Forskolin as an activator of cyclic AMP accumulation and lipolysis in rat adipocytes.
Forskolin as an activator of cyclic AMP accumulation and lipolysis in rat adipocytes.
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DOI：
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发表时间：
1982-07
影响因子：
3.6
通讯作者：
I. Litosch;T. Hudson;I. Mills;S. Li;J. Fain
中科院分区：
文献类型：
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作者：
I. Litosch;T. Hudson;I. Mills;S. Li;J. Fain
毛喉素增加了环磷酸腺苷在离体脂肪细胞中的积累，并显着增强环磷酸腺苷的升高，由于异丙肾上腺素。在脂肪细胞膜中，毛喉素刺激腺苷酸环化酶活性的浓度为0.1 μ M或更高。毛喉素不影响EC 50激活腺苷酸环化酶，但增加异丙肾上腺素的最大效果。无论是可溶性或颗粒性低Km环AMP磷酸二酯酶活性的影响，毛喉素。低浓度的毛喉素（0.1-1.0 μ M），这显着提高环AMP水平，并没有增加脂解，而类似的增加环AMP水平由于异丙肾上腺素提高脂解。毛喉素不抑制环腺苷酸依赖性蛋白激酶激活的三酰甘油脂肪酶或随后的三酰甘油水解。较高浓度的毛喉素（10-100 μ M）确实增加了脂解。由于毛喉素增加的环腺苷酸的生产和脂解被抑制的抗脂解剂胰岛素和N6-（苯基异丙基）腺苷。甲状腺功能减退症降低了毛喉素刺激环磷酸腺苷产生和脂解的能力。这些结果表明，毛喉素通过激活腺苷酸环化酶增加脂肪细胞中环AMP的产生。脂解被毛喉素激活，但总环AMP浓度高于儿茶酚胺。
Forskolin increased cyclic AMP accumulation in isolated adipocytes and markedly potentiated the elevation of cyclic AMP due to isoproterenol. In adipocyte membranes, forskolin stimulated adenylate cyclase activity at concentrations of 0.1 microM or greater. Forskolin did not affect the EC50 for activation of adenylate cyclase but did increase the maximal effect of isoproterenol. Neither the soluble nor particulate low-Km cyclic AMP phosphodiesterase activity was affected by forskolin. Low concentrations of forskolin (0.1-1.0 microM), which significantly elevated cyclic AMP levels, did not increase lipolysis, whereas similar increases in cyclic AMP levels due to isoproterenol elevated lipolysis. Forskolin did not inhibit the activation of triacylglycerol lipase by cyclic AMP-dependent protein kinase or the subsequent hydrolysis of triacylglycerol. Higher concentrations of forskolin (10-100 microM) did increase lipolysis. Both the increased cyclic AMP production and lipolysis due to forskolin were inhibited by the antilipolytic agents insulin and N6-(phenylisopropyl)adenosine. Hypothyroidism reduced the ability of forskolin to stimulate cyclic AMP production and lipolysis. These results indicate that forskolin increases cyclic AMP production in adipocytes through an activation of adenylate cyclase. Lipolysis is activated by forskolin but at higher concentrations of total cyclic AMP than for catecholamines.