Khan F S, Fotherby K
J Steroid Biochem. 1983 Nov;19(5):1657-60. doi: 10.1016/0022-4731(83)90386-2.
The sulphation of a number of contraceptive steroids by rabbit tissue in vitro was investigated. With liver tissue the three synthetic gestagens (norethisterone, norgesterel and lynestrenol) were sulphated at different rates and none was sulphated as rapidly as dehydroepiandrosterone; sulphation occurred at the tertiary 17 beta-hydroxyl group. The synthetic oestrogen ethynyloestradiol was sulphated more rapidly than dehydroepiandrosterone, both mono and disulphates being formed. Of the other tissues studied, sulphation occurred with stomach and lung but not with heart, spleen, muscle, kidney or adipose tissue. These in vitro studies provide confirmation of in vivo findings regarding sulphate conjugates of the synthetic steroids.
对兔组织在体外对多种甾体避孕药进行硫酸化作用的情况进行了研究。在肝脏组织中,三种合成孕激素(炔诺酮、18-甲基炔诺酮和炔雌醇)的硫酸化速率各不相同,且均不如脱氢表雄酮硫酸化得快;硫酸化发生在叔位17β-羟基上。合成雌激素乙炔雌二醇的硫酸化比脱氢表雄酮更快,会形成单硫酸盐和双硫酸盐。在所研究的其他组织中,胃和肺会发生硫酸化作用,而心脏、脾脏、肌肉、肾脏或脂肪组织则不会。这些体外研究证实了关于合成甾体硫酸盐结合物的体内研究结果。