Technology for screening estrogen active compound by competitiveness enzyme-linked receptor compatible reaction

A compound and estrogen technology, applied in the field of analysis and testing, can solve the problems of laboratory difficulties, unreported technology for screening estrogen active compounds, and expensive reagents.

Inactive Publication Date: 2009-04-22
RES CENT FOR ECO ENVIRONMENTAL SCI THE CHINESE ACAD OF SCI
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Problems solved by technology

Although this method has high accuracy, it is difficult for general laboratories to carry out due to the expensive reagents and the need for radioactive manipulation.
At...

Method used

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specific Embodiment approach

[0025] The patent of the present invention is a rapid screening technology for competitive estrogen-active compounds based on estrogen receptor-ligand interaction. Its basic estrogenic activity is evaluated based on the competitive binding ability of test compounds to estrogen receptor protein ERα-LBD or ERβ-LBD and the competition of endogenous estrogen 17β estradiol to ERα-LBD or ERβ-LBD The binding capacities were compared to obtain the estrogenic activity of the test compound relative to 17β estradiol, which was expressed by the relative affinity coefficient. The specific implementation is as follows:

[0026] (1) The test compound solution is diluted exponentially by 10, and the above-mentioned competitive enzyme-linked receptor affinity reaction analysis method is used to preliminarily determine the concentration range of its binding to the estrogen receptor.

[0027] (2) On a 96-well microtiter plate, the compound to be tested is diluted in multiples, and the above-men...

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Abstract

The invention belongs to the technical field of assay and test and relates to a technology for rapid screening of estrogenic active compounds. The basic principle is to arrange test compounds, immobilized 17beta estradiol and estrogen receptor proteins ERalpha-LBD or ERbeta-LBD in the same reaction system to lead the test compounds and the immobilized 17beta estradiol to be competitively bound with the ERalpha-LBD or the ERbeta-LBD, and the number of the estrogen receptor proteins which are combined on the immobilized 17beta estradiol is finally detected by the enzyme-linked reaction. The basic evaluation basis of the estrogenic activity is to contrast the competitive binding capacities of the test compounds and the 17beta estradiol to the estrogen receptor proteins ERalpha-LBD or the ERbeta-LBD, thereby evaluating the estrogenic activity of the test compounds. The technology has wide application prospects in the aspects of toxicological studies of environmental pollutants, studies of metabolites of compounds, toxicity evaluation of industrial products, drug screening, analysis of active ingredients, etc.

Description

technical field [0001] The patent of the present invention belongs to the technical field of analysis and testing, and relates to a technology for rapid screening of estrogen-active compounds. This technology has broad application prospects in the toxicological research of environmental pollutants, the research of compound metabolites, the toxicity evaluation of industrial products, drug screening and active ingredient analysis. Background technique [0002] The health effects of environmental pollutants are a common concern. In recent years, more and more compounds that were considered "safe" and widely used have been proved to have estrogen or anti-estrogen activity, which can cause a series of estrogen-dependent physiological and biochemical process disorders, leading to experiments or wild animals. Abnormal embryonic development, decreased reproductive capacity, and abnormal sex differentiation. Although the pathways and biological effects of these compounds on organis...

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Application Information

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IPC IPC(8): G01N33/74G01N33/53G01N33/566
Inventor 江桂斌时国庆周群芳史建波
Owner RES CENT FOR ECO ENVIRONMENTAL SCI THE CHINESE ACAD OF SCI
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