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Metformin Impedes Oxidation of LDL In Vitro

Christine Rossmann1, Cornelia Ranz1, Gerd Kager1

  • 1Division of Medicinal Chemistry, Otto Loewi Research Centre, Medical University of Graz, 8010 Graz, Austria.

Pharmaceutics
|August 26, 2023
PubMed

Insights

Metformin, a common diabetes drug, was found to significantly impede low-density lipoprotein (LDL) oxidation. This suggests metformin may help prevent atherosclerosis and cardiovascular disease by protecting against LDL damage.

Area of Science:

  • Biochemistry
  • Cardiovascular Science
  • Pharmacology

Background:

  • Type 2 diabetes is prevalent, with metformin as a primary treatment.
  • Oxidation of low-density lipoprotein (LDL) is a key factor in endothelial dysfunction and atherosclerosis.
  • Understanding agents that can impede LDL oxidation is crucial for cardiovascular disease (CVD) prevention.

Purpose of the Study:

  • To investigate metformin's potential to inhibit LDL oxidation.
  • To assess the impact of metformin on the cytotoxic effects of oxidized LDL (oxLDL).

Main Methods:

  • LDL oxidation induced by CuCl2 in the presence of varying metformin concentrations.
  • Assessment of LDL oxidation via lipid hydroperoxides, malondialdehyde, electrophoretic mobility, and immune epitopes.
  • Evaluation of oxLDL cytotoxicity on EA.hy926 vascular endothelial cells using alamarBlue assay.
  • Quantum chemical calculations to determine reaction energetics between metformin and lipid oxidation radicals.

Main Results:

  • Metformin demonstrated a dose-dependent inhibition of LDL oxidation markers (lipid hydroperoxides, malondialdehyde, immune epitopes).
  • Metformin reduced the cytotoxicity of LDL oxidized in its presence.
  • Quantum chemical analysis indicated metformin primarily scavenges hydroxyl radicals, with endergonic reactions against hydroperoxyl and superoxide radicals.

Conclusions:

  • Metformin effectively impedes LDL oxidation, likely through scavenging hydroxyl radicals.
  • Beyond its glucose-lowering effects, metformin may offer protective benefits against atherosclerosis and associated CVD.
  • Metformin's anti-atherosclerotic potential warrants further investigation.
Keywords:
antioxidantsatherosclerosiscopper ionsdiabeteslipid oxidationlow density lipoprotein

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