2-(methylamino)ethyl]-5-isoquinoline-sulfonamide), an inhibitor of cyclic AMP-regulated protein kinase, completely prevented forskolin-induced desensitization but only partially blocked isoproterenol-induced desensitization. These results indicate that the cyclic AMP signalling cascade has a major inhibitory influence on receptor- and G-protein-activated inositol lipid signaling.
在火鸡红细胞中研究了环磷酸腺苷(cAMP)和肌醇脂质信号系统的相互作用。用福斯可林或8-溴-cAMP预处理细胞,使细胞内cAMP浓度升高,导致从处理过的细胞制备的膜中磷脂酶C对G蛋白激活剂的反应性显著降低。反应性降低的半衰期约为5分钟,将脱敏细胞转移到无药物培养基后,反应性可恢复。用福斯可林预处理细胞以浓度依赖的方式抑制肌醇磷酸的形成,在预处理期间添加磷酸二酯酶抑制剂异丁基甲基黄嘌呤(IBMX)可增加福斯可林使磷脂酶C活性脱敏的能力。IBMX在火鸡红细胞中也对福斯可林刺激的cAMP积累产生类似的增强作用。用异丙肾上腺素预处理细胞,与福斯可林一样,可部分抑制对G蛋白激活剂、P2y嘌呤受体和β-肾上腺素能受体激动剂的肌醇磷酸生成。在细胞预处理期间存在IBMX时,异丙肾上腺素诱导磷脂酶C活性脱敏的能力也增强。H8(N-[2-(甲氨基)乙基]-5-异喹啉磺酰胺),一种环磷酸腺苷调节蛋白激酶的抑制剂,完全阻止了福斯可林诱导的脱敏,但仅部分阻断了异丙肾上腺素诱导的脱敏。这些结果表明,环磷酸腺苷信号级联对受体和G蛋白激活的肌醇脂质信号有主要的抑制作用。