Pitavastatin increases ABCA1-mediated lipid efflux from Fu5AH rat hepatoma cells

Biochem Biophys Res Commun. 2004 Aug 27;321(3):670-4. doi: 10.1016/j.bbrc.2004.07.020.


ATP binding cassette A1 (ABCA1) is responsible in vivo for the formation of HDL by promoting the lipidation of apoprotein A-I (apoA-I) via cholesterol and phospholipid efflux from the liver. Treatment of patients with statins produces an increase in HDL plasma level, but the underlying mechanism is not completely understood. In this work we investigated the ability of pitavastatin to modulate ABCA1-mediated efflux from Fu5AH rat hepatoma cells, that here we demonstrate to express functional ABCA1 upon treatment with 22OH/cRA. In both basal and ABCA1 expressing cells pitavastatin 0.1-50microM induced a dose-dependent increase in cholesterol efflux to apoA-I; this effect was reversed by mevalonate or geranyl geraniol. A stimulatory effect was also observed on phospholipid efflux. Similar results were obtained with compactin, suggesting a class-related effect of statins. These results indicate a potential mechanism for the improvement in HDL plasma profile observed in patients treated with statins.

Publication types

  • Research Support, Non-U.S. Gov't
  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • ATP Binding Cassette Transporter 1
  • ATP-Binding Cassette Transporters / metabolism*
  • Animals
  • Biological Transport
  • Carcinoma, Hepatocellular / metabolism
  • Cell Line, Tumor
  • Cholesterol / metabolism
  • Diterpenes / metabolism
  • Dose-Response Relationship, Drug
  • Enzyme Inhibitors / pharmacology*
  • Humans
  • Lipid Metabolism*
  • Liver Neoplasms / metabolism
  • Mevalonic Acid / metabolism
  • Quinolines / pharmacology*
  • Rats


  • ABCA1 protein, human
  • ATP Binding Cassette Transporter 1
  • ATP-Binding Cassette Transporters
  • Diterpenes
  • Enzyme Inhibitors
  • Quinolines
  • Cholesterol
  • geranylgeraniol
  • pitavastatin
  • Mevalonic Acid