Lipoic Acid: its antioxidant and anti-inflammatory role and clinical applications

Curr Top Med Chem. 2015;15(5):458-83. doi: 10.2174/1568026615666150114161358.


Lipoic acid (LA) is an antioxidant able to produce its effects in aqueous or lipophilic environments. Lipoate is the conjugate base of lipoic acid, and the most prevalent form of LA under physiological conditions. It presents a highly negative reduction potential, increases the expression of antioxidant enzymes and participates in the recycling of vitamins C and E. Due to these properties, LA is called the "universal antioxidant". LA is also involved with anti-inflammatory action, independently of its antioxidant activity. This review was carried out, aiming to identify, analyze, and rationalize the various clinical, physiopathological and/or physiological situations in which LA, through oral supplementation, was tested on human and animal (rats and mice) models. LA was mainly tested in cardiovascular diseases (CVD), obesity, pain, inflammatory diseases and aging. LA uses in CVD and obesity, in humans, are controversial. On the other hand, beneficial effects on inflammation and pain were observed. LA supplementation in animal models may prolong life, has neuroprotective effects and presents positive effects against cancer. Differences observed in human and animal models can be due, in part, to different treatments (LA combined with other antioxidants, different doses) and to the variety of biomarkers investigated in animal experiments. These results suggest the need for further clinical trials to guide health professionals regarding the safety of prescription of this supplement.

Publication types

  • Review

MeSH terms

  • Aging / drug effects*
  • Aging / metabolism
  • Animals
  • Anti-Inflammatory Agents / metabolism
  • Anti-Inflammatory Agents / pharmacology*
  • Antioxidants / metabolism
  • Antioxidants / pharmacology*
  • Ascorbic Acid / metabolism
  • Clinical Trials as Topic
  • Disease Models, Animal
  • Humans
  • Inflammation / drug therapy
  • Inflammation / metabolism
  • Inflammation / pathology
  • Oxidative Stress / drug effects
  • Pain / drug therapy*
  • Pain / metabolism
  • Pain / pathology
  • Reactive Oxygen Species / antagonists & inhibitors*
  • Reactive Oxygen Species / metabolism
  • Thioctic Acid / metabolism
  • Thioctic Acid / pharmacology*
  • Vitamin E / metabolism


  • Anti-Inflammatory Agents
  • Antioxidants
  • Reactive Oxygen Species
  • Vitamin E
  • Thioctic Acid
  • Ascorbic Acid