Martucci C, Fishman J
Endocrinology. 1977 Dec;101(6):1709-15. doi: 10.1210/endo-101-6-1709.
The uterotrophic activities of the catechol metabolites of estradiol 2-hydroxyestrone, 2-methoxyestrone and 2-hydroxyestradiol were measured under conditions of continuous administration of sc implanted paraffin pellets. The activity of these estrogens was compared to that of estradiol-17beta and its other principal metabolites estrone, estriol and 15alpha-hydroxyestriol (estetrol). The major catechol estrogens, 2-hydroxyestrone and 2-methoxyestrone, and the pregnancy metabolite, 15alpha-hydroxyestriol, exhibited no uterotrophic activity. The minor catecholestrogen, 2-hydroxyestradiol, showed some activity whose character was different from that exhibited by implants of estradiol, estrone and estriol all of which were equipotent uterotrophic agents. Implants of 2-hydroxyestrone in the presence of estradiol or estriol pellets did not diminish the response to the latter indicating that the 2-hydroxyestrone is not antiestrogenic under these conditions. It is concluded that the direction of estradiol metabolism can have a profound influence on the expression of peripheral hormonal activity with hydroxylation at C-2 terminating and hydroxylation at C-16 extending it.
在连续皮下植入石蜡丸剂的条件下，测定了雌二醇的儿茶酚代谢物2-羟基雌酮、2-甲氧基雌酮和2-羟基雌二醇的子宫营养活性。将这些雌激素的活性与17β-雌二醇及其其他主要代谢物雌酮、雌三醇和15α-羟基雌三醇（雌四醇）的活性进行了比较。主要的儿茶酚雌激素2-羟基雌酮和2-甲氧基雌酮，以及妊娠代谢物15α-羟基雌三醇，均未表现出子宫营养活性。次要的儿茶酚雌激素2-羟基雌二醇表现出一些活性，其性质与雌二醇、雌酮和雌三醇植入物所表现出的活性不同，而雌二醇、雌酮和雌三醇都是等效的子宫营养剂。在雌二醇或雌三醇丸剂存在的情况下，2-羟基雌酮植入物并未减弱对后者的反应，这表明在这些条件下2-羟基雌酮不具有抗雌激素作用。结论是，雌二醇代谢的方向可对外周激素活性的表达产生深远影响，C-2位羟基化终止外周激素活性，而C-16位羟基化则增强外周激素活性。
