酚类化合物雌激素效应的比较研究

Comparative study of phenolic compounds estrogenic and anti-estrogenic activities

采用重组人雌激素受体基因片段(hER)及共激活因子(GRIP1)双杂交酵母检测体系,检测9种酚类物质的类雌激素和抗雌激素效应.结果表明,所检测的化合物中有3种同时表现出雌激素诱导与抑制活性;2种只表现出雌激素诱导活性;1种只表现出雌激素抑制活性;3种均没有雌激素诱导与抑制活性.结构分析表明:酚类中产生雌激素活性的物质具有取代基位于对位且邻位没有大的取代基团的结构;烷基在对位的酚类物质也能显示出雌激素拮抗活性.所采用的双杂交酵母检测体系适用于外源物质的雌激素活性检测,具有较高的灵敏度;结合外源物的雌激素诱导与抑制活性,用于分析污染物的体内作用方式。

The estrogenic and anti-estrogenic activities of 9 phenolic compounds were detected using recombined two-hybrid estrogenic receptor （hER） and co-activator （GRIP1） yeast assay. 9 detected phenolic compounds, 3 compounds had both estrogenic and anti-estrogenic activities; 2 compounds had estrogenic agonistic activities; 1 compound had anti-estrogenic activities; 3 compounds didn＇t show any estrogenic or anti-estrogenic activities. The function of tested compounds was dependant on their structure： the positive compounds had a phenol ring with a moiety of appropriate substitution at the para-position, and that substitution of a bulky moiety at the ortho-position reduces activity. And phenol with alkyl at the para-position also could induce estrogenic anti-agonistic activities. The two-hybrid yeast system used had high sensitivity and could be used with the estrogenic agonistic and antagonistic activities to analyze the research on disrupt mechanism ofxenobiotics.