Editor's Note
Vaccinium myrtillus  L. (bilberry) fruit is a berry with a high content of anthocyanins, bioactive secondary metabolites that are considered to play a major role in the health-promoting properties of bilberries.   in vivo  study was designed to assess the possible influence of bilberry extract on drug-metabolizing enzymes (DMEs). The authors conclude that the consumption of bilberries as a food supplement should not pose a risk of interacting with co-administered drugs based on their metabolism.
Highlights
  • Bilberry extract administered to rats in water affected few biochemical parameters, generally without clinical consequences.
  • Physiological, hematological and antioxidant parameters remained at control levels.
  • Cytochromes P450 were modulated mildly or not at all (with the exception of CYP2E1 and CYP2C11 activity).
  • Bilberries consumption had very low, if any, potential to affect carbonyl-reducing or conjugating enzymes.

Abstract
Vaccinium myrtillus  L. (bilberry) fruit is a blue-colored berry with a high content of anthocyanins. These bioactive secondary metabolites are considered to play a major role in the health-promoting properties of bilberries. Our  in vivo  study was designed to assess the possible influence of bilberry extract on drug-metabolizing enzymes (DMEs). Rats were exposed to bilberry extract in drinking water at two concentrations (0.15 and 1.5 g/L). Selected DMEs were determined (mRNA expression and enzymatic activity) after 29 and 58 days in rat liver. In addition, a panel of antioxidant, physiological, biochemical and hematological parameters was studied; these parameters did not demonstrate any impact of bilberry extract on the health status of rats. A significant increase in activity was observed in cytochrome P450 (CYP) 2C11 (131% of control) and CYP2E1 (122% of control) after a 29-day administration, while the consumption of a higher concentration for a longer time led to a mild activity decrease. Slight changes were observed in some other DMEs, but they remained insignificant from a physiological perspective. According to our results, we conclude that the consumption of bilberries as a food supplement should not pose a risk of interacting with co-administered drugs based on their metabolism.