Source:http://linkedlifedata.com/resource/pubmed/id/12659833
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Predicate | Object |
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
2
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pubmed:dateCreated |
2003-3-27
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pubmed:abstractText |
In this study, the metabolic activation of 2-nitrofluorene (NF) to estrogenic compounds was examined. NF was negative in estrogen reporter assays using estrogen-responsive yeast and human breast cancer cell line MCF-7. However, the compound exhibited estrogenic activity after incubation with liver microsomes of 3-methylcholanthrene-treated rats in the presence of NADPH. Minor estrogenic activity was observed when liver microsomes of untreated or phenobarbital-treated rats were used instead of those from 3-methylcholanthrene-treated rats. When the compound was incubated with the liver microsomes of 3-methylcholanthrene-treated rats in the presence of NADPH, 7-hydroxy-2-nitrofluorene (7-OH-NF) was formed as a major metabolite. However, little of the metabolite was formed by liver microsomes of untreated or phenobarbital-treated rats. Rat recombinant cytochrome P450 1A1 exhibited a significant oxidase activity toward NF, affording 7-OH-NF. Liver microsomes of phenobarbital-treated rats also enhanced oxidase activity toward NF. In this case, 9-hydroxy-2-nitrofluorene was formed. 7-OH-NF exhibited a significant estrogenic activity, while the activity of 9-hydroxy-2-nitrofluorene was much lower. These results suggest that the estrogenic activity of NF was due to formation of the 7-hydroxylated metabolite by liver microsomes.
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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-nitrofluorene,
http://linkedlifedata.com/resource/pubmed/chemical/Air Pollutants,
http://linkedlifedata.com/resource/pubmed/chemical/Estradiol,
http://linkedlifedata.com/resource/pubmed/chemical/Estradiol Congeners,
http://linkedlifedata.com/resource/pubmed/chemical/Fluorenes,
http://linkedlifedata.com/resource/pubmed/chemical/Phenobarbital
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pubmed:status |
MEDLINE
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pubmed:month |
Apr
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pubmed:issn |
0006-291X
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pubmed:author | |
pubmed:issnType |
Print
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pubmed:day |
4
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pubmed:volume |
303
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
419-26
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pubmed:dateRevised |
2006-11-15
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pubmed:meshHeading |
pubmed-meshheading:12659833-Air Pollutants,
pubmed-meshheading:12659833-Animals,
pubmed-meshheading:12659833-Biotransformation,
pubmed-meshheading:12659833-Estradiol,
pubmed-meshheading:12659833-Estradiol Congeners,
pubmed-meshheading:12659833-Fluorenes,
pubmed-meshheading:12659833-Male,
pubmed-meshheading:12659833-Microsomes, Liver,
pubmed-meshheading:12659833-Phenobarbital,
pubmed-meshheading:12659833-Rats,
pubmed-meshheading:12659833-Rats, Sprague-Dawley
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pubmed:year |
2003
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pubmed:articleTitle |
Estrogenic activity of an environmental pollutant, 2-nitrofluorene, after metabolic activation by rat liver microsomes.
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pubmed:affiliation |
Graduate School of Biomedical Sciences, Programs for Pharmaceutical Sciences, Hiroshima University, Kasumi 1-2-3, Minami-ku, Hiroshima, Japan.
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pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't
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