Linked Life Data

3524823

Source:http://linkedlifedata.com/resource/pubmed/id/3524823

Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
6
pubmed:dateCreated
1986-9-18
pubmed:abstractText
In the present study, the biodisposition of 4-demethoxydaunorubicin (4DDM) and its 13-dihydrometabolite was compared with daunorubicin (DM) and its metabolite in rabbit serum, and the results were considered in the light of this DM analog's pharmacokinetic behavior in mice. In rabbit serum, the levels of the 13-OH derivative of both DM and 4DDM (daunorubicinol and 4-demethoxydaunorubicinol) were higher than in mice. In vitro metabolic studies with mouse and rabbit cytosol indicated that the hepatic metabolism was quantitatively important for both analogs (70%-90% for DM and 4DDM was reduced to the 13-OH metabolite), but the rabbit had a much higher specific capacity to metabolize these compounds. DM seemed a better substrate for cytoplasmic aldoketoreductase, the enzyme affinity in rabbits being three times higher than for 4DDM. Cytotoxicity studies in vitro showed that 4-demethoxydaunorubicinol, unlike daunorubicinol, was as cytotoxic as the parent compound, and this suggests this metabolic step does not inactivate 4DDM but contributes to its high and long-lasting biological activity in vivo.
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:month
Jun
pubmed:issn
0361-5960
pubmed:author
pubmed:issnType
Print
pubmed:volume
70
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
697-702
pubmed:dateRevised
2006-11-15
pubmed:meshHeading
pubmed:year
1986
pubmed:articleTitle
Comparative metabolism of daunorubicin and 4-demethoxydaunorubicin in mice and rabbits.
pubmed:publicationType
Journal Article, Comparative Study, In Vitro, Research Support, Non-U.S. Gov't