代谢物
化学
色谱法
衍生化
气相色谱-质谱法
质谱法
尿
气相色谱法
依西美坦
芳香化酶
生物化学
医学
癌症
内科学
乳腺癌
作者
Gustavo de Albuquerque Cavalcanti,Bruno Carius Garrido,Felipe Dias Leal,Marina Padilha,Xavier de la Torre,Francisco Radler de Aquino Neto
出处
期刊:Steroids
[Elsevier]
日期:2011-09-01
卷期号:76 (10-11): 1010-1015
被引量:14
标识
DOI:10.1016/j.steroids.2011.04.001
摘要
Exemestane is an aromatase enzyme complex inhibitor. Its metabolism in humans is not fully described and there is only one known metabolite: 17β-hydroxyexemestane. In this work, excretion studies were performed with four volunteers aiming at the detection of new exemestane metabolites in human urine by gas chromatography coupled to mass spectrometry (GC–MS) after enzymatic hydrolysis and liquid–liquid extraction. Urine samples collected from four volunteers were analyzed separately. The targets of the study were mainly the 6-exomethylene oxidized metabolites. Two unreported metabolites were identified in both free and glucuconjugated urine fractions from all four volunteers, both of them were the result of the 6-exomethylene moiety oxidation: 6ξ-hydroxy-6ξ-hydroxymethylandrosta-1,4-diene-3,17-dione (metabolite 1) and 6ξ-hydroxyandrosta-1,4-diene-3,17-dione (metabolite 2). Furthermore, only in glucoconjugated fractions from all volunteers, one metabolite arising from the A-ring reduction was identified as well, 3ξ-hydroxy-5ξ-androst-1-ene-6-methylene-17-one (metabolite 3). The molecular formulae of all these metabolites were ascertained by the determination of exact masses using gas chromatography coupled to high resolution mass spectrometry (GC–HRMS). Moreover, all metabolites were confirmed using an alternative derivatization with methoxyamine and MSTFA/TMS-imidazole.
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