Ezetimib influences the expression of raft-associated antigens in human monocytes

Cytometry A. 2006 Mar;69(3):206-8. doi: 10.1002/cyto.a.20229.

Abstract

Aminopeptidase N (CD13) was recently identified as a molecular target of the cholesterol absorption inhibitor Ezetimib. Regarding that CD13 is expressed in lipid rafts of monocytic cells, we have investigated whether Ezetimib influences raft function in these cells. Expression of raft-associated antigens (CD11b, CD13, CD14, CD16, CD36, and CD64) was followed by flow cytometry and/or immunoblot in human monocyte-derived macrophages in response to in vitro administration of Ezetimib. Cellular redistribution of CD13 was assessed by confocal imaging. Ezetimib significantly decreased the surface expression of CD13, CD16, CD64, and CD36; furthermore, it induced a shift of CD13 from plasma membrane to intracellular vesicles, and thus it quite likely modulated monocytic raft-assembly.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Anticholesteremic Agents / pharmacology
  • Antigens, CD / analysis
  • Antigens, CD / metabolism
  • Antigens, Surface / analysis*
  • Antigens, Surface / metabolism
  • Azetidines / pharmacology*
  • CD11b Antigen / analysis
  • CD11b Antigen / metabolism
  • CD13 Antigens / analysis
  • CD13 Antigens / metabolism
  • CD36 Antigens / analysis
  • CD36 Antigens / metabolism
  • Cell Differentiation / drug effects
  • Cell Membrane / chemistry
  • Cell Membrane / drug effects
  • Cell Membrane / metabolism
  • Ezetimibe
  • Flow Cytometry
  • GPI-Linked Proteins
  • Humans
  • Lipopolysaccharide Receptors / analysis
  • Lipopolysaccharide Receptors / metabolism
  • Macrophage Colony-Stimulating Factor / pharmacology
  • Macrophages / cytology
  • Macrophages / drug effects*
  • Macrophages / metabolism
  • Membrane Microdomains / chemistry
  • Membrane Microdomains / drug effects*
  • Membrane Microdomains / metabolism
  • Microscopy, Fluorescence
  • Monocytes / cytology
  • Monocytes / drug effects
  • Monocytes / metabolism
  • Protein Transport / drug effects
  • Receptors, IgG / analysis
  • Receptors, IgG / metabolism

Substances

  • Anticholesteremic Agents
  • Antigens, CD
  • Antigens, Surface
  • Azetidines
  • CD11b Antigen
  • CD36 Antigens
  • FCGR3B protein, human
  • GPI-Linked Proteins
  • Lipopolysaccharide Receptors
  • Receptors, IgG
  • Macrophage Colony-Stimulating Factor
  • CD13 Antigens
  • Ezetimibe