title: Effect of grapefruit juice, naringin, naringenin, and bergamottin on the intestinal carrier-mediated transport of talinolol in rats.
abstract: 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.
authors.affiliation: Department of Pharmaceutics, College of Pharmacy, University of Florida, 1600 SW Archer Road, P.O. Box 100494, Gainesville, FL 32610, USA.
authors.forename: Whocely Victor
authors.initials: WV
authors.lastname: de Castro
authors.forename: Susanne
authors.initials: S
authors.lastname: Mertens-Talcott
authors.forename: Hartmut
authors.initials: H
authors.lastname: Derendorf
authors.forename: Veronika
authors.initials: V
authors.lastname: Butterweck
mesh_terms: D020168:ATP Binding Cassette Transporter, Subfamily B, Member 1 / Q000378:metabolism; D000818:Animals; D001628:Beverages / Q000032:analysis; D001692:Biological Transport / Q000187:drug effects; D032083:Citrus paradisi / Q000737:chemistry*; D044950:Flavanones / Q000494:pharmacology*; D005638:Fruit / Q000737:chemistry; D011564:Furocoumarins / Q000494:pharmacology*; D007413:Intestinal Mucosa / Q000378:metabolism*; D008297:Male; D011412:Propanolamines / Q000097:blood / Q000493:pharmacokinetics*; D051381:Rats; D017207:Rats, Sprague-Dawley; D013045:Species Specificity
chemical_list: D020168:ATP Binding Cassette Transporter, Subfamily B, Member 1; D044950:Flavanones; D011564:Furocoumarins; D011412:Propanolamines; C011550:talinolol; C005273:naringenin; C068337:bergamottin; C005274:naringin