| The pharmacology of the antioxidant lipoic acid. | |
| | |
MedLine Citation:
|
PMID: 9378235 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
|
1. Lipoic acid is an example of an existing drug whose therapeutic effect has been related to its antioxidant activity. 2. Antioxidant activity is a relative concept: it depends on the kind of oxidative stress and the kind of oxidizable substrate (e.g., DNA, lipid, protein). 3. In vitro, the final antioxidant activity of lipoic acid is determined by its concentration and by its antioxidant properties. Four antioxidant properties of lipoic acid have been studied: its metal chelating capacity, its ability to scavenge reactive oxygen species (ROS), its ability to regenerate endogenous antioxidants and its ability to repair oxidative damage. 4. Dihydrolipoic acid (DHLA), formed by reduction of lipoic acid, has more antioxidant properties than does lipoic acid. Both DHLA and lipoic acid have metal-chelating capacity and scavenge ROS, whereas only DHLA is able to regenerate endogenous antioxidants and to repair oxidative damage. 5. As a metal chelator, lipoic acid was shown to provide antioxidant activity by chelating Fe2+ and Cu2+; DHLA can do so by chelating Cd2+. 6. As scavengers of ROS, lipoic acid and DHLA display antioxidant activity in most experiments, whereas, in particular cases, pro-oxidant activity has been observed. However, lipoic acid can act as an antioxidant against the pro-oxidant activity produced by DHLA. 7. DHLA has the capacity to regenerate the endogenous antioxidants vitamin E, vitamin C and glutathione. 8. DHLA can provide peptide methionine sulfoxide reductase with reducing equivalents. This enhances the repair of oxidatively damaged proteins such as alpha-1 antiprotease. 9. Through the lipoamide dehydrogenase-dependent reduction of lipoic acid, the cell can draw on its NADH pool for antioxidant activity additionally to its NADPH pool, which is usually consumed during oxidative stress. 10. Within drug-related antioxidant pharmacology, lipoic acid is a model compound that enhances understanding of the mode of action of antioxidants in drug therapy. |
| | |
Authors:
|
G P Biewenga; G R Haenen; A Bast |
Related Documents
:
|
11572595 - Kinetic model for phenolic compound oxidation by fenton's reagent. 16787035 - Antioxidant and antiradical activities in extracts of hazelnut kernel (corylus avellana... 22062255 - Free range rearing of pigs with access to pasture grazing - effect on fatty acid compo... 18205305 - Oxidative transformation of natural and synthetic phenolic mixtures by trametes versico... 10622165 - Concentration of volatile fatty acids in digesta samples obtained from healthy cows and... 8055925 - Carbamoyl phosphate and ureagenesis are not involved in amino-acid-stimulated glycogene... |
Publication Detail:
|
Type: Journal Article; Review |
Journal Detail:
|
Title: General pharmacology Volume: 29 ISSN: 0306-3623 ISO Abbreviation: Gen. Pharmacol. Publication Date: 1997 Sep |
Date Detail:
|
Created Date: 1997-11-10 Completed Date: 1997-11-10 Revised Date: 2005-11-16 |
Medline Journal Info:
|
Nlm Unique ID: 7602417 Medline TA: Gen Pharmacol Country: ENGLAND |
Other Details:
|
Languages: eng Pagination: 315-31 Citation Subset: IM |
Affiliation:
|
Leiden/Amsterdam Center for Drug Research, Vrije Universiteit, Department of Pharmacochemistry, The Netherlands. |
Export Citation:
|
APA/MLA Format Download EndNote Download BibTex |
| MeSH Terms | |
Descriptor/Qualifier:
|
Animals Antioxidants / metabolism, pharmacokinetics, pharmacology* Humans Oxidative Stress / drug effects Thioctic Acid / metabolism, pharmacokinetics, pharmacology* |
| Chemical | |
Reg. No./Substance:
|
0/Antioxidants; 62-46-4/Thioctic Acid |
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
Previous Document: Peripheral-type benzodiazepine receptors.
Next Document: Gender differences in activities of mouse esterase and sensitivities to DFP and sarin toxicity.