Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
2
pubmed:dateCreated
1991-3-22
pubmed:abstractText
The hepatotoxicity and uptake mechanism of lithocholate and its glucuronide and sulfate were studied using isolated rat hepatocytes. Cytotoxicity was in the order of lithocholate greater than lithocholate-glucuronide greater than lithocholate-sulfate; their 50% cytotoxic concentrations on hepatocytes were 50, 150 and 700 microM, respectively. Thus, glucuronidation as well as sulfation acted to detoxify lithocholate, not relating to the previously reported higher cholestatic effect of lithocholate-glucuronide than lithocholate. Lithocholate uptake was linear up to 50 microM, whereas the uptakes of lithocholate-glucuronide and sulfate were saturable with an apparent Km and Vmax of 32 microM and 6.4 nmol/min per 10(6) cells for lithocholate-glucuronide and 26 microM and 11.8 nmol/min per 10(6) cells for lithocholate-sulfate. Na+ replacement by choline+ had no effect on the uptake of lithocholate and lithocholate-glucuronide, whereas it slightly inhibited lithocholate-sulfate uptake. Lithocholate-glucuronide uptake was inhibited by lithocholate-sulfate and sulfobromophthalein, whereas lithocholate-glucuronide and sulfobromophthalein had no effect on lithocholate-sulfate uptake. These data indicate that hepatic lithocholate uptake is mediated by simple diffusion, and that hepatic uptake of lithocholate-glucuronide and sulfate is mainly mediated by a Na(+)-independent carrier.
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:month
Jan
pubmed:issn
0006-3002
pubmed:author
pubmed:issnType
Print
pubmed:day
31
pubmed:volume
1091
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
173-8
pubmed:dateRevised
2006-11-15
pubmed:meshHeading
pubmed:year
1991
pubmed:articleTitle
Cytotoxic effect and uptake mechanism by isolated rat hepatocytes of lithocholate and its glucuronide and sulfate.
pubmed:affiliation
Department of Medicine, Teikyo University School of Medicine, Japan.
pubmed:publicationType
Journal Article, Comparative Study