Kaempferol activates human steroid and xenobiotic receptor-mediated cytochrome P450 3A4 transcription / 浙江大学学报·医学版
Journal of Zhejiang University. Medical sciences
;
(6): 14-17, 2006.
Article
in Chinese
| WPRIM
| ID: wpr-355153
ABSTRACT
<p><b>OBJECTIVE</b>To investigate whether kaempferol stimulates pregnane X receptor (PXR)-mediated transcription of CYP3A4.</p><p><b>METHODS</b>Transient cotransfection reporter gene assay was performed with PXR expression plasmid and a reporter plasmid containing the XREs in the CYP3A4 gene promoter in HepG(2)cells.</p><p><b>RESULTS</b>Kaempferol activated PXR-mediated transcription of CYP3A4 in a dose, time-dependent manner. In the dose-response study, kaempferol exposure at concentrations of 1.0 x 10(-3), 1.0 x 10(-2), 0.1, 1.0 and 10.0 mol/L for 24 h increased CYP3A4 transcription by (1.31+/-0.27), (1.45+/-0.36), (1.96+/-0.50), (2.90+/-1.07) and (7.93+/-0.75) fold, respectively compared with 0.1% DMSO (P<0.05). The results from time-course study showed that after 48 h exposure 1.0 and 10.0 mol/L of kaempferol enhanced the transcription of CYP3A4 by (3.73+/-1.21) fold and (8.42+/-1.47) fold, respectively.</p><p><b>CONCLUSION</b>Kaempferol may be a human CYP3A4 gene inducer through PXR, and may affect the metabolism of a large number of substrates of CYP3A4 simultaneously taken.</p>
Full text:
Available
Index:
WPRIM (Western Pacific)
Main subject:
Pathology
/
Pharmacology
/
Transcription, Genetic
/
Tumor Cells, Cultured
/
Transfection
/
Receptors, Steroid
/
Genes, Reporter
/
Carcinoma, Hepatocellular
/
Cytochrome P-450 Enzyme System
/
Kaempferols
Limits:
Humans
Language:
Chinese
Journal:
Journal of Zhejiang University. Medical sciences
Year:
2006
Type:
Article
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