Cell lipid metabolism modulators 2-bromopalmitate, D609, monensin, U18666A and probucol shift discoidal HDL formation to the smaller-sized particles: implications for the mechanism of HDL assembly

Biochim Biophys Acta. 2016 Dec;1861(12 Pt A):1968-1979. doi: 10.1016/j.bbalip.2016.09.017. Epub 2016 Sep 24.

Abstract

ATP-binding cassette transporter A1 (ABCA1) mediates formation of disc-shaped high-density lipoprotein (HDL) from cell lipid and lipid-free apolipoprotein A-I (apo A-I). Discoidal HDL particles are heterogeneous in physicochemical characteristics for reasons that are understood incompletely. Discoidal lipoprotein particles similar in characteristics and heterogeneity to cell-formed discoidal HDL can be reconstituted from purified lipids and apo A-I by cell-free, physicochemical methods. The heterogeneity of reconstituted HDL (rHDL) is sensitive to the lipid composition of the starting lipid/apo A-I mixture. To determine whether the heterogeneity of cell-formed HDL is similarly sensitive to changes in cell lipids, we investigated four compounds that have well-established effects on cell lipid metabolism and ABCA1-mediated cell cholesterol efflux. 2-Bromopalmitate, D609, monensin and U18666A decreased formation of the larger-sized, but dramatically increased formation of the smaller-sized HDL. 2-Bromopalmitate did not appear to affect ABCA1 activity, subcellular localization or oligomerization, but induced dissolution of the cholesterol-phospholipid complexes in the plasma membrane. Arachidonic and linoleic acids shifted HDL formation to the smaller-sized species. Tangier disease mutations and inhibitors of ABCA1 activity wheat germ agglutinin and AG 490 reduced formation of both larger-sized and smaller-sized HDL. The effect of probucol was similar to the effect of 2-bromopalmitate. Taking rHDL formation as a paradigm, we propose that ABCA1 mutations and activity inhibitors reduce the amount of cell lipid available for HDL formation, and the compounds in the 2-bromopalmitate group and the polyunsaturated fatty acids change cell lipid composition from one that favors formation of the larger-sized HDL particles to one that favors formation of the smaller-sized species.

Keywords: HDL heterogeneity; Inhibitors of ABCA1-mediated cholesterol efflux; Mechanism of HDL formation; Reconstituted HDL; Tangier disease mutations.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't

MeSH terms

  • ATP Binding Cassette Transporter 1 / metabolism
  • Androstenes / pharmacology*
  • Animals
  • Apolipoprotein A-I / metabolism
  • Bridged-Ring Compounds / pharmacology*
  • Cell Line
  • Cell Line, Tumor
  • Cell Membrane / drug effects
  • Cell Membrane / metabolism
  • Cholesterol / metabolism
  • Fatty Acids, Unsaturated / metabolism
  • Humans
  • Lipid Metabolism / drug effects*
  • Lipoproteins, HDL / metabolism*
  • Macrophages / metabolism
  • Mice
  • Monensin / pharmacology*
  • Norbornanes
  • Palmitates / pharmacology*
  • Particle Size
  • Phospholipids / metabolism
  • Probucol / pharmacology*
  • RAW 264.7 Cells
  • Thiocarbamates
  • Thiones / pharmacology*

Substances

  • ATP Binding Cassette Transporter 1
  • Androstenes
  • Apolipoprotein A-I
  • Bridged-Ring Compounds
  • Fatty Acids, Unsaturated
  • Lipoproteins, HDL
  • Norbornanes
  • Palmitates
  • Phospholipids
  • Thiocarbamates
  • Thiones
  • 2-bromopalmitate
  • 3-beta-(2-(diethylamino)ethoxy)androst-5-en-17-one
  • tricyclodecane-9-yl-xanthogenate
  • Monensin
  • Cholesterol
  • Probucol