Plant phenols as in vitro inhibitors of glutathione S-transferase(s)

Biochem Biophys Res Commun. 1984 Apr 30;120(2):427-33. doi: 10.1016/0006-291x(84)91271-3.

Abstract

Ellagic acid, a commonly occurring plant phenol, was shown to be a potent in vitro inhibitor of GSH-transferase(s) activity. Other plant phenols such as ferrulic acid, caffeic acid and chlorogenic acid also showed a concentration dependent inhibition of GSH-transferase(s) activity. The I50 values of ellagic acid, caffeic acid, chlorogenic acid and ferrulic acid were 8.3 X 10(-5)M, 14.0 X 10(-5)M, 20.0 X 10(-5)M and 22.0 X 10(-5)M respectively, suggesting that ellagic acid is the most potent inhibitor of all the four studied plant phenols. At 55 microM concentration of ellagic acid, a significant inhibition (35-47%) was observed on GSH-transferase activity towards CDNB, p-nitrobenzyl chloride and 1,2-epoxy-3-(p-nitrophenoxy)propane as substrates. Ellagic acid inhibited GSH-transferase(s) activity in a non-competitive manner with respect to CDNB while with respect to GSH it inhibited the enzyme activity in a competitive manner. Other phenolic compounds purpurogallin , quercetin, alizarin and monolactone also showed a concentration dependent inhibition of the enzyme activity with a I50 of 0.8 X 10(-5)M, 1.0 X 10(-5)M, 8.0 X 10(-5)M and 16.0 X 10(-5)M respectively. These inhibitors of GSH-transferase(s) activity should be useful in studying the in vitro enzyme mediated reactions of exogenous and endogenous compounds.

Publication types

  • Comparative Study
  • Research Support, U.S. Gov't, Non-P.H.S.
  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Animals
  • Caffeic Acids / pharmacology
  • Carboxylic Acids / pharmacology*
  • Chlorogenic Acid / pharmacology
  • Coumaric Acids / pharmacology
  • Dinitrochlorobenzene / metabolism
  • Dose-Response Relationship, Drug
  • Ellagic Acid / pharmacology
  • Glutathione Transferase / antagonists & inhibitors*
  • Liver / enzymology*
  • Plants / analysis*
  • Rats

Substances

  • Caffeic Acids
  • Carboxylic Acids
  • Coumaric Acids
  • Dinitrochlorobenzene
  • Ellagic Acid
  • Chlorogenic Acid
  • ferulic acid
  • Glutathione Transferase
  • caffeic acid