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Alpha-lipoic acid: molecular mechanisms and therapeutic potential in diabetes

Publication: Canadian Journal of Physiology and Pharmacology
25 September 2015


Diabetes is a chronic metabolic disease with a high prevalence worldwide. Diabetes and insulin resistance are associated with the development of cardiovascular and nervous diseases. The development of these disorders reflects complex pathological processes in which the oxidative stress caused by reactive oxygen species (ROS) and reactive nitrogen species (RNS) plays a pivotal role. It is widely accepted that diabetes impairs endothelial nitric oxide synthase (eNOS) activity and increases the production of ROS, thus resulting in diminished NO bioavailability and increased oxidative stress. Alpha-lipoic acid (LA) possesses beneficial effects both in the prevention and in the treatment of diabetes. LA is a potent antioxidant with insulin-mimetic and anti-inflammatory activity. LA in the diet is quickly absorbed, transported to the intracellular compartments, and reduced to dihydrolipoic acid (DHLA) under the action of enzymes. LA, which plays an essential role in mitochondrial bioenergetic reactions, has drawn considerable attention as an antioxidant for use in managing diabetic complications such as retinopathy, neuropathy and other vascular diseases.


Le diabète est un désordre métabolique chronique avec une prévalence élevée à travers le monde. Cette pathologie et la résistance à l’insuline sont associées au développement d’atteintes cardiovasculaires et nerveuses. Le développement de ces atteintes reflète des processus pathologiques complexes mettant en jeu un stress oxydatif qui joue un rôle majeur en impliquant les espèces radicalaires oxygénées (ERO) et nitro-oxygénées (ERN). Il est généralement admis que le diabète modifie l’activité des oxyde nitrique synthases endothéliales (eNOS), conduisant à une diminution de la biodisponibilité du NO et une augmentation du stress oxydatif. L’acide alpha-lipoïque (AL) possède des effets bénéfiques dans la prévention et le traitement du diabète. AL est un antioxydant puissant pourvu d’activités insulino-mimétiques et anti-inflammatoires. AL présent dans la nourriture est rapidement absorbé, transporté dans les compartiments intracellulaires et réduit en acide dihydrolipoïque (ADHL) sous l’effet d’enzymes. AL qui joue un rôle essentiel dans les réactions bioénergétiques mitochondriales, suscite beaucoup d’attention comme antioxydant dans la prise en charge des complications liées au diabète telles que les rétinopathies, les neuropathies et les autres atteintes vasculaires.

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Published In

cover image Canadian Journal of Physiology and Pharmacology
Canadian Journal of Physiology and Pharmacology
Volume 93Number 12December 2015
Pages: 1021 - 1027


Received: 13 September 2014
Accepted: 13 April 2015
Version of record online: 25 September 2015


This Invited Review is part of a Special Issue entitled “Pharmacology of vitamins and beyond. Part 2.”


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Key Words

  1. lipoic acid
  2. antioxidant
  3. diabetes
  4. metabolism
  5. prevention
  6. treatment


  1. acide lipoïque
  2. antioxydant
  3. diabètes
  4. métabolisme
  5. prévention
  6. traitement



Luc Rochette
Laboratoire de Physiopathologie et Pharmacologies Cardio-Métaboliques (LPPCM), INSERM UMR866, Université de Bourgogne, Facultés de Médecine et de Pharmacie, 7 Boulevard Jeanne d’Arc, 21033 Dijon Cedex, France.
Steliana Ghibu [email protected]
Department of Pharmacology, Physiology and Pathophysiology, Faculty of Pharmacy, “UMF Iuliu Haţieganu”, 6 Louis Pasteur Street, 400349 Cluj-Napoca, Romania.
Adriana Muresan
Department of Physiology, Faculty of Medicine, “UMF Iuliu Haţieganu” Cluj-Napoca, Romania.
Catherine Vergely
Laboratoire de Physiopathologie et Pharmacologies Cardio-Métaboliques (LPPCM), INSERM UMR866, Université de Bourgogne, Facultés de Médecine et de Pharmacie, 7 Boulevard Jeanne d’Arc, 21033 Dijon Cedex, France.

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127. Overproduction of α-Lipoic Acid by Gene Manipulated Escherichia coli
128. Effect of dietary oxidized tyrosine products on insulin secretion via the oxidative stress-induced mitochondria damage in mice pancreas
129. α-Lipoic acid as the main pharmacological drug for in- and outpatient treatment of diabetic polyneuropathy
130. Lipoic acid protects gastric mucosa from ethanol-induced injury in rat through a mechanism involving aldehyde dehydrogenase 2 activation
131. Microbiota and Neurological Disorders: A Gut Feeling
132. A Clinical Trial about a Food Supplement Containing α-Lipoic Acid on Oxidative Stress Markers in Type 2 Diabetic Patients
133. Epigenetic Treatment of Neurodegenerative Disorders: Alzheimer and Parkinson Diseases
134. Type 1 5′-deiodinase activity is inhibited by oxidative stress and restored by alpha-lipoic acid in HepG2 cells

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