The bioavailability and distribution of trans-resveratrol are constrained by ABC transporters

Arch Biochem Biophys. 2012 Nov 15;527(2):67-73. doi: 10.1016/ Epub 2012 Jun 26.


The ABC proteins are a family of membrane transporters that mediates the extrusion from cells of a wide variety of structurally unrelated substrates. The current review focuses on the role of these efflux pumps located in the intestine on the low oral bioavailability of trans-resveratrol. The enterocytes hold in the apical membrane three transporters, namely, P-glycoprotein (P-gp), multidrug resistance associated protein 2 (MRP2) and breast cancer resistance protein (BCRP), whereas the basolateral membrane contains multidrug resistance associated protein 3 (MRP3). The use of different specific inhibitors of these transporters as well as knockout mice enabled us to conclude that MRP2 and BCRP are involved in the extrusion of trans-resveratrol glucuronide and sulfate to the intestinal lumen without the participation of P-gp. The role of these transporters as a bottleneck in the absorption of trans-resveratrol cannot be undervalued affecting not only the bioavailability of its glucuronide and sulfate but also their distribution in the different organs.

Publication types

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

MeSH terms

  • ATP-Binding Cassette Transporters / metabolism*
  • Animals
  • Biological Availability
  • Humans
  • Intestinal Absorption
  • Resveratrol
  • Stilbenes / metabolism
  • Stilbenes / pharmacokinetics*


  • ATP-Binding Cassette Transporters
  • Stilbenes
  • Resveratrol