Direct and indirect antioxidant properties of α-lipoic acid and therapeutic potential

Mol Nutr Food Res. 2013 Jan;57(1):114-25. doi: 10.1002/mnfr.201200608.


Diabetes has emerged as a major threat to worldwide health. The exact mechanisms underlying the disease are unknown; however, there is growing evidence that the excess generation of reactive oxygen species (ROS) associated with hyperglycemia, causes oxidative stress in a variety of tissues. In this context, various natural compounds with pleiotropic actions like α-lipoic acid (LA) are of interest, especially in metabolic diseases such as diabetes. LA, either as a dietary supplement or a therapeutic agent, modulates redox potential because of its ability to match the redox status between different subcellular compartments as well as extracellularly. Both the oxidized (disulfide) and reduced (di-thiol: dihydro-lipoic acid, DHLA) forms of LA show antioxidant properties. LA exerts antioxidant effects in biological systems through ROS quenching but also via an action on transition metal chelation. Dietary supplementation with LA has been successfully employed in a variety of in vivo models of disease associated with an imbalance of redox status: diabetes and cardiovascular diseases. The complex and intimate association between increased oxidative stress and increased inflammation in related disorders such as diabetes, makes it difficult to establish the temporal sequence of the relationship.

Publication types

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

MeSH terms

  • Animals
  • Antioxidants / pharmacology*
  • Cardiovascular Diseases / drug therapy
  • Cardiovascular Diseases / prevention & control
  • Chelating Agents / metabolism
  • Diabetes Mellitus / drug therapy
  • Diabetes Mellitus / prevention & control
  • Dietary Supplements*
  • Endothelial Cells / drug effects
  • Humans
  • Hyperglycemia / drug therapy
  • Inflammation / drug therapy
  • Inflammation / prevention & control
  • Mitochondria / drug effects
  • Mitochondria / metabolism
  • Oxidation-Reduction / drug effects
  • Oxidative Stress
  • Reactive Oxygen Species / metabolism
  • Thioctic Acid / analogs & derivatives*
  • Thioctic Acid / chemistry
  • Thioctic Acid / pharmacology*


  • Antioxidants
  • Chelating Agents
  • Reactive Oxygen Species
  • Thioctic Acid
  • dihydrolipoic acid