Moger W H
Life Sci. 1985 Sep 2;37(9):869-73. doi: 10.1016/0024-3205(85)90522-3.
To explore the mechanism of gonadotropin-releasing hormone (GnRH) action on Leydig cell steroidogenesis the effects of a GnRH analog (GnRHa) were compared to those of 12-O-tetradecanoylphorbol 13-acetate (TPA). Both compounds acutely stimulated androgen production 2-4 fold with EC50's of 9 nM (TPA) and 0.2 nM (GnRHa). The effects of TPA and GnRHa were not additive and neither compound acutely altered the luteinizing hormone (LH) concentration-response relationship. After 24 h of exposure to TPA or GnRHa the ability of LH to stimulate androgen production was impaired. The parallel effects of TPA and GnRHa on Leydig cell steroidogenesis suggest that they are acting via similar mechanisms; presumably the activation protein kinase C.
为探究促性腺激素释放激素(GnRH)对睾丸间质细胞类固醇生成作用的机制,将一种GnRH类似物(GnRHa)的作用与12 - O - 十四烷酰佛波醇13 - 乙酸酯(TPA)的作用进行了比较。两种化合物均能急性刺激雄激素生成,使其增加2 - 4倍,TPA的半数有效浓度(EC50)为9 nM,GnRHa的EC50为0.2 nM。TPA和GnRHa的作用并非相加性的,且两种化合物均未急性改变促黄体生成素(LH)浓度 - 反应关系。在暴露于TPA或GnRHa 24小时后,LH刺激雄激素生成的能力受损。TPA和GnRHa对睾丸间质细胞类固醇生成的平行作用表明它们通过相似的机制发挥作用;推测是激活蛋白激酶C。