Effects of kaempferol and quercetin on cytochrome 450 activities in primarily cultured rat hepatocytes / 浙江大学学报·医学版
Journal of Zhejiang University. Medical sciences
;
(6): 18-22, 2006.
Article
in Chinese
| WPRIM
| ID: wpr-355152
ABSTRACT
<p><b>OBJECTIVE</b>To observe the effects of kaempferol and quercetin on the activity of cytochrome P450 in rat hepatocytes.</p><p><b>METHODS</b>Primarily cultured rat hepatocytes were exposed to kaempferol or quercetin in concentrations of 0.1, 1, 10 micromol/L for 12 h, 24 h and 48 h. Hepatocytes CYP isoemzymes-erythromycin N-demethylase (ERND) and aminopyrine N-demethylase (ADM) activities were determined by Nash methods. Erythromycin (10 micromol/L) was used as positive control and DMSO(0.1%) as solvent control.</p><p><b>RESULTS</b>Kaempferol and quercetin inhibited ENRD activity in a dose-and time-dependent manner. In dose-response study, the ENRD activities in kaempferol (0.1,1 and 10 micromol/L) treated groups were (0.088+/-0.008), (0.074+/-0.006) and (0.041+/-0.003)micromol/(mg.min(-1)), respectively. ENRD activity in quercetin treated groups at the same concentrations were (0.082+/-0.007), (0.063+/-0.007) and (0.034+/-0.005) micromol/(mg.min(-1)), respectively. In time-courses study, the ENRD activity exposed to 10 micromol/L kaempferol or quercetin for 12 h and 48 h were (0.053+/-0.006) and (0.037+/-0.007) micromol/(mg.min(-1)), or (0.067+/-0.005) and (0.032+/-0.004) micromol/(mg.min(-1)). ADM activity was inhibited only by kaempferol in 10 mol/L at 24 h, but was not significantly altered by quercetin at any concentration tested.</p><p><b>CONCLUSION</b>In the present condition, kaempferol and quercetin act as potential CYP3A4 inhibitors as they can significantly inhibit ENRD in primarily cultured rat hepatocytes.</p>
Full text:
Available
Index:
WPRIM (Western Pacific)
Main subject:
Pathology
/
Pharmacology
/
Quercetin
/
Tumor Cells, Cultured
/
Carcinoma, Hepatocellular
/
Hepatocytes
/
Cytochrome P-450 Enzyme System
/
Kaempferols
/
Dose-Response Relationship, Drug
/
Cytochrome P-450 CYP3A
Limits:
Animals
Language:
Chinese
Journal:
Journal of Zhejiang University. Medical sciences
Year:
2006
Type:
Article
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