Human apolipoprotein AI mimetic peptides for the treatment of atherosclerosis

Curr Opin Investig Drugs. 2003 Sep;4(9):1100-4.

Abstract

The effects of apolipoprotein (Apo) AI mimetic peptide synthesized from D- and L-amino acids on atherosclerotic lesion formation were investigated in low-density lipoprotein (LDL) receptor-deficient mice on a Western diet and in apoE null mice. In addition, their effects on the inflammatory changes induced in LDL-receptor mice fed a Western diet following influenza A infection were studied. When apolipoprotein AI mimetic peptides synthesized from either D- or L-amino acids were administered to LDL-receptor null mice, only peptides synthesized from D-amino acids were stable in the circulation and enhanced the ability of high-density lipoprotein (HDL) to protect LDL against oxidation. Administration of the peptide D-4F to LDL-receptor null mice and apoE null mice decreased lesion size. Additionally, in LDL receptor null mice after influenza infection, D-4F treatment increased plasma HDL levels and paraoxonase activity, and inhibited increased in LDL-cholesterol and peak levels of interleukin-6 post-infection. Injection of female mice with male macrophages, and subsequent measurement of the male 'sry' gene, revealed a marked increase in macrophage traffic into the aortic arch after infection that was prevented by administration of D-4F. This indicates that: (i) oral D-4F has powerful anti-atherosclerotic properties, and (ii) the loss of the anti-inflammatory properties of HDL after influenza infection in mice is associated with increased arterial macrophage traffic that can be prevented by administration of D-4F.

Publication types

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

MeSH terms

  • Animals
  • Apolipoprotein A-I / therapeutic use*
  • Arteriosclerosis / complications
  • Arteriosclerosis / drug therapy*
  • Arteriosclerosis / metabolism
  • Arteriosclerosis / physiopathology
  • Cholesterol, HDL / blood
  • Cholesterol, LDL / blood
  • Disease Models, Animal
  • Humans
  • Influenza, Human / complications
  • Influenza, Human / metabolism
  • Receptors, LDL / genetics
  • Receptors, LDL / metabolism
  • Vasodilation / drug effects

Substances

  • Apolipoprotein A-I
  • Cholesterol, HDL
  • Cholesterol, LDL
  • D-4F peptide
  • Receptors, LDL