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Related Experiment Videos

Antibiotic exposure does not influence MRP2 functional expression in Caco-2 cells.

Hannah Prime-Chapman1, Vanessa Moore, Barry H Hirst

  • 1Institute for Cell and Molecular Biosciences, University of Newcastle, Medical School, Newcastle upon Tyne NE2 4HH, UK.

Journal of Drug Targeting
|April 26, 2005
PubMed
Summary

Common antibiotics like gentamicin and penicillin-streptomycin do not alter multidrug resistance-associated protein 2 (MRP2) expression or function in Caco-2 cells. This suggests antibiotics do not impact the oral bioavailability of MRP2 drug substrates.

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Area of Science:

  • Pharmacology
  • Cell Biology
  • Drug Metabolism

Background:

  • Multidrug resistance-associated protein 2 (MRP2) actively transports drugs, affecting oral bioavailability.
  • Caco-2 cells are a standard in vitro model for predicting oral drug absorption.
  • Caco-2 cell cultures frequently use antibiotics, potentially influencing MRP2 expression.

Purpose of the Study:

  • To determine if common antibiotic regimens affect MRP2 functional expression in Caco-2 cells.
  • To assess the impact of gentamicin and penicillin-streptomycin on MRP2 activity and protein levels.

Main Methods:

  • Caco-2 cells were cultured with or without gentamicin or penicillin-streptomycin for up to 9 weeks.
  • MRP2 functional activity was measured via calcein efflux assays.

Related Experiment Videos

  • MRP2 protein expression was quantified using immunoblots.

    • Main Results:

    • Neither antibiotic treatment consistently altered calcein efflux across the apical (MRP2) or basolateral membranes.
    • Antibiotic exposure did not lead to significant changes in MRP2 protein expression.
    • No effect on MRP2 functional activity was observed in intestinal enterocytic Caco-2 cells.

    Conclusions:

    • Routine antibiotic use in Caco-2 cell cultures does not affect apical MRP2 functional activity.
    • In vivo, recent antibiotic courses are unlikely to influence the oral bioavailability of MRP2 substrate drugs.