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玉米赤霉烯酮和顺式玉米赤霉烯酮新的I相和II相代谢产物的雌激素活性。

Estrogenicity of novel phase I and phase II metabolites of zearalenone and cis-zearalenone.

作者信息

Drzymala Sarah S, Binder Jennifer, Brodehl Antje, Penkert Martin, Rosowski Mark, Garbe Leif-Alexander, Koch Matthias

机构信息

Department of Analytical Chemistry, Reference Materials, Federal Institute for Materials Research and Testing (BAM), 12489, Berlin, Germany.

Institute of Medical Biotechnology, Department of Biotechnology, Technische Universität Berlin, 13355, Berlin, Germany.

出版信息

Toxicon. 2015 Oct;105:10-2. doi: 10.1016/j.toxicon.2015.08.027. Epub 2015 Sep 1.

DOI:10.1016/j.toxicon.2015.08.027
PMID:26335359
Abstract

Zearalenone and its cis-isomer, cis-zearalenone, are nonsteroidal mycotoxins that elicit an estrogenic response upon binding to the estrogen receptor. This study compares the estrogenicity of eleven congeners including novel metabolites as 15-OH-zearalenone, zearalenone-14-sulfate, α-cis-zearalenol and β-cis-zearalenol using the E-Screen assay. Overall, a change in the configuration from trans to cis retains significant estrogenic activity. In contrast, alterations of the aromatic moiety including hydroxylation and sulfation showed a markedly decreased estrogenicity when compared to zearalenone.

摘要

玉米赤霉烯酮及其顺式异构体顺式玉米赤霉烯酮是一类非甾体霉菌毒素,它们在与雌激素受体结合后会引发雌激素反应。本研究使用E-Screen试验比较了11种同系物的雌激素活性,其中包括新型代谢产物,如15-羟基玉米赤霉烯酮、玉米赤霉烯酮-14-硫酸盐、α-顺式玉米赤霉烯醇和β-顺式玉米赤霉烯醇。总体而言,从反式到顺式的构型变化保留了显著的雌激素活性。相比之下,与玉米赤霉烯酮相比,包括羟基化和硫酸化在内的芳香部分的改变显示出雌激素活性明显降低。

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