Shiverick K T, Delorme A M, Scammell J G, Fregly M J
J Pharmacol Exp Ther. 1982 Jun;221(3):564-9.
The effects of chronic treatment with thyroxine (T4) and estradiol on hepatic microsomal metabolism of estrogens to catechol products were studied and the extent to which activity in vitro correlated with serum estradiol concentrations in vivo was assessed. Female rats were treated with either estradiol benzoate (EB; 56 micrograms/kg/day from silastic implants), T4 (50 micrograms/kg/day, s.c.) or combined EB + T4 for 35 days. Animals treated with EB + T4, but not T4 alone, showed a significant increase above controls both in the concentration of triiodothyronine in serum and food consumption. Serum concentrations of endogenous estradiol in untreated control and T4-treated animals were similar. Although both EB-treated groups received comparable doses of steroid from silastic implants, the concentration of estradiol in serum was 30% lower in EB + T4-treated animals than in animals treated with EB alone. Formation of catechol estrogen metabolites by hepatic microsomes was not significantly altered by EB and T4 administered separately, but enzyme activity was increased significantly with combined hormonal therapy. In contrast, microsomal hydroxylation of testosterone was not increased by treatment with EB + T4, data which suggest that total steroid hydroxylase activity was not enhanced by combined hormonal administration. Correlation analysis of microsomal catechol estrogen formation in vitro with serum concentrations of estradiol in vivo indicated related to the concentration of estrogen in serum only after coadministration of a low dose of T4 with EB.
研究了甲状腺素(T4)和雌二醇长期治疗对雌激素在肝脏微粒体中代谢为儿茶酚产物的影响,并评估了体外活性与体内血清雌二醇浓度的相关程度。给雌性大鼠分别用苯甲酸雌二醇(EB;通过硅橡胶植入物给予56微克/千克/天)、T4(50微克/千克/天,皮下注射)或联合使用EB + T4进行治疗,为期35天。接受EB + T4治疗的动物,但单独使用T4治疗的动物未出现这种情况,其血清中三碘甲状腺原氨酸浓度和食物消耗量均显著高于对照组。未治疗的对照组和T4治疗组动物的内源性雌二醇血清浓度相似。尽管两个接受EB治疗的组从硅橡胶植入物中获得的类固醇剂量相当,但接受EB + T4治疗的动物血清中雌二醇浓度比单独接受EB治疗的动物低30%。单独给予EB和T4时,肝脏微粒体形成儿茶酚雌激素代谢产物的情况没有显著改变,但联合激素治疗时酶活性显著增加。相反,用EB + T4治疗并未增加睾酮的微粒体羟基化,这些数据表明联合激素给药并未增强总类固醇羟化酶活性。体外微粒体儿茶酚雌激素形成与体内血清雌二醇浓度的相关性分析表明,仅在低剂量T4与EB共同给药后,其与血清中雌激素浓度相关。