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己烯雌酚在叙利亚金仓鼠胎儿体内的氧化代谢产物。

Oxidative metabolites of diethylstilbestrol in the fetal Syrian golden hamster.

作者信息

Maydl R, Metzler M

出版信息

Teratology. 1984 Dec;30(3):351-7. doi: 10.1002/tera.1420300307.

Abstract

14C-Diethylstilbestrol was administered orally, intraperitoneally, and intrafetally to 15-day pregnant hamsters at a dose of 20 mg/kg body weight, and the radioactivity was determined in the fetus, placenta, and maternal liver after 6 hours. Significant amounts of radioactivity were found in these tissues in every case, indicating maternal-fetal and fetal-maternal transfer of diethylstilbestrol. Part of the radioactivity found in the tissues could not be extracted even after excessive washing. This implied the presence of reactive metabolites. In the fetal and placental extracts, eight oxidative metabolites of diethylstilbestrol were identified by mass fragmentography as hydroxy- and methoxy-derivatives of diethylstilbestrol, pseudodiethylstilbestrol, and dienestrol. The presence of oxidative metabolites in the hamster fetus and the covalent binding to tissue macromolecules are possibly associated with the fetotoxic effects of diethylstilbestrol.

摘要

给怀孕15天的仓鼠经口、腹腔内和经胎儿途径给予剂量为20毫克/千克体重的14C - 己烯雌酚,6小时后测定胎儿、胎盘和母体肝脏中的放射性。在每种情况下,这些组织中均发现大量放射性,表明己烯雌酚存在母胎和胎母转移。即使经过过度洗涤,组织中发现的部分放射性仍无法提取。这意味着存在反应性代谢物。通过质量碎片分析法在胎儿和胎盘提取物中鉴定出己烯雌酚的八种氧化代谢物,为己烯雌酚、假己烯雌酚和dienestrol的羟基和甲氧基衍生物。仓鼠胎儿中氧化代谢物的存在以及与组织大分子的共价结合可能与己烯雌酚的胚胎毒性作用有关。

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