Murugesan K, Vij U, Lal B, Farooq A
Department of Reproductive Biology, All India Institute of Medical Sciences, New Delhi.
Steroids. 1989 Jun;53(6):695-712. doi: 10.1016/0039-128x(89)90061-5.
The biotransformation of estradiol (E2) and estrone (E1) in the uterus of rabbits treated with norgestrel (NG), norethindrone (NET), norethindrone acetate (NETA), progesterone (P4), and E2 either by subcutaneous injection in oil or by intrauterine steroid-releasing silastic implants was carried out under an in vitro short-term incubation system. The studies have shown that E2 stimulates 17 beta-hydroxysteroid dehydrogenase (17 beta-OHSD) much more than P4 as compared to untreated controls. The kinetic studies on E2 metabolism in the presence of added coenzyme NAD showed an initial rapid estrone formation and a gradual reconversion of E1 to E2. The addition of NADPH, ATP, and glucose-6-phosphate facilitates the reconversion of E1 to E2. The interconversion of E2 and estrone in the presence of coenzymes was five- to ten-fold higher in the endometrium than in the myometrium per milligram protein. Both E2 and progestins stimulate the uterine 17 beta-OHSD activity in rabbit uterus. This study further suggested that the hormone-induced metabolism of estradiol and estrone in the rabbit uterus is essentially modulated by the availability of coenzymes.
在体外短期孵育系统下，对经皮下注射油剂或子宫内植入含左炔诺孕酮（NG）、炔诺酮（NET）、醋酸炔诺酮（NETA）、孕酮（P4）和雌二醇（E2）的硅橡胶释放甾体植入物处理的家兔子宫中雌二醇（E2）和雌酮（E1）的生物转化进行了研究。研究表明，与未处理的对照组相比，E2刺激17β-羟类固醇脱氢酶（17β-OHSD）的作用比P4强得多。在添加辅酶NAD的情况下对E2代谢的动力学研究表明，最初快速形成雌酮，随后E1逐渐重新转化为E2。添加NADPH、ATP和6-磷酸葡萄糖有助于E1重新转化为E2。在存在辅酶的情况下，每毫克蛋白质中，子宫内膜中E2和雌酮的相互转化比子宫肌层高5至10倍。E2和孕激素均刺激家兔子宫中的子宫17β-OHSD活性。该研究进一步表明，家兔子宫中激素诱导的雌二醇和雌酮代谢主要受辅酶可用性的调节。
