Alpha lipoic acid (ALA), a vitamin-like substance found in foods and produced by the body in limited amounts, may be the most valuable of all the antioxidant nutrients. In addition to neutralizing both oxygen and nitrogen free radicals, ALA has been studied for its ability to actually repair oxidative damage, to regenerate other antioxidants and chelate excess metals.^(1,2)

ALA is one of many substances produced by the body in large quantities in young people, but production declines with aging. Health conscious individuals may inadvertently limit their intake of this important nutrient by reducing their intake of red meat, one of the richest dietary sources of ALA. Lipoic acid deficiency has been linked to muscle wasting, brain atrophy and increased lactic acid accumulation. Lower serum levels of lipoic acid are frequently found in patients with cirrhosis of the liver, diabetes and heart disease.⁽¹⁾

Unlike other antioxidants, ALA is both hydrophylic (water soluble) and lipophylic (fat soluble), enabling it to act both inside the cell and in the intracellular spaces. Because of its universal solubility, ALA is able to neutralize both hydroxyl and singlet-oxygen free radicals, two of the most dangerous types, wherever they are found. It works to prevent free radical damage regardless of whether it is in the brain fluids, blood, stored fat, the heart, pancreas, kidneys, liver, bone or cartilage. Its protective effects extend to virtually every cell in every organ and tissue. The addition of Bioperine® to Alpha Lipoic Acid insures enhanced uptake and bioavailability.

These characteristics enable ALA to easily cross the blood-brain barrier and increase brain energy.⁽¹⁾ It has been shown to improve long-term memory in aged mice, probably by preventing free radical damage to cell membranes.⁽¹⁵⁾ Other studies support a neuro-protective role against various chemicals.

ALA supplements actually give you two antioxidants in one. As ALA does its work, it is reduced to dihydrolipoic acid (DHLA), another important antioxidant that can deactivate peroxyl and other types of free radicals. When DHLA is oxidized, it reverts back to ALA. The molecule goes back and forth automatically in the body accomplishing many important and beneficial functions.^(1,2)

In order to deactivate free radicals, antioxidants must give up an electron. Therefore, their effective "life" is limited. DHLA is able to restore the missing electrons and extend the life of other antioxidants. It replenishes vitamin C and indirectly recycles vitamin E so that those antioxidants remain active longer. Supplemental ALA also helps maintain a normal ratio of reduced to oxidized co-enzyme Q₁₀. In addition, ALA and DHLA provoke the cell to produce significantly higher levels of glutathione, the indispensable cellular antioxidant synthesized within the mitochondrion.^(1,2)

Burt Berkson, M.D., Ph.D., author of The Alpha Lipoic Acid Breakthrough, believes ALA to be an excellent therapeutic agent for many types of liver disorders. In his book he describes how administering intravenous ALA saved the lives of four people who suffered severe liver damage after eating poisonous mushrooms. Two weeks later the patients’ liver function tests were normal and they felt fine.⁽¹⁾ In vitro studies indicate that ALA may be beneficial to patients with acute and chronic alcohol toxicity.⁽⁸⁾ ALA is also an effective chelating agent for mercury, arsenic, copper, excess iron, cadmium, excess calcium, zinc and lead. Excesses of these metals can overwhelm the liver’s detoxification system, increase free radicals and oxidative stress, and cause serious damage to tissues and organs.⁽¹⁾

ALA also functions as a co-enzyme in sugar metabolism. In a study of adult diabetic patients, ALA increased cellular uptake and burning of glucose by approximately 50%.⁽³⁾ In two double-blind, placebo controlled trials, ALA significantly reduced symptoms of diabetic peripheral neuropathy (pain, burning, paresthesia and numbness) in the feet and improved cardiac autonomic dysfunction in non-insulin dependent diabetics.⁽⁴⁾ In both lean and obese diabetic patients, ALA also prevents hyperglycemia-induced increments of serum lactate and pyruvate levels and it increases insulin sensitivity and glucose effectiveness.⁽⁶⁾

ALA speeds the body’s breakdown and burning of sugar, which occurs primarily in muscle cells. Efficient burning of glucose is essential for normal muscle energy. A 33-year-old woman who suffered from a genetic defect affecting cellular energy production was treated with ALA. Glucose uptake, glucose burning, muscle-energy metabolism and muscle strength increased, as documented by laboratory tests.⁽¹¹⁾ Since ALA can increase energy levels in muscle cells, it may be valuable in sports nutrition and weight control.

