Effects of plant-derived phenols on rat liver cytochrome P450 2B1 activity

Anticancer Res. May-Jun 2002;22(3):1699-703.


Dietary constituents contain a variety of compounds that are known to modulate liver enzyme activity. In this report, the plant-derived phenols catechin, chlorogenic acid, diosmin, epigallo-catechin gallate (EGCG), naringenin, quercetin and resveratrol were studied for their effects on the activity of cytochrome P450 2B1 in liver microsomes from 6- and 20-month male Fisher F344 rats. The compounds at two concentrations (0.1 and 0.25 mM) were incubated with 0.2 mg liver microsomal protein and 50 microM 7-ethoxy-4-trifluoromethyl coumarin (EFC). O-deethylation of EFC to the fluorescence product 7-hydroxy-4-trifluoromethyl coumarin (HFC) is catalyzed by CYP450 2B1. EGCG, naringenin, quercetin and resveratrol inhibited the in vitro O-deethylation of EFC in liver microsomes from both 6- and 20-month rats. Quercetin was the most effective inhibitor. Catechin inhibited the in vitro O-deethylation of EFC only in microsomes from 6-month-old rats whereas diosmin inhibited the reaction only in microsomes from 20-month-old rats. Chlorogenic acid inhibited the in vitro O-deethylation of EFC in microsomes from both age groups at the 0.25 mM concentration only. These results suggest that plant phenols have varied effects on liver microsomal cytochrome P450 2B1 activity that may be influenced by the age of the animal.

MeSH terms

  • Alkylation / drug effects
  • Animals
  • Catechin / analogs & derivatives
  • Catechin / pharmacology
  • Chlorogenic Acid / pharmacology
  • Coumarins / metabolism
  • Cytochrome P-450 CYP2B1 / antagonists & inhibitors
  • Cytochrome P-450 CYP2B1 / metabolism*
  • Diosmin / pharmacology
  • Flavanones*
  • Flavonoids / pharmacology
  • Fluorescence
  • Male
  • Microsomes, Liver / drug effects*
  • Microsomes, Liver / enzymology*
  • Phenols / pharmacology*
  • Plant Extracts / pharmacology
  • Plants / chemistry
  • Quercetin / pharmacology
  • Rats
  • Rats, Inbred F344
  • Resveratrol
  • Stilbenes / pharmacology


  • Coumarins
  • Flavanones
  • Flavonoids
  • Phenols
  • Plant Extracts
  • Stilbenes
  • 7-ethoxy-4-trifluoromethylcoumarin
  • Chlorogenic Acid
  • 7-hydroxy-4-trifluoromethylcoumarin
  • Diosmin
  • Catechin
  • Quercetin
  • epigallocatechin gallate
  • Cytochrome P-450 CYP2B1
  • naringenin
  • Resveratrol