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Bromocriptine modulates P-glycoprotein function

S Orlowski1, D Valente, M Garrigos

  • 1Section de Biophysique des Protéines et des Membranes, DBCM, CEA, Centre d'Etudes de Saclay, Gif/Yvette, France. orlowski@dsvidf.cea.fr

Biochemical and Biophysical Research Communications
|March 26, 1998
PubMed
Summary
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Bromocriptine (BCT) partially reverses multidrug resistance (MDR) mediated by P-glycoprotein (P-gp). BCT inhibits P-gp

Area of Science:

  • Biochemistry
  • Pharmacology
  • Cell Biology

Background:

  • Multidrug resistance (MDR) is often mediated by P-glycoprotein (P-gp), a membrane transporter.
  • P-gp effluxes various amphiphilic molecules, including cytotoxic drugs and reversing agents.
  • Bromocriptine (BCT) is an ergot alkaloid with known D2 dopaminergic receptor agonist activity.

Purpose of the Study:

  • To investigate the effects of bromocriptine (BCT) on P-glycoprotein (P-gp) function.
  • To determine if BCT can modulate P-gp-mediated drug transport and ATPase activity.

Main Methods:

  • Utilized Chinese hamster lung fibroblasts (DC-3F/ADX) exhibiting MDR.
  • Prepared P-gp-containing membrane vesicles for biochemical assays.
  • Assessed basal and drug-stimulated P-gp MgATPase activity in the presence of BCT and its metabolites.

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Main Results:

  • BCT (4 microM) partially reversed vincristine resistance in MDR cells.
  • BCT inhibited basal P-gp MgATPase activity with an IC50 of 0.30 +/- 0.15 microM.
  • BCT exhibited competitive inhibition of verapamil-stimulated ATPase and non-competitive inhibition of progesterone- and vinblastine-stimulated ATPase.

Conclusions:

  • BCT interacts specifically with P-gp, likely inhibiting its drug transport function.
  • BCT's modulatory effects on P-gp ATPase activity suggest a role in overcoming MDR.
  • Hydroxylated BCT metabolites show varied effects, with monohydroxylated forms impacting P-gp ATPase activity.