Gurpide E, Marks C
J Clin Endocrinol Metab. 1981 Feb;52(2):252-5. doi: 10.1210/jcem-52-2-252.
Specimens of proliferative and secretory endometrium which differ in the levels of 17 beta-estradiol dehydrogenase activity, were superfused with mixtures of [3H]estradiol ([3H]E2) and [3H]ethynyl estradiol ([3H]EE) in the presence and absence of diethylstilbestrol. Concentrations of labeled E2, EE, and estrone were measured in homogenates and in nuclei isolated from the superfused tissues. The relative proportions of [3H]EE and [3H]E2 bound to nuclear receptor were much higher in secretory than in proliferative endometrium. Since EE binds to the estrogen receptor but is not a substrate for 17 beta-estradiol dehydrogenase, these results demonstrate the influence of metabolism on the binding of E2 to the receptor. The elevated enzymatic activity present in secretory endometrium also accounts for the relatively lower concentration of [3H]E2 and the increased [3H]estrone to [3H]E2 ratio in the superfused tissue.
对具有不同17β - 雌二醇脱氢酶活性水平的增殖期和分泌期子宫内膜标本，在存在和不存在己烯雌酚的情况下，用[³H]雌二醇（[³H]E2）和[³H]乙炔雌二醇（[³H]EE）的混合物进行灌流。在匀浆以及从灌流组织中分离出的细胞核中，测量标记的E2、EE和雌酮的浓度。与增殖期子宫内膜相比，[³H]EE和[³H]E2与核受体结合的相对比例在分泌期子宫内膜中要高得多。由于EE与雌激素受体结合，但不是17β - 雌二醇脱氢酶的底物，这些结果证明了代谢对E2与受体结合的影响。分泌期子宫内膜中存在的酶活性升高也解释了灌流组织中[³H]E2浓度相对较低以及[³H]雌酮与[³H]E2的比率增加的原因。
