Current Medicinal Chemistry

Atta-ur-Rahman, FRS
Honorary Life Fellow
Kings College
University of Cambridge


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Physiological Effect and Therapeutic Application of Alpha Lipoic Acid

Author(s): Sungmi Park, Udayakumar Karunakaran, Nam Ho Jeoung, Jae-Han Jeon and In-Kyu Lee

Affiliation: Department of Internal Medicine, Kyungpook National University School of Medicine, 130 Dongdukro, Jung-gu, Daegu, Republic of Korea, 700-721.

Keywords: α-keto acid dehydrogenase complex, Cardiovascular disease, Endothelial dysfunction, Glutathione, Glycine cleavage enzyme, Reactive oxygen species, Thiol-disulfide, Thioredoxin.


Reactive oxygen species and reactive nitrogen species promote endothelial dysfunction in old ageand contribute to the development of cardiovascular diseases such as atherosclerosis, diabetes, and hypertension. α-lipoic acid was identified as a catalytic agent for oxidative decarboxylation of pyruvate and α-ketoglutarate in 1951, and it has been studied intensively by chemists, biologists, and clinicians who have been interested in its role in energetic metabolism and protection from reactive oxygen species-induced mitochondrial dysfunction. Consequently, many biological effects of α- lipoic acid supplementation can be attributed to the potent antioxidant properties of α-lipoic acid and dihydro α-lipoic acid. The reducing environments inside the cell help to protect from oxidative damage and the reduction-oxidation status of α-lipoic acid is dependent upon the degree to which the cellular components are found in the oxidized state. Although healthy young humans can synthesize enough α-lipoic acid to scavenge reactive oxygen species and enhance endogenous antioxidants like glutathione and vitamins C and E, the level of α-lipoic acid significantly declines with age and this may lead to endothelial dysfunction. Furthermore, many studies have reported α-lipoic acid can regulate the transcription of genes associated with anti-oxidant and anti-inflammatory pathways. In this review, we will discuss recent clinical studies that have investigated the beneficial effects of α-lipoic acid on endothelial dysfunction and propose possible mechanisms involved.

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Article Details

Page: [3636 - 3645]
Pages: 10
DOI: 10.2174/0929867321666140706141806