[Effects of kaempferol and quercetin on cytochrome 450 activities in primarily cultured rat hepatocytes]

Zhejiang Da Xue Xue Bao Yi Xue Ban. 2006 Jan;35(1):18-22.
[Article in Chinese]

Abstract

Objective: To observe the effects of kaempferol and quercetin on the activity of cytochrome P450 in rat hepatocytes.

Methods: 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.

Results: 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.

Conclusion: In the present condition, kaempferol and quercetin act as potential CYP3A4 inhibitors as they can significantly inhibit ENRD in primarily cultured rat hepatocytes.

Publication types

  • English Abstract
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Aminopyrine N-Demethylase / metabolism
  • Animals
  • Carcinoma, Hepatocellular / enzymology
  • Cytochrome P-450 CYP3A / metabolism*
  • Cytochrome P-450 Enzyme System / metabolism*
  • Dose-Response Relationship, Drug
  • Hepatocytes / metabolism
  • Kaempferols / pharmacology*
  • Liver Neoplasms / enzymology*
  • Liver Neoplasms / pathology
  • Quercetin / pharmacology*
  • Rats
  • Tumor Cells, Cultured

Substances

  • Kaempferols
  • kaempferol
  • Cytochrome P-450 Enzyme System
  • Quercetin
  • Cytochrome P-450 CYP3A
  • Aminopyrine N-Demethylase