Lumsden M A, West C P, Hawkins R A, Bramley T A, Rumgay L, Baird D T
Department of Obstetrics and Gynaecology, University of Edinburgh.
J Endocrinol. 1989 May;121(2):389-96. doi: 10.1677/joe.0.1210389.
Since uterine leiomyomata (fibroids) are not found in conditions where oestradiol is either absent or present only in low concentrations, oestradiol is considered to be an important factor in the control of fibroid growth. To investigate whether this is due to a direct effect on the tissue, oestradiol and progestogen receptors were measured in tissue removed at hysterectomy from 12 normally cycling women and 13 women who had received the gonadotrophin-releasing hormone (GnRH) agonist Zoladex (ICI 118630) as a subcutaneous depot given at monthly intervals for 3 months preoperatively and a third group of three women who had received the antioestrogen tamoxifen (20 mg daily) for 3 months before surgery. Both unoccupied oestradiol receptors (measured by separating bound from free hormone with dextran-coated charcoal; DCC) and 'total' receptor populations (as measured by an enzyme immunoassay) were measured in each fibroid and adjoining myometrium. There was significantly more binding of both oestradiol and progestogen to fibroid than to myometrium in both the control (P less than 0.01) and agonist-treated groups (P less than 0.05). Oestradiol binding to fibroids in women treated with Zoladex exceeded that in the normally cycling women (P less than 0.05) which in turn exceeded that in the tamoxifen-treated group (P less than 0.05). However, the binding of progestogen, measured by DCC showed the reverse trend. These results may be explained by the low circulating oestradiol concentration in the GnRH agonist-treated women leading to low receptor occupancy.
由于在雌二醇缺乏或仅以低浓度存在的情况下未发现子宫平滑肌瘤（纤维瘤），因此雌二醇被认为是控制纤维瘤生长的重要因素。为了研究这是否是由于对组织的直接作用，对12名正常月经周期女性以及13名在术前3个月每月皮下注射一次促性腺激素释放激素（GnRH）激动剂诺雷德（ICI 118630）的女性在子宫切除术中切除的组织，以及第三组3名在手术前3个月每天服用抗雌激素他莫昔芬（20毫克）的女性的组织进行了雌二醇和孕激素受体检测。在每个纤维瘤和相邻的子宫肌层中都测量了未占据的雌二醇受体（通过用葡聚糖包被的活性炭分离结合态与游离态激素来测量；DCC）和“总”受体群体（通过酶免疫测定法测量）。在对照组（P<0.01）和激动剂治疗组（P<0.05）中，纤维瘤对雌二醇和孕激素的结合均明显多于子宫肌层。用诺雷德治疗的女性中纤维瘤对雌二醇的结合超过正常月经周期女性（P<0.05），而正常月经周期女性又超过他莫昔芬治疗组（P<0.05）。然而，通过DCC测量的孕激素结合呈现相反的趋势。这些结果可能是由于GnRH激动剂治疗的女性循环雌二醇浓度低导致受体占有率低所致。
