Moutaouakkil M, Prost O, Dahan N, Adessi G L
J Steroid Biochem. 1984 Sep;21(3):321-8. doi: 10.1016/0022-4731(84)90286-3.
Estrone and dehydroepiandrosterone (DHA) sulfatase activities were studied in the uterus and liver of female guinea-pigs (albino variety). The two activities were found in particulates, with the highest specific activity in microsomes. The effects of pH, buffers, temperature and the non-competitive inhibition of DHA sulfate on estrone sulfatase provided arguments for the existence of two distinct sulfatases. However, acrylamide gel electrophoresis of the solubilized microsome sulfatases gave a single peak for the two activities. In the uterus, the apparent Km of estrone and DHA sulfatases were 26.4 and 15.6 microM. Solubilized microsomal estrone sulfatase was inhibited by unconjugated steroids. The apparent Km of estrone sulfatase in liver was 10.7 microM. Estrone and DHA sulfatase activities were consistently lower in liver than in uterus and no DHA sulfatase activity was detected in fetal liver. In the uterus, the same sulfatase activities were found in female fetuses, castrated or mature females. Estrone sulfatase was significantly increased in the uterus of pregnant females (60-65 days gestation). Estrone sulfate was injected in vivo into mature castrated females. A significant increase in uterine weight and in uterine progesterone receptors was observed. The cytosol progesterone receptors were characterized by their Kd (1.40 nM) and by sucrose density gradient. It is concluded that the variations of estrone sulfatase activity in target tissues like the uterus may control the intracellular levels of biologically active estrogens.
对雌性豚鼠(白化变种)的子宫和肝脏中的雌酮硫酸酯酶和脱氢表雄酮(DHA)硫酸酯酶活性进行了研究。这两种酶活性存在于微粒体部分,其中微粒体中的比活性最高。pH、缓冲液、温度以及DHA硫酸盐对雌酮硫酸酯酶的非竞争性抑制作用的影响为存在两种不同的硫酸酯酶提供了依据。然而,对溶解的微粒体硫酸酯酶进行丙烯酰胺凝胶电泳时,这两种酶活性出现了一个单一峰。在子宫中,雌酮硫酸酯酶和DHA硫酸酯酶的表观Km分别为26.4和15.6微摩尔。溶解的微粒体雌酮硫酸酯酶受到未结合类固醇的抑制。肝脏中雌酮硫酸酯酶的表观Km为10.7微摩尔。肝脏中的雌酮和DHA硫酸酯酶活性始终低于子宫,且在胎儿肝脏中未检测到DHA硫酸酯酶活性。在子宫中,雌性胎儿、去势雌性或成熟雌性中发现了相同的硫酸酯酶活性。怀孕雌性(妊娠60 - 6日)子宫中的雌酮硫酸酯酶显著增加。将硫酸雌酮体内注射到成熟去势雌性体内。观察到子宫重量和子宫孕酮受体显著增加。通过其解离常数(1.40纳摩尔)和蔗糖密度梯度对胞质孕酮受体进行了表征。结论是,子宫等靶组织中雌酮硫酸酯酶活性的变化可能控制生物活性雌激素的细胞内水平。