Decrease of P-glycoprotein activity in K562/ADR cells by MbetaCD and filipin and lack of effect induced by cholesterol oxidase indicate that this transporter is not located in rafts

J Bioenerg Biomembr. 2004 Dec;36(6):533-43. doi: 10.1007/s10863-004-9000-8.

Abstract

The effect of low-density membrane domains on function of the plasma membrane transporter P-glycoprotéine (P-gp), involved in multidrug resistance (MDR) phenotype, has been investigated in K562/ADR cells. To this end we reversibly altered the cholesterol content of K562/ADR cells by using methyl-beta-cyclodextrin as a cholesterol chelator and conversely we repleted them through incubation with cholesterol in culture medium. We also used the cholesterol-binding fluorochrome filipin and cholesterol oxidase. Our data show that either cholesterol depletion or complex formation with filipin resulted in a strong decrease of P-gp activity. However, when cells were incubated with cholesterol oxidase that are known to disrupt rafts, no modification of the P-gp activity was observed. In addition, using a free-detergent methodology to separate by ultracentrifugation, "light," "heavy," and "extra heavy" fractions we show that no P-gp is found in the "light" fraction where rafts are usually detected. Altogether, our data strongly suggest that, in this cell line, P-gp is not localized in rafts.

Publication types

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

MeSH terms

  • ATP Binding Cassette Transporter, Subfamily B, Member 1 / metabolism*
  • Anthracyclines / metabolism
  • Blotting, Western
  • Cell Membrane Permeability / drug effects
  • Cholesterol / metabolism*
  • Cholesterol Oxidase / metabolism*
  • Cholesterol Oxidase / pharmacology
  • Doxorubicin / metabolism
  • Drug Resistance, Multiple / physiology*
  • Filipin / metabolism*
  • Filipin / pharmacology
  • Humans
  • Protein Transport / drug effects
  • Spectrometry, Fluorescence
  • Sphingolipid Activator Proteins / metabolism
  • Tumor Cells, Cultured
  • beta-Cyclodextrins / metabolism*
  • beta-Cyclodextrins / pharmacology

Substances

  • ATP Binding Cassette Transporter, Subfamily B, Member 1
  • Anthracyclines
  • Sphingolipid Activator Proteins
  • beta-Cyclodextrins
  • methyl-beta-cyclodextrin
  • Doxorubicin
  • Filipin
  • Cholesterol
  • Cholesterol Oxidase