Schorderet-Slatkine S, Baulieu E E
Endocrinology. 1982 Oct;111(4):1385-7. doi: 10.1210/endo-111-4-1385.
The diterpene, forskolin, is a potent and reversible inhibitor of progesterone-induced meiosis in Xenopus laevis oocytes (ED50 of inhibition approximately 3 microM). Forskolin alone increases cAMP concentration in oocytes, but, unlike with cholera toxin treatment, there is no lag phase, and reversibility is obtained by washing the cells. Progesterone decreases the forskolin effect on cAMP accumulation, but cAMP concentration remains above the level observed in oocytes treated with progesterone alone. The data corroborate the previously-established antagonistic effect of cAMP on progesterone-induced meiosis. Preliminary experiments in the presence of a phosphodiesterase inhibitor suggest that, as in other biological systems, forskolin is an activator of adenylate cyclase in xenopus laevis oocytes. Contrary to what is observed when forskolin is present in the incubation medium, no effect of the diterpene is recorded after its injection into oocytes, evoking a site of action at the external side of the membrane.
二萜类化合物毛喉素是非洲爪蟾卵母细胞中孕酮诱导减数分裂的一种强效可逆抑制剂(抑制作用的半数有效浓度约为3微摩尔)。单独使用毛喉素可增加卵母细胞中的环磷酸腺苷(cAMP)浓度,但与霍乱毒素处理不同的是,不存在延迟期,通过洗涤细胞可实现可逆性。孕酮会降低毛喉素对cAMP积累的影响,但cAMP浓度仍高于仅用孕酮处理的卵母细胞中观察到的水平。这些数据证实了此前确立的cAMP对孕酮诱导减数分裂的拮抗作用。在存在磷酸二酯酶抑制剂的情况下进行的初步实验表明,与其他生物系统一样,毛喉素是非洲爪蟾卵母细胞中腺苷酸环化酶的激活剂。与在孵育培养基中存在毛喉素时观察到的情况相反,将该二萜类化合物注射到卵母细胞后未记录到其作用,这表明其作用位点在细胞膜外侧。