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Predicate | Object |
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
8
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pubmed:dateCreated |
1984-5-30
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pubmed:abstractText |
The estrogen responsive human breast cancer MCF-7 cell culture was examined for its response to 2-hydroxyestrone a principal metabolite of estradiol. Addition of 2-hydroxyestrone to the cell cultures in concentration of 10(-9) - 10(-6) M had no effect on cell growth and proliferation because of rapid O-methylation of the catechol estrogen by catechol O-methyltransferase which is highly active in these cells. In the presence of quinalizarin, a potent catechol O-methyltransferase inhibitor which reduces the O-methylation of the steroid, 10(-7) M and 10(-8) M 2-hydroxyestrone markedly suppresses the growth and proliferation of the cells. The tumor cell growth-inhibitory action of the catechol estrogen was neutralized by the presence of 10(-9) M estradiol. The catechol estrogen inhibition of cell growth is not observed in the estrogen receptor-negative human breast cancer cell lines MDA-MB-231 and MDA-MB-330 providing evidence that the inhibition is specific and is estrogen receptor-mediated. In contrast, the 16 alpha-hydroxylated metabolites of estradiol, estriol and 16 alpha-hydroxyestrone, are effective stimulators of MCF-7 cell proliferation with the latter exhibiting potency in excess of that expected from its estrogen receptor affinity. The present results represent the first observation of a specific receptor-mediated antiestrogenic action of 2-hydroxyestrone and suggest that the physiological regulation of the agonist activity of the primary estrogen may involve in situ generation of catechol estrogen.
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pubmed:grant | |
pubmed:language |
eng
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pubmed:journal | |
pubmed:citationSubset |
IM
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pubmed:chemical |
http://linkedlifedata.com/resource/pubmed/chemical/2-hydroxyestrone,
http://linkedlifedata.com/resource/pubmed/chemical/Estradiol,
http://linkedlifedata.com/resource/pubmed/chemical/Estrogen Antagonists,
http://linkedlifedata.com/resource/pubmed/chemical/Estrogens, Catechol,
http://linkedlifedata.com/resource/pubmed/chemical/Estrone,
http://linkedlifedata.com/resource/pubmed/chemical/Hydroxyestrones,
http://linkedlifedata.com/resource/pubmed/chemical/Receptors, Estrogen
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pubmed:status |
MEDLINE
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pubmed:month |
Apr
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pubmed:issn |
0021-9258
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pubmed:author | |
pubmed:issnType |
Print
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pubmed:day |
25
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pubmed:volume |
259
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
4840-5
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pubmed:dateRevised |
2007-11-14
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pubmed:meshHeading |
pubmed-meshheading:6325410-Breast Neoplasms,
pubmed-meshheading:6325410-Cell Division,
pubmed-meshheading:6325410-Cell Line,
pubmed-meshheading:6325410-Estradiol,
pubmed-meshheading:6325410-Estrogen Antagonists,
pubmed-meshheading:6325410-Estrogens, Catechol,
pubmed-meshheading:6325410-Estrone,
pubmed-meshheading:6325410-Female,
pubmed-meshheading:6325410-Humans,
pubmed-meshheading:6325410-Hydroxyestrones,
pubmed-meshheading:6325410-Kinetics,
pubmed-meshheading:6325410-Receptors, Estrogen
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pubmed:year |
1984
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pubmed:articleTitle |
Antiestrogen action of 2-hydroxyestrone on MCF-7 human breast cancer cells.
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pubmed:publicationType |
Journal Article,
Research Support, U.S. Gov't, P.H.S.
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