Tamoxifen decreases cholesterol sevenfold and abolishes lipid lesion development in apolipoprotein E knockout mice

Circulation. 1997 Mar 18;95(6):1542-8. doi: 10.1161/01.cir.95.6.1542.

Abstract

Background: Apolipoprotein E (apo E) knockout mice develop severe vascular lipid lesions resembling human atherosclerotic plaques, irrespective of the fat content of their diet.

Methods and results: Oral tamoxifen (TMX) at a dose of 1.9 mg.kg body wt-1.d-1 abolished lipid lesion development, assayed by oil red O staining, whether the mice were fed a normal diet or a diet with high fat content. The TMX-treated mice showed a sevenfold decrease in total cholesterol. However, the proportion of plasma cholesterol present in VLDL remained unchanged, whereas the proportion in LDL decreased by 37%, and that in HDL increased by 64%. Consistent with the shift from LDL to HDL cholesterol, there was a 62% decrease in total triglycerides. The concentrations of active and acid-activatable latent plus active TGF-beta in the aorta were substantially elevated by TMX (87% and 24% increase, respectively).

Conclusions: Although the mechanism of cardiovascular protection by TMX in apo E knockout mice is unknown, the inhibition of lipid lesion formation may be attributable to the changes in lipoprotein profile and the elevated levels of TGF-beta, both of which are thought to be protective against atherosclerosis in humans and animal models.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Anticholesteremic Agents / pharmacology*
  • Apolipoproteins E / genetics*
  • Blood Vessels / drug effects*
  • Blood Vessels / metabolism
  • Blood Vessels / pathology
  • Cell Differentiation / drug effects
  • Cholesterol / blood*
  • Dietary Fats / pharmacology*
  • Lipoproteins / blood
  • Male
  • Mice
  • Mice, Knockout / physiology*
  • Tamoxifen / pharmacology*
  • Transforming Growth Factor beta / metabolism

Substances

  • Anticholesteremic Agents
  • Apolipoproteins E
  • Dietary Fats
  • Lipoproteins
  • Transforming Growth Factor beta
  • Tamoxifen
  • Cholesterol