Martucci C P, Fishman J
Endocrinology. 1979 Dec;105(6):1288-92. doi: 10.1210/endo-105-6-1288.
The biological activity of a series of natural catechol estrogens was examined under conditions of continuous administration. 2-Hydroxyestradiol (2OH-E2), 2-methoxyestradiol (2MeOE2), 4-hydroxyestrone (4OH-E1), 4-methoxyestradiol (4MeOE2), 2-hydroxyestrone (2OH-E1), and 4-methoxyestrone (4MeOE1) were delivered at the rate of 1 microgram/h from osmotic pumps implanted in ovariectomized rats. Uterine growth and plasma LH concentrations were measured 24, 48, and 72 h after implantation. Little or no uterotropic activity was exhibited by the 2-hydroxylated metabolites 2OH-E1 and 2MeOE2 at any interval, while 2OH-E2 exhibited anomalous uterotropic activity, which terminated at 48 h. The 4-hydroxylated compounds 4MeOE2, 4OH-E1, and 4MeOE1 all produced substantial and progressive uterine growth. Tonic LH secretion was suppressed by 2OH-E2, 4OH-E1, and 4MeOE1 in proportion to their uterotropic activity. 2OH-E1 was the only substance which increased plasma LH concentrations. The nuclear receptor occupancy by 2OH-E2 was substantially shorter than that of E2. Binding studies of the test and other related estrogens to the uterine cytosol estradiol receptor showed that their relative binding affinities in many instances did not correlate with their biological activities.
在持续给药条件下检测了一系列天然儿茶酚雌激素的生物活性。将2-羟基雌二醇（2OH-E2）、2-甲氧基雌二醇（2MeOE2）、4-羟基雌酮（4OH-E1）、4-甲氧基雌二醇（4MeOE2）、2-羟基雌酮（2OH-E1）和4-甲氧基雌酮（4MeOE1）以1微克/小时的速率从植入去卵巢大鼠体内的渗透泵中释放。在植入后24、48和72小时测量子宫生长和血浆促黄体生成素（LH）浓度。2-羟基化代谢物2OH-E1和2MeOE2在任何时间段均未表现出明显的促子宫生长活性，而2OH-E2表现出异常的促子宫生长活性，该活性在48小时时终止。4-羟基化化合物4MeOE2、4OH-E1和4MeOE1均引起子宫显著且持续的生长。2OH-E2、4OH-E1和4MeOE1对LH的基础分泌抑制作用与其促子宫生长活性成比例。2OH-E1是唯一能提高血浆LH浓度的物质。2OH-E2与核受体的结合时间明显短于雌二醇（E2）。对受试雌激素及其他相关雌激素与子宫胞质雌二醇受体的结合研究表明，它们在许多情况下的相对结合亲和力与其生物活性不相关。
