Grapefruit juice-drug interactions: Grapefruit juice and its components inhibit P-glycoprotein (ABCB1) mediated transport of talinolol in Caco-2 cells. Academic Article uri icon


  • To investigate the potential interaction between selected ingredients of grapefruit juice and, the transport of talinolol, a P-gp substrate, across Caco-2 cells monolayers was determined in the absence and presence of distinct concentrations of grapefruit juice, bergamottin, 6',7'-dihydroxybergamottin, 6',7'-epoxybergamottin, naringin, and naringenin. Talinolol permeability was selectively inhibited by grapefruit juice and its components. The furano coumarin, 6',7'-epoxybergamottin, was the most potent inhibitor (IC(50) = 0.7 microM), followed by 6',7'-dihydroxybergamottin (IC(50) = 34 microM) and bergamottin that did not show any inhibition at concentrations up to 10 microM. The flavonoid aglycone naringenin was around 10-fold more potent than its glycoside naringin with IC(50) values of 236 and 2409 microM, respectively. The flavonoids and furanocoumarins tested in this study are in the same range of concentration they are present in the juice contributing, therefore, for the overall inhibitory effect of GFJ on P-gp activity. The in vitro data suggest that compounds present in grapefruit juice are able to inhibit the P-gp activity modifying the disposition of drugs that are P-gp substrates such as talinolol.

published proceedings

  • J Pharm Sci

altmetric score

  • 0.25

author list (cited authors)

  • de Castro, W. V., Mertens-Talcott, S., Derendorf, H., & Butterweck, V.

citation count

  • 73

complete list of authors

  • de Castro, Whocely Victor||Mertens-Talcott, Susanne||Derendorf, Hartmut||Butterweck, Veronika

publication date

  • May 2007