Alpha-lipoic acid: physiologic mechanisms and indications for the treatment of metabolic syndrome

Expert Opin Investig Drugs. 2007 Mar;16(3):291-302. doi: 10.1517/13543784.16.3.291.


In animal experiments, the potent antioxidant and free radical scavenger alpha-lipoic acid has been shown to cause weight loss, ameliorate insulin resistance and atherogenic dyslipidemia, as well as to lower blood pressure, all of these being components of the metabolic syndrome. Recent investigations on its mechanisms of action indicate that alpha-lipoic acid can affect central and peripheral modulation of 5'-AMP-activated protein kinase, activate PPAR-alpha and PPAR-gamma, modulate PPAR-regulated genes and upregulate the expression of PPAR-gamma mRNA and protein in cardiac tissue and aorta smooth muscle. To a large extent, these findings can explain the observed beneficial metabolic effects of alpha-lipoic acid, supporting its potential application as a therapeutic agent for the treatment of the metabolic syndrome.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Adipogenesis / drug effects
  • Animals
  • Antioxidants / pharmacology*
  • Humans
  • Metabolic Syndrome / drug therapy*
  • Metabolic Syndrome / metabolism
  • PPAR alpha / metabolism
  • PPAR gamma / metabolism
  • Phosphotransferases (Phosphate Group Acceptor) / metabolism
  • Thioctic Acid / pharmacology*
  • Thioctic Acid / therapeutic use


  • Antioxidants
  • PPAR alpha
  • PPAR gamma
  • Thioctic Acid
  • AMP-dependent kinase (ATP-forming)
  • Phosphotransferases (Phosphate Group Acceptor)