Barth A, Chemnitius K H, Schneider B, Klinger W
Arch Int Pharmacodyn Ther. 1986 Sep;283(1):5-15.
Ethinylestradiol (EE), administered to male Wistar rats for 5 or 14 days, decreased bile flow and biliary excretion of ICG in bile fistula rats in dependence on dose. The bile acid excretion rate was not constantly influenced. EE pretreatment of rats also diminished the in vitro accumulation of eosine in liver slices. The new estrogens STS 651 and STS 661 decreased bile flow, ICG excretion and in vitro eosine accumulation to nearly the same extent as did EE pretreatment; bile acid excretion was not influenced significantly. Evidently the 14 alpha-15 alpha-methylen structure in STS 651 and STS 661 as well as the additional methoxygroup in C3 position did not protect against cholestatic effects of estrogens. The new 17 beta-trimethyl-silyloxy-estrogen J 303 did not show cholestatic effects in rats. This structure is able to prevent the formation of toxic estrogen metabolites in rats.
给雄性Wistar大鼠连续5天或14天服用炔雌醇（EE），会使胆管瘘大鼠的胆汁流量和胆汁中吲哚菁绿（ICG）的胆汁排泄量依剂量减少。胆汁酸排泄率未受到持续影响。对大鼠进行EE预处理也会减少肝切片中伊红的体外蓄积。新型雌激素STS 651和STS 661使胆汁流量、ICG排泄及体外伊红蓄积减少的程度与EE预处理几乎相同；胆汁酸排泄未受到显著影响。显然，STS 651和STS 661中的14α-15α-亚甲基结构以及C3位上额外的甲氧基并不能防止雌激素的胆汁淤积作用。新型17β-三甲基硅氧基雌激素J 303在大鼠中未表现出胆汁淤积作用。这种结构能够防止大鼠体内形成有毒的雌激素代谢产物。
