Lipoic acid. Kinetics and pluripotent biological properties and derivatives

Mol Biol Rep. 2021 Sep;48(9):6539-6550. doi: 10.1007/s11033-021-06643-z. Epub 2021 Aug 22.

Abstract

Lipoic acid (LA) is globally known and its supplements are widely used. Despite its importance for the organism it is not considered a vitamin any more. The multiple metabolic forms and the differences in kinetics (absorption, distribution and excretion), as well as the actions of its enantiomers are analysed in the present article together with its biosynthetic path. The proteins involved in the transfer, biotransformation and activity of LA are mentioned. Furthermore, the safety and the toxicological profile of the compound are commented, together with its stability issues. Mechanisms of lipoic acid intervention in the human body are analysed considering the antioxidant and non-antioxidant characteristics of the compound. The chelating properties, the regenerative ability of other antioxidants, the co-enzyme activity and the signal transduction by the implication in various pathways will be discussed in order to be elucidated the pleiotropic effects of LA. Finally, lipoic acid integrating analogues are mentioned under the scope of the multiple pharmacological actions they acquire towards degenerative conditions.

Keywords: Lipoic acid; Metabolism of lipoic acid; Neuroprotective derivatives; Properties of lipoic acid.

Publication types

  • Review

MeSH terms

  • Animals
  • Anti-Inflammatory Agents / adverse effects
  • Anti-Inflammatory Agents / chemistry
  • Anti-Inflammatory Agents / metabolism*
  • Antioxidants / adverse effects
  • Antioxidants / chemistry
  • Antioxidants / metabolism*
  • Antipsychotic Agents / adverse effects
  • Antipsychotic Agents / chemistry
  • Antipsychotic Agents / metabolism*
  • Chelating Agents / adverse effects
  • Chelating Agents / chemistry
  • Chelating Agents / metabolism*
  • Dietary Supplements
  • Humans
  • Hypnotics and Sedatives / adverse effects
  • Hypnotics and Sedatives / chemistry
  • Hypnotics and Sedatives / metabolism*
  • Hypoglycemic Agents / adverse effects
  • Hypoglycemic Agents / chemistry
  • Hypoglycemic Agents / metabolism*
  • Immunomodulating Agents / adverse effects
  • Immunomodulating Agents / chemistry
  • Immunomodulating Agents / metabolism*
  • Kinetics
  • Oxidation-Reduction
  • Signal Transduction
  • Thioctic Acid / adverse effects
  • Thioctic Acid / analogs & derivatives*
  • Thioctic Acid / chemistry
  • Thioctic Acid / metabolism*

Substances

  • Anti-Inflammatory Agents
  • Antioxidants
  • Antipsychotic Agents
  • Chelating Agents
  • Hypnotics and Sedatives
  • Hypoglycemic Agents
  • Immunomodulating Agents
  • Thioctic Acid