Söderqvist G, Olsson H, Wilking N, von Schoultz B, Carlström K
Department of Obstetrics and Gynecology, Karolinska Institute, Karolinska Hospital, Stockholm, Sweden.
J Steroid Biochem Mol Biol. 1994 Feb;48(2-3):221-4. doi: 10.1016/0960-0760(94)90148-1.
The metabolism of [3H]estrone sulfate ([3H]E1S) was studied in normal breast tissue from 10 premenopausal women without oral contraceptives (OC), in 12 OC users and in 9 untreated postmenopausal women. [3H]E1S was converted into estrone ([3H]E1) and estradiol-17 beta ([3H]E2) by tissue samples from all three groups of women, with only minor formation of other unconjugated compounds. The rate of [3H]E2 formation was significantly higher in premenopausal women without OC than in postmenopausal women. Among premenopausal women, OC users had a significantly lower rate of total hydrolysis and of [3H]E1 formation than non-users. The rate of total hydrolysis of [3H]E1S in normal breast tissue from all three groups of women was similar to that in muscle, but the rate of [3H]E2 formation was ten times higher. Both total hydrolysis rate and rate of [3H]E2 formation were significantly lower in normal breast tissue than in breast carcinoma and in normal and neoplastic endometrium. The specific ability of normal breast tissue to convert E1S into the terminal biologically active estrogen E2 may be important for estrogenic stimulation of the breast in subjects with low circulating E2 levels. The lower rate of E1 formation in OC users may reflect an inhibitory effect of the progestagen compound in such preparations.
在10名未服用口服避孕药（OC）的绝经前女性、12名服用OC的女性以及9名未经治疗的绝经后女性的正常乳腺组织中，对[3H]硫酸雌酮（[3H]E1S）的代谢进行了研究。所有三组女性的组织样本均将[3H]E1S转化为雌酮（[3H]E1）和雌二醇-17β（[3H]E2），仅少量生成其他未结合化合物。未服用OC的绝经前女性中[3H]E2的生成速率显著高于绝经后女性。在绝经前女性中，服用OC的女性总水解率和[3H]E1生成率显著低于未服用者。三组女性正常乳腺组织中[3H]E1S的总水解率与肌肉中的相似，但[3H]E2的生成速率高出十倍。正常乳腺组织中的总水解率和[3H]E2生成率均显著低于乳腺癌组织以及正常和肿瘤性子宫内膜组织。正常乳腺组织将E1S转化为最终生物活性雌激素E2的特定能力，对于循环E2水平较低的受试者乳腺的雌激素刺激可能很重要。服用OC的女性中E1生成率较低可能反映了此类制剂中孕激素化合物的抑制作用。
