Effect of grapefruit juice, naringin, naringenin, and bergamottin on the intestinal carrier-mediated transport of talinolol in rats

J Agric Food Chem. 2008 Jun 25;56(12):4840-5. doi: 10.1021/jf0728451. Epub 2008 May 22.


The effect of two varieties of grapefruit juice (white and ruby red) and its selected components (naringin, naringenin, and bergamottin) was investigated on the activity of the P-glycoprotein (P-gp) in male Sprague-Dawley rats. Talinolol, a nonmetabolized P-gp substrate, was used as a marker compound. The white grapefruit juice (GFJ) had a minor effect on talinolol pharmacokinetics, but the ruby red GFJ reduced the C max and the AUC (0-infinity) by 60% and 50% of the control, respectively. However, among the GFJ constituents tested, bergamottin (0.22 mg/kg) was the most potent component augmenting the C max and the AUC (0-infinity) of talinolol by 2.4- and 1.8-fold, respectively, if compared to the control group. The flavonoids naringenin (0.7 mg/kg) and naringin (2.4 and 9.4 mg/kg) had a similar effect increasing the talinolol C max and AUC (0-infinity) by 1.5- to 1.8-fold, respectively. In conclusion, the effect of GFJ on P-gp activity seems to depend on the variety, the concentration of compounds in the juice, and the composition of different ingredients.

Publication types

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

MeSH terms

  • ATP Binding Cassette Transporter, Subfamily B, Member 1 / metabolism
  • Animals
  • Beverages / analysis
  • Biological Transport / drug effects
  • Citrus paradisi / chemistry*
  • Flavanones / pharmacology*
  • Fruit / chemistry
  • Furocoumarins / pharmacology*
  • Intestinal Mucosa / metabolism*
  • Male
  • Propanolamines / blood
  • Propanolamines / pharmacokinetics*
  • Rats
  • Rats, Sprague-Dawley
  • Species Specificity


  • ATP Binding Cassette Transporter, Subfamily B, Member 1
  • Flavanones
  • Furocoumarins
  • Propanolamines
  • talinolol
  • naringenin
  • bergamottin
  • naringin