Vladusic E A, Bussmann L E, Visconti P E, Stoka A M, Rodriguez J B, Gros E G, Charreau E H
Instituto de Biología y Medicina Experimental (IBYME)-CONICET, Buenos Aires, Argentina.
J Steroid Biochem Mol Biol. 1994 Aug;50(3-4):181-7. doi: 10.1016/0960-0760(94)90027-2.
The effects of juvenile hormone-III (JH-III) and the JH analogue 2-(4-phenoxyphenoxy)-ethoxyte-trahydropiran on testicular steroidogenesis were studied. By using cultured MA-10 Leydig tumor cells as a model, these compounds were found to be potent inhibitors of LH/hCG steroidogenic action in a dose-dependent manner. Scatchard plot analysis of the binding data indicated that the JH analogue did not significantly alter the affinity nor the number of hCG binding sites, as well as GTP binding to plasma membranes. JH analogue inhibited the stimulatory action of both cholera toxin and forskolin on cAMP production and the concomitant steroidogenic response. JH analogue inhibited (Bu)2cAMP-stimulated progesterone synthesis, indicating that a process downstream to the adenylyl cyclase in the steroidogenic pathway is also affected.
研究了保幼激素III(JH-III)和JH类似物2-(4-苯氧基苯氧基)-乙氧基四氢吡喃对睾丸类固醇生成的影响。以培养的MA-10睾丸间质细胞瘤细胞为模型,发现这些化合物是以剂量依赖方式对LH/hCG类固醇生成作用的有效抑制剂。对结合数据的Scatchard作图分析表明,JH类似物不会显著改变hCG结合位点的亲和力和数量,以及GTP与质膜的结合。JH类似物抑制霍乱毒素和福斯高林对cAMP生成的刺激作用以及伴随的类固醇生成反应。JH类似物抑制(Bu)2cAMP刺激的孕酮合成,表明类固醇生成途径中腺苷酸环化酶下游的一个过程也受到影响。