hexestrol的致癌性和代谢活化。

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Liehr詹,Ballatore Dague BB, Ulubelen AA

hexestrol的致癌性和代谢活化。

化学生物相互作用。1985年10月;55 (1 - 2):157 - 76。

PubMed ID

2998630 (在PubMed

]

文摘

合成雌激素hexestrol致癌活性的测定在男性的叙利亚仓鼠。在90%和100%之间的动物对待hexestrol或3 ',5 ' 3”5”-tetradeuteriohexestrol植入皮下,25毫克丸,被发现后与肾癌6 - 7个月。体外hexestrol新陈代谢,由phenobarbital-induced鼠肝微粒体,导致3 ' -hydroxyhexestrol的形成。这种代谢物鉴定相比真实的参考材料合成的氧化hexestrol Fremy的盐。己烯雌酚代谢物不能检测到。尿液中男性的叙利亚仓鼠,3“-hydroxyhexestrol 3”-methoxyhexestrol 1-hydroxyhexestrol和其他羟化和/或methoxylated hexestrol代谢物被确定。再一次,没有检测己烯雌酚作为hexestrol体内代谢物。3 ' -hydroxyhexestrol当时的反应性研究来确定这种儿茶酚雌激素发挥了作用在hexestrol致癌性。辣根过氧化物酶催化的氧化3 -hydroxyhexestrol 3 ', 4 ' -hexestrol醌。这种氧化反应也可以进行non-enzymatically使用硅藻土作为氧化剂氧化银或银碳酸盐。 The quinone was unstable (t1/2 in methylene chloride: 53 min). It reacted with sulfur-containing compounds such as mercaptoethanol by Michael addition to form 3'-(2-hydroxyethylthio)-5'-hydroxyhexestrol. 3',4'-Hexestrol quinone reacted with simple amines such as ethylamine to form N-ethyl-aminohexestrol. The chemical reactions described above were carried out to test the reactivity of identified or suspected metabolic intermediates of hexestrol. It was concluded that carcinogenicity of hexestrol was not based on its conversion to diethylstilbestrol. Rather, catechol estrogen formation may be necessary for the carcinogenic action of hexestrol in analogy to events observed earlier with estradiol.

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药物

Hexestrol