Kono S, Matsumura M, Higa H, Sunagawa H
Nihon Naibunpi Gakkai Zasshi. 1987 May 20;63(5):712-7. doi: 10.1507/endocrine1927.63.5_712.
The hypocholesterolemic effect of 2-methoxyestrone (2-MeOE1), 2-methoxyestriol (2-MeOE3) and estradiol-17 beta (E2-17 beta) was investigated in two experimental systems of normocholesterolemic and dietary hypercholesterolemic rats that had undergone oophorectomy. Each compound was subcutaneously administered for 6 consecutive days at a dose of 10 micrograms per day in the former systems and at 300 micrograms per day in the latter system, respectively. The hypocholesterolemic effect was in the following relation: 2-MeOE3 = E2 - 17 beta greater than 2-MeOE1. In the latter system, the serum total cholesterol level of individual rats in both 2-MeOE3- and E2-17 beta-administered groups returned to normal. No uterotrophic activity was exhibited by either 2-MeOE1 or 2-MeOE3, while E2-17 beta exhibited an anomalous activity. The effect of 2-MeOE1 and 2-MeOE3 on body weight was not exhibited, while E2-17 beta reduced it slightly. The results suggest that catechol estrogen 2-monomethyl ether plays an important role in lipid metabolism through estrogen receptor independent mechanisms and has a pharmacologically important effect on hyperlipidemia and atherosclerosis.
在已接受卵巢切除术的正常胆固醇血症和饮食性高胆固醇血症大鼠的两个实验系统中，研究了2-甲氧基雌酮（2-MeOE1）、2-甲氧基雌三醇（2-MeOE3）和雌二醇-17β（E2-17β）的降胆固醇作用。在前一个系统中，每种化合物均以每天10微克的剂量连续皮下注射6天，在后一个系统中则以每天300微克的剂量注射。降胆固醇作用呈以下关系：2-MeOE3 = E2 - 17β > 2-MeOE1。在后一个系统中，给予2-MeOE3和E2-17β的两组中，各只大鼠的血清总胆固醇水平均恢复正常。2-MeOE1和2-MeOE3均未表现出子宫营养活性，而E2-17β表现出异常活性。2-MeOE1和2-MeOE3对体重无影响，而E2-17β使其略有降低。结果表明，儿茶酚雌激素2-单甲醚通过不依赖雌激素受体的机制在脂质代谢中起重要作用，对高脂血症和动脉粥样硬化具有重要的药理作用。
