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Effects of oral anorexiant sibutramine on the expression of cytochromes P450s in human hepatocytes and cancer cell lines
R. Vrzal, B. Knoppová, P. Bachleda, Z. Dvořák,
Language English Country United States
Document type Journal Article, Research Support, Non-U.S. Gov't
Grant support
NT13591
MZ0
CEP Register
Digital library NLK
Full text - Article
Source
NLK
Medline Complete (EBSCOhost)
from 2012-06-01 to 1 year ago
PubMed
24038852
DOI
10.1002/jbt.21516
Knihovny.cz E-resources
- MeSH
- Cyclobutanes pharmacology MeSH
- Hepatocytes drug effects enzymology MeSH
- Isoenzymes biosynthesis MeSH
- Real-Time Polymerase Chain Reaction MeSH
- Anti-Obesity Agents pharmacology MeSH
- Humans MeSH
- RNA, Messenger genetics isolation & purification MeSH
- Cell Line, Tumor MeSH
- Primary Cell Culture MeSH
- Cytochrome P-450 Enzyme System biosynthesis MeSH
- Blotting, Western MeSH
- Check Tag
- Humans MeSH
- Publication type
- Journal Article MeSH
- Research Support, Non-U.S. Gov't MeSH
Sibutramine is a serotonin-norepinephrine reuptake inhibitor that was used for weight-loss management in obese patients. Even though it was officially withdrawn from the market in 2010, it is still present in some tainted weight-loss pills (as reported by US Food and Drug Administration). Thus, it is still reasonable to study the effects of this compound. The aim of this work was to investigate the potential of sibutramine to induce CYP1A1/CY3A4 in human cancer cell lines and CYP1A1/2, CYP2A6, CYP2B6, and CYP3A4 in human hepatocytes, a competent model of metabolically active cells. The levels of mRNA and protein of CYP1A1/1A2/3A4/2A6/2B6 were compared with the typical inducers, 2,3,7,8-tetrachlorodibenzo-p-dioxin (TCDD) and rifampicin (RIF) for CYP1A1/2 and for other CYPs, respectively. The mRNA and protein levels of all genes in either cancer cell lines or human hepatocytes were induced when treated with typical inducers but not with sibutramine.
References provided by Crossref.org
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