Stengel D, Guenet L, Desmier M, Insel P, Hanoune J
Mol Cell Endocrinol. 1982 Nov-Dec;28(3):681-90. doi: 10.1016/0303-7207(82)90155-1.
Forskolin, a natural diterpene, is a novel, potent activator of a variety of adenylate cyclase systems; its mechanism and site of action are still disputed. We report here that, while forskolin activates liver adenylate cyclase up to 15-fold, it does not activate cyclase of ram sperm which comprises a pure catalytic subunit. However, forskolin activation of sperm adenylate cyclase activity could be observed after reconstitution with the regulatory component-enriched membrane from human erythrocytes. The diterpene weakly (3-5-fold) activated the cytosolic, soluble cyclase found in rat and ram tests, but this effect was lost when the cyclase was purified by gel chromatography. Our data are not compatible with the hypothesis that forskolin acts directly on the catalytic subunit, but rather suggest that it acts via another regulatory component, part of, or different from, the GTP-binding regulatory complex.
福斯高林是一种天然二萜，是多种腺苷酸环化酶系统的新型强效激活剂；其作用机制和作用位点仍存在争议。我们在此报告，虽然福斯高林可将肝脏腺苷酸环化酶的活性激活至15倍，但它不会激活由纯催化亚基组成的公羊精子的环化酶。然而，在用富含调节成分的人红细胞膜进行重组后，可以观察到福斯高林对精子腺苷酸环化酶活性的激活作用。该二萜对大鼠和公羊睾丸中的胞质可溶性环化酶有较弱的激活作用（3至5倍），但当通过凝胶色谱法纯化环化酶时，这种作用就消失了。我们的数据与福斯高林直接作用于催化亚基的假设不相符，而是表明它通过另一种调节成分起作用，该调节成分是GTP结合调节复合物的一部分或与之不同。
