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Genistein and Glyceollin Effects on ABCC2 (MRP2) and ABCG2 (BCRP) in Caco-2 Cells

Chandler Schexnayder1, Robert E Stratford2

  • 1Department of Basic Pharmaceutical Sciences, College of Pharmacy, Xavier University of Louisiana, New Orleans, LA 70125, USA. cschexn2@xula.edu.

International Journal of Environmental Research and Public Health
|December 26, 2015
PubMed

Insights

Soy phytoestrogens called glyceollins inhibit intestinal drug transporters ATP Binding Cassette C2 (MRP2) and ATP Binding Cassette G2 (BCRP). This suggests glyceollins may affect the absorption of co-administered drugs and phytochemicals.

Area of Science:

  • Pharmacology
  • Nutritional Science
  • Cell Biology

Background:

  • Glyceollins are soy-derived phytoestrogens with known anti-proliferative properties.
  • Intestinal drug transporters, including MRP2 and BCRP, play crucial roles in drug absorption and bioavailability.
  • Understanding the interactions between dietary compounds and these transporters is vital for predicting drug efficacy and safety.

Purpose of the Study:

  • To investigate the effects of glyceollins on the function of intestinal ATP Binding Cassette C2 (MRP2) and ATP Binding Cassette G2 (BCRP) transporters.
  • To compare the effects of glyceollins with genistein on these transporters.
  • To assess the potential impact of glyceollins on the absorption of co-administered substances.

Main Methods:

  • Utilized the Caco-2 cell intestinal epithelial cell model.
  • Assessed MRP2 function using 5 (and 6)-carboxy-2',7'-dichloroflourescein (CDF) as a substrate.
  • Evaluated BCRP function using BODIPY-prazosin as a substrate.
  • Compared glyceollin activity with known inhibitors (MK-571 for MRP2, Ko143 for BCRP) and genistein.

Main Results:

  • Glyceollins significantly inhibited MRP2-mediated CDF transport, comparable to the MRP2 inhibitor MK-571.
  • Glyceollins demonstrated concentration-dependent inhibition of BCRP-mediated BODIPY-prazosin efflux, similar in potency to the BCRP inhibitor Ko143.
  • In contrast, genistein did not significantly affect MRP2 activity and showed a modest increase in BCRP efflux.

Conclusions:

  • Glyceollins inhibit key intestinal efflux transporters MRP2 and BCRP.
  • These inhibitory effects suggest glyceollins could alter the absorption of co-administered phytochemicals and pharmaceuticals.
  • Further research is warranted to elucidate the clinical implications of glyceollin-transporter interactions on drug bioavailability.
Keywords:
BCRPMRP2drug-food interactiongenisteinglyceollinisoflavonoidsphytoestrogen

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