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Using Caco-2 Cells to Study Lipid Transport by the Intestine
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Glyceollin Effects on MRP2 and BCRP in Caco-2 Cells, and Implications for Metabolic and Transport Interactions

Chukwuemezie Chimezie1, Adina Ewing1, Chandler Schexnayder1

  • 1Department of Basic Pharmaceutical Sciences, College of Pharmacy, Xavier University of Louisiana, New Orleans, Louisiana 70125.

Journal of Pharmaceutical Sciences
|August 22, 2015
PubMed

Insights

Glyceollins from soybeans impact intestinal drug transporters MRP2 and BCRP, affecting how the body processes compounds. This study reveals glyceollins inhibit these transporters, potentially influencing drug efficacy and interactions.

Area of Science:

  • Pharmacology
  • Biochemistry
  • Nutraceuticals

Background:

  • Glyceollins are soybean phytoalexins with therapeutic potential for cancer, diabetes, and cardiovascular diseases.
  • Understanding their intestinal disposition is crucial for therapeutic applications and predicting interactions.

Purpose of the Study:

  • To investigate the effects of glyceollins on apical efflux transporters MRP2 and BCRP in Caco-2 cells.
  • To determine if glyceollins influence the transport of substrates for MRP2 and BCRP.

Main Methods:

  • Utilized Caco-2 cell models to assess glyceollins' impact on MRP2 and BCRP.
  • Employed 5-(and 6)-carboxy-2',7'-dichloroflourescein (CDF) for MRP2 activity and BODIPY-prazosin for BCRP activity.
  • Evaluated glyceollins' effect on genistein metabolite efflux.

Main Results:

  • Glyceollins demonstrated concentration-dependent reversal of MRP2-mediated CDF transport.
  • Glyceollins exhibited concentration-dependent inhibition of BCRP-mediated BODIPY-prazosin efflux.
  • Glyceollin did not alter MRP2 or BCRP expression after 24-hour exposure; interaction was with genistein metabolism, not metabolite transport.

Conclusions:

  • Glyceollins directly inhibit intestinal efflux transporters MRP2 and BCRP.
  • These findings suggest glyceollins may influence the absorption and efficacy of co-administered drugs.
  • Further research is needed to elucidate the clinical implications of glyceollin-transporter interactions.
Keywords:
active transportdrug interactionefflux pumpsflavonoidsfood effectsgenisteinglyceollinintestinal absorptionintestinal metabolismphytoestrogen

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