玉米赤霉烯酮霉菌毒素中人类雌激素活性的构效关系。

Structure-activity relationships for human estrogenic activity in zearalenone mycotoxins.

作者信息

Shier W T, Shier A C, Xie W, Mirocha C J

机构信息

Department of Medicinal Chemistry, University of Minnesota, Minneapolis, MN 55455, USA.

出版信息

Toxicon. 2001 Sep;39(9):1435-8. doi: 10.1016/s0041-0101(00)00259-2.

DOI:10.1016/s0041-0101(00)00259-2

PMID:11384734

Abstract

Zearalenones are estrogenic Fusarium mycotoxins consisting of a resorcinol moiety fused to a 14-member macrocyclic lactone. Using an improved MCF7 human breast cell proliferation assay, we have compared the estrogenicity of 17 chromatographically-homogeneous zearalenones. Both similarities and substantial differences from published results in intact animal systems were observed. Substantial human estrogenicity was retained even in analogs lacking hydroxylation on the aromatic and macrocyclic rings.

摘要

玉米赤霉烯酮是具有雌激素活性的镰刀菌霉菌毒素，由一个与14元大环内酯稠合的间苯二酚部分组成。使用改进的MCF7人乳腺细胞增殖试验，我们比较了17种色谱纯的玉米赤霉烯酮的雌激素活性。观察到与完整动物系统中已发表结果的相似性和显著差异。即使在芳香环和大环上缺乏羟基化的类似物中，也保留了显著的人雌激素活性。