Alpha-lipoic acid (ALA ; (R ) -5- (1,2- dithiolan -3 -yl ) -pentanoic acid ) is considered one of the most effective antioxidants- not only does it scavenge free oxygen radicals, it also strengthens the natural protection of the body against anti-oxidation and regenerates the the reduced molecules of other antoxidants- such as vitamin C and E.8 Alpha-lipoic acid was once consiered as one of the vitamins, but later studies have shown that it can be synthesized in the body. It is also present in food, where the highest concentration of it can be found in broccoli and spinach.3
Because of its characteristics, Alpha-lipoic acid can be used in the treatment of heavy metal and fungal poisoning, diabetes, cirrhosis of the liver, and in neurodegenerative diseases or brain lesions, chemotherapy, hypertension. More and more studies have shown its effectiveness in the treatment of multiple sclerosis and autoimmune diseases (i.e. asthma).
Alpha-lipoic acid is well absorbed from the digestive tract, and also readily crosses the blood-brain barrier. It is considered to be an extremely effective substance.
The body uses free radicals (or reactive oxygen forms) for defense against pathogens, and as signaling molecules. Because of their high reactivity, an excess of free radicals is dangerous for the body. Caused by excessive amounts of free radicals, oxidative stress contributes to a number of pathological changes and may lead to neurodegeneration, atherosclerosis, cancer, inflammatory diseases and many others. Many studies have confirmed that Alpha-lipoic acid's ability to neutralize highly reactive hydroxyl radicals (OH*), singlet oxygen (1O2), hypochlorous acid (HOCl) and peroxynitrite (ONOO-), as well as peroxyl radicals. Some of the metabolites of alpha-lipoic acid and bisnorliponin tetranorliponin also have the ability to scavenge free radicals.
Mechanisms of antioxidation become less effective with age, which is why older people are more vulnerable to negative effects of oxidative stress. The old tissues of organisms tend to have a decrease in the activity of natural enzymes: glutathione reductase, glutathione peroxidase and glutathione S-transferase, and increased lipid peroxidation. The administration of alpha lipoic acid increases the level of both enzymatic and non-enzymatic antioxidants and reduces lipid peroxidation.3,8
Alpha- lipoic acid reduces the secretion of inflammatory markers (proinflammatory cytokines: interferon and interleukin 4), reduces the influx of T cells and macrophages to the central nervous system, and also inhibits the activity of metalloproteinases secreted by leukocytes. These properties confirm the immunomodulatory effects of alpha-lipoic acid.
Studies on mice suggest an important role of alpha-lipoic acid in the treatment of multiple sclerosis through the inhibition of neuronal demyelination. They also demonstrate the potential use in the treatment of autoimmune diseases related to hyperactivity of the immune system - such as asthma.
Alpha-lipoic acid can reduce the negative effects of heavy metal poisoning- such as mercury, arsenic, cadmium, and lead. Studies suggest that alpha-lipoic acid has the ability to remove accumulated mercury from the kidneys, but also increases the amount by which it is removed along with bile. Moreover, it was observed that the damage to nerve tissue caused by mercury poisoning is limited due to the anti-oxidant effects of alpha-lipoic acid.5
In the case of specific metals, various mechanisms correspond with the health benefits of alpha-lipoic acid. For example, in the case of arsenic poisoning, alpha-lipoic acid slows down the rate at which aresnic is absorbed into the digestive system. In the case of lead poisoning, alpha-lipoic acid prevents the peroxidation of lipids and helps maintain the balance between the reduced and oxidated forms of glutathione. It does not; however, have any effect on the amount of lead accumulated in the blood or tissue.3
Studies on rats have confirmed that alpha-lipoic acid effectively limits the damage done to the heart and testicles caused by administered cyclophosphamide. A reduction in damage to the kidney and inner ear associated with the administration of cisplatin, and a reduced platinum accumulation in the kidneys was also observed.3
Many classic chemotherapy treatments cause a decrease in the activity of antioxidant enzymes (Catalase, superoxide dismutase, glutathione reductase, glutathione peroxidase and glutathione S-transferase) as well as an increase in the peroxidation of lipids. Alpha-lipoic acid significantly limits these changes, often bringing the above-mentioned parameters back to control values.3
Alpha-lipoic acid has a number of hypoglycemic properties. It reduces the accumulation of triacylglycerols in the pancreas (which leads to cell damage), prevents insulin resistance, and increases the efficiency of insulin in stimulating glucose uptake into muscle cells, glycogen synthesis and glucose oxidation. Alpha-lipoic acid has a particular positive effect in type 2 diabetes both in the early stages and during complications of this disease (eg. diabetic neuropathy or kidney damage).2,3,7,9
Alpha-lipoic acid prevents damage caused by ischemia and reperfusion.1
It also protects against the negative effects of hypoxia of many different organs: such as heart, liver, retina and brain. In the case of nerve cell hypoxia, it has been stated that alpha-lipoic acid prevents the drop of neuronal density, and may also have an anti-apoptotic effect.3
Alpha-lipoic acid normalizes blood pressure, and prevents pathological changes in blood vessels and kidneys: these include hypertrophy of the aorta, renal arteries and arterioles, glomerular damage and proteinuria, caused by hypertension. Studies suggest that alpha-lipoic acid reduces the production of endothelin 1 – a specific protein that causes the contraction of blood vessels and stimulates the formation of vascular smooth muscle cells; the overexpression of which is often accompanied by hypertension.3
Studies used doses from 200 to 600mg.
Alpha-lipoic acid shows no serious adverse effects and is considered to be safe and well tolerated by humans.
1. Chidlow, G., Schmidt, K.-G., Wood, J. P. M., Melena, J., & Osborne, N. N. (2002). Alpha-lipoic acid protects the retina against ischemia-reperfusion. Neuropharmacology, 43(6), 1015-1025.
2. Golbidi, S., Badran, M., & Laher, I. (2011). Diabetes and alpha lipoic acid. Frontiers in Pharmacology, 2 NOV, 69.
3. Malińska, D., Winiarska, K., (2005) Kwas liponowy – charakterystyka i zastosowanie w terapii. Postępy Higieny i Medycyny Doświadczalnej. 59: 535-543.
4. Packer, L., Witt, E. H., & Tritschler, H. J. (1995). Alpha-lipoic acid as a biological antioxidant. Free Radical Biology and Medicine.
5. Patrick, L. (2002). Mercury toxicity and antioxidants: Part 1: role of glutathione and alpha-lipoic acid in the treatment of mercury toxicity. Alternative medicine review : a journal of clinical therapeutic, 7(6), 456-471.
6. Shay, K., Moreau, R., & Smith, E. (2009). Alpha-lipoic acid as a dietary supplement: molecular mechanisms and therapeutic potential. Biochimica et Biophysica …, 1790(10), 1149-1160.
7. Singh, U., & Jialal, I. (2008). Alpha-lipoic acid supplementation and diabetes. Nutrition reviews, 66(11), 646-57.
8. Wollin, S. D., & Jones, P. J. (2003). Alpha-lipoic acid and cardiovascular disease. J Nutr, 133(11), 3327-3330.
9. Vallianou, N., Evangelopoulos, A., & Koutalas, P. (2009). Alpha-lipoic Acid and diabetic neuropathy. The review of diabetic studies : RDS, 6(4), 230-236.
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