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Assessment of the estrogenicity of isoflavonoids, using MCF-7-ERE-Luc cells

Title
Assessment of the estrogenicity of isoflavonoids, using MCF-7-ERE-Luc cells
Authors
Joung, KEKim, YWSheen, YY
Ewha Authors
신윤용
SCOPUS Author ID
신윤용scopus
Issue Date
2003
Journal Title
ARCHIVES OF PHARMACAL RESEARCH
ISSN
0253-6269JCR Link
Citation
vol. 26, no. 9, pp. 756 - 762
Keywords
genisteinbiochanin AdaidzeinEEQ17 beta-estradiolERE
Publisher
PHARMACEUTICAL SOCIETY KOREA
Indexed
SCIE; SCOPUS; KCI WOS scopus
Abstract
In the current study, our research focused on the estrogenic activity of isoflavonoids, mainly genistein, biochanin A and daidzein. Genistein enhanced the reporter gene expression of MCF-7-ERE-Luc cells, at a concentration as low as 10 nM, with a concentration of 100 nM the achieved gene expression effects were similar to those of 10 pM 17beta-estradiol. Based on the estrogenic activities of biochanin A and daidzein, hydroxyl groups at the 4' and 5 positions are needed for the maximal effect of the genistein. The estrogenic effects of these isoflavonoids were inhibited by the concomitant treatment with tamoxifen. The data showed that the estrogenic effects of isoflavonoids were mediated through estrogen receptors. When the isoflavonoids were tested as mixtures, the estrogenic effects were lower than the arithmetic sum of those induced by each individual isoflavonoid. The estrogenic potency of each isoflavonoid was presented at EC50 levels with a 17beta-estradiol equivalent concentration (EEQ) based on the dose response of each chemical. The EC(50)s and EEQs of genistein, biochanin A and daidzein were 4.15, 0.89 and 0.18 muM, and 15.0, 5.12 and 1.83 muM/M, respectively. Our data clearly demonstrated that the pERE-luciferase reporter gene assay was suited for the sensitive and quantitative measurement, and large scale screening, of the estrogenicity of chemicals in vitro.
DOI
10.1007/BF02976687
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약학대학 > 약학과 > Journal papers
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