Because of its antioxidant capabilities and its ability to boost glutathione production and recycle other antioxidants, ALA can also play a role in cardiovascular health. Both ALA and DHLA are extremely powerful for deactivating peroxynitrite, a particularly dangerous type of free radical formed by combination of superoxide radicals and nitric oxide. It contributes to the development of atherosclerosis, lung disease, neurological disorders and chronic inflammation, such as that associated with rheumatoid arthritis and inflammatory bowel disease.⁽⁷⁾ Ischemia/reperfusion injury results from the large number of free radicals generated when blood flow is restored after surgery. ALA treatment before and after reperfusion can lessen or prevent such injury to the heart, brain and peripheral nerve tissues.^(12-14)

In a pilot study, supplementation with 150 mg. of lipoic acid 3 times a day was shown to increase plasma ascorbate, glutathione and T-helper cells and to optimize the ratio of T-helper cells to T-suppressor cells. Other studies have demonstrated that lipoic acid also helps to inhibit HIV replication by decreasing the activity of reverse transcriptase.⁽⁵⁾ Apoptosis (programmed cell death) is triggered by cellular oxidation and can be prevented with antioxidants. DHLA has been shown to prevent apoptosis in thymus cells.⁽¹⁰⁾

Based on animal experiments, ALA may have value in preventing cataracts which are caused by oxidative stress in the lens.⁽⁹⁾ Since ALA is both water-soluble and fat-soluble, it can get deep into the eye tissues and destroy free radicals that cause protein changes resulting in cataracts. Animals given chemicals to induce cataracts had a 60% reduction in cataract formation when treated with ALA.⁽¹⁾

Russian scientists who treated children exposed to radiation after the nuclear incident in Chernobyl reported ALA, used by itself or with vitamin E, to be an effective treatment for radiation poisoning. They noted that abnormal liver and kidney functions were also corrected. ALA has been shown to protect the bone marrow of mice from radiation injury, has been reported to neutralize the toxic effects of radiation in animals and to alleviate the harmful effects of cancer chemotherapy in humans.⁽¹⁾

WARNING: This publication and the product contained herein have not been approved or evaluated by the Food and Drug Administration. This publication, and the product contained herein are not intended to diagnose, treat, cure or prevent any disease. The product relates to nutritional support only.

1. Berkson, B., The Alpha Lipoic Acid Breakthrough, Prima Publishing, Rocklin, CA, 1998.

2. Biewenga, G., Haenen G., Bast, A., "The pharmacology of the antioxidant lipoic acid", Gen. Pharmacol., 1997 Sept;29(3):315-31.

3. Jacob, S., et al. "Enhancement of glucose disposal in patients with type 2 diabetes by alpha-lipoic acid." Arzn.-Forsch, 1995;45:872-4.

4. Ziegler D., Gries, F., "Alpha-lipoic acid in the treatment of diabetic peripheral and cardiac autonomic neuropathy", Diabetes, 1997 Sept;46 Suppl 2:S62-6.

5. Meletis, C., "Basic Nutrient Support for Proper Immune Function", Alternative & Complementary Therapies, Feb., 1999, p. 44.

6. Konrad, T., et al. "Alpha-lipoic acid treatment decreases serum lactate and pyruvate concentrations and improves glucose effectiveness in lean and obese patients with type 2 diabetes", Diabetes Care, 1999 Feb;22(2):280-7.

7. Whiteman, M., et al. "Protection against peroxynitrite-dependent tyrosine nitration and a1-antiproteinase inactivation by oxidized and reduced lipoic acid", FEBS Letters, 1996;379:74-6.

8. Wickramasinghe, S., Hasan, R., "In Vitro Effects of Vitamin C, Thioctic Acid and Dihydrolipoic Acid on the Cytotoxicity of Post-Ethanol Serum", Biochemical Pharmacology, 1992;43(3):407-11.

9. Maitra, I., et al. "Alpha-lipoic acid prevents buthionine sulfoximine- induced cataract formation in newborn rats", Free Radical Biology & Medicine, 1995;18:823-829.

10. Bustamante, J., et al. "Antioxidant inhibition of thymocyte apoptosis by dihydrolipoic acid", Free Radical Biol. & Med., 1995; 19:339-47.

11. Barbiroli, B., et al. "Lipoic (thioctic acid) increases brain energy availability and skeletal muscle performance as shown in vivo 31:-MRS in a patient with mitochondrial cytopathy", J. Neurol., 1995;242:472-7.

12. Schonhit, K., et al. "Effect of alpha-lipoic acid and dihydrolipoic acid on ischemia/reperfusion injury of the heart and heart mitochondria", Biochimica et Biophysica Acta., 1995;1271:335-42.

13. Greenamyre, J., et al. "The endogenous cofactors, thioctic acid and dihydrolipoic acid, are neuroprotective angainst NMDA and malonic acid lesions of striatum", Neuroscience Letters, 1994;171:17-20

14. Mitsui, Y, et al. "Alpha-lipoic acid provides neuroprotection from ischemia-reperfusion injury of peripheral nerve", J. Neuro. Sci., