Stimulation by forskolin of the thyroid adenylate cyclase, cyclic amp accumulation and iodine metabolism
Stimulation by forskolin of the thyroid adenylate cyclase, cyclic amp accumulation and iodine metabolism
复制标题
毛喉素刺激甲状腺腺苷酸环化酶、循环放大器积累和碘代谢
DOI：
10.1016/0303-7207(83)90009-6
复制
发表时间：
1983
影响因子：
4.1
通讯作者：
J. Dumont
中科院分区：
文献类型：
--
作者：
J. Sande;P. Cochaux;J. Mockel;J. Dumont
Forskolin 是一种二萜降血压药物，可激活大脑和其他一些组织中的腺苷酸环化酶（Seamon 等，1981）。 Forskolin 激活颗粒制剂中的腺苷酸环化酶，并增强狗甲状腺切片中环 AMP 的积累。这些影响在几分钟内达到最大，并且随后保持恒定。毛喉素对完整细胞的作用在洗涤后迅速消失。它再现了两种已知的环 AMP 介导的 TSH 效应：分泌激活和蛋白质碘化激活。因此，毛喉素为研究甲状腺细胞中环 AMP 水平的特定升高的作用提供了一个非常方便的工具。 Mn2+ 不会降低毛喉素对腺苷酸环化酶的激活作用，从而解开 TSH 和 PGE1 的作用。这表明，毛喉素在甲状腺中的作用也超出了受体水平。毛喉素对环 AMP 积累的作用受到甲状腺、乙酰胆碱、碘化物、去甲肾上腺素、PGF1α 和腺苷中已知的该系统负调节因子的抑制。另一方面，毛喉素增强了 TSH、PGE 和霍乱毒素的作用。这些数据表明，虽然毛喉素的作用不需要受体，但它不会将它们与腺苷酸环化酶的催化单元解偶联。
Forskolin, a diterpene hypotensive drug, activates adenylate cyclase in brain and in some other tissues (Seamon et al., 1981). Forskolin activated adenylate cyclase in particulate preparations and enhanced cyclic AMP accumulation in slices of dog thyroid. These effects were maximal within minutes and remained constant afterwards. The action of forskolin on intact cells disappeared rapidly after washing. It reproduced two known cyclic AMP-mediated TSH effects: the activation of secretion and of protein iodination. Forskolin thus provides a very convenient tool for the study of the action of defined elevations of cyclic AMP level in thyroid cells. The activation by forskolin of adenylate cyclase was not reduced by Mn2+which uncouples TSH and PGE1action. This suggests that in the thyroid also, forskolin acts beyond the receptor level. The effect of forskolin on cyclic AMP accumulation was inhibited by the known negative regulators of this system in the thyroid, acetylcholine, iodide, norepinephrine, PGF1αand adenosine. On the other hand, forskolin potentiated the effects of TSH, PGE, and cholera toxin. These data show that, though it does not require the receptors for its action, forskolin does not uncouple them from the catalytic unit of adenylate cyclase.