Title |
Interaction of Phytoestrogens with Estrogen Receptors α and β
|
---|---|
Published in |
Biological and Pharmaceutical Bulletin, January 2001
|
DOI | 10.1248/bpb.24.351 |
Pubmed ID | |
Authors |
Keiko MORITO, Toshiharu HIROSE, Junei KINJO, Tomoki HIRAKAWA, Masafumi OKAWA, Toshihiro NOHARA, Sumito OGAWA, Satoshi INOUE, Masami MURAMATSU, Yukito MASAMUNE |
Abstract |
The human estrogen receptor (hER) exists as two subtypes, hER alpha and hER beta, that differ in the C-terminal ligand-binding domain and in the N-terminal transactivation domain. In this study, we investigated the estrogenic activities of soy isoflavones after digestion with enteric bacteria in competition binding assays with hER alpha or hER beta protein, and in a gene expression assay using a yeast system. The estrogenic activities of these isoflavones were also investigated by the growth of MCF-7 breast cancer cells. Isoflavone glycoside binds weakly to both receptors and estrogen receptor-dependent transcriptional expression is poor. The aglycones bind more strongly to hER beta than to hER alpha. The binding affinities of genistein, dihydrogenistein and equol are comparable to the binding affinity of 17 beta-estradiol. Equol induces transcription most strongly with hER alpha and hER beta. The concentration required for maximal gene expression is much higher than expected from the binding affinities of the compounds, and the maximal activity induced by these compounds is about half the activity of 17 beta-estradiol. Although genistin binds more weakly to the receptors and induces transcription less than does genistein, it stimulates the growth of MCF-7 cells more strongly than does genistein. |
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Country | Count | As % |
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Demographic breakdown
Type | Count | As % |
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Practitioners (doctors, other healthcare professionals) | 1 | 33% |
Mendeley readers
Geographical breakdown
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Singapore | 1 | <1% |
Spain | 1 | <1% |
Japan | 1 | <1% |
Greece | 1 | <1% |
United States | 1 | <1% |
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Student > Master | 29 | 16% |
Student > Bachelor | 26 | 14% |
Researcher | 20 | 11% |
Other | 10 | 5% |
Other | 37 | 20% |
Unknown | 32 | 17% |
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Biochemistry, Genetics and Molecular Biology | 26 | 14% |
Medicine and Dentistry | 24 | 13% |
Pharmacology, Toxicology and Pharmaceutical Science | 12 | 6% |
Chemistry | 11 | 6% |
Other | 25 | 13% |
Unknown | 41 | 22% |