Biotransformation of the mineralocorticoid receptor antagonists spironolactone and canrenone by human CYP11B1 and CYP11B2: Characterization of the products and their influence on mineralocorticoid receptor transactivation
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- 作者：Lina Schiffera ; 1 ; Anne-Rose Mü ; llera ; 1 ; Anna Hoblera ; Simone Brixius-Anderkoa ; Josef Zappb ; Frank Hannemanna ; Rita Bernhardta ; ritabern@mx.uni-saarland.de" class="auth_mail" title="E-mail the corresponding author
- 关键词：AdR ; adrenodoxin reductase ; Adx ; adrenodoxin ; DOC ; 11-deoxycorticosterone ; E. coli ; Escherichia coli ; MR ; mineralocorticoid receptor ; MRA ; mineralocorticoid receptor antagonist ; NMR ; nuclear magnetic resonance ; RSS ; 11-deoxycortisol (Reichstein&rsquo ; s substance S)
- 刊名：Journal of Steroid Biochemistry and Molecular Biology
- 出版年：2016
- 出版时间：October 2016
- 年：2016
- 卷：163
- 期：Complete
- 页码：68-76
- 全文大小：1533 K
文摘
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Human CYP11B1 and CYP11B2 are shown to convert spironolactone and canrenone.
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Metabolites are identified by NMR as 11β-, 18- and 19-hydroxylated derivatives.
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Metabolism alters the antagonistic effects on the mineralocorticoid receptor.
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Consideration of CYP11B1 and CYP11B2 as drug-metabolizers is conclusively suggested.