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Predicate | Object |
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
4
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pubmed:dateCreated |
1981-9-22
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pubmed:abstractText |
Microsomal monoxygenases can oxidize the axial hydroxyl of the terminal digitoxosyl of digoxin (dg-3), digoxigenin bis-, and digoxigenin mono-digitoxoside (dg-2 and dg-1, respectively) to an oxo-group. The corresponding metabolites (15'-dehydro-dg-3, 9'-dehydro-dg-2, and 3'-dehydro-1, respectively) have been identified by chromatographic and chemical methods. Only after this oxibation the terminal sugar can be split off, presumably by beta-elimination. Therefore, for the degradation of dg-3 three successive cytochrome P450 catalyzed oxidations are necessary before digoxigenin (dg-0) can be obtained. The highest oxibation rate was observed with dg-1 (120-150 pmoles/mg microsomal protein/min) and by far the lowest with dg-2 (6-7 pmoles/min) as the substrate (concentration was 30/microM). The latter may contribute to the effect that dg-2 is the main dg-3 metabolite in vivo. Pretreatment of rats with canrenoate enhanced the microsomal oxidation of dg-3, dg-2, and dg-1 by a factor of 3.2, 2.3 and 1.3, respectively. In contrast, there was no increase after pretreatment with phenobarbital.
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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/Cytochrome P-450 Enzyme System,
http://linkedlifedata.com/resource/pubmed/chemical/Digoxigenin,
http://linkedlifedata.com/resource/pubmed/chemical/Digoxin,
http://linkedlifedata.com/resource/pubmed/chemical/Phenobarbital,
http://linkedlifedata.com/resource/pubmed/chemical/digoxigenin-bis(digitoxoside)
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pubmed:status |
MEDLINE
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pubmed:issn |
0378-7966
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pubmed:author | |
pubmed:issnType |
Print
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pubmed:volume |
5
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
225-32
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pubmed:dateRevised |
2011-2-2
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pubmed:meshHeading |
pubmed-meshheading:7250146-Animals,
pubmed-meshheading:7250146-Cytochrome P-450 Enzyme System,
pubmed-meshheading:7250146-Digoxigenin,
pubmed-meshheading:7250146-Digoxin,
pubmed-meshheading:7250146-Enzyme Induction,
pubmed-meshheading:7250146-Male,
pubmed-meshheading:7250146-Microsomes, Liver,
pubmed-meshheading:7250146-Phenobarbital,
pubmed-meshheading:7250146-Rats
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pubmed:year |
1980
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pubmed:articleTitle |
Cleavage of digoxigenin digitoxosides by rat liver microsomes.
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pubmed:publicationType |
Journal Article
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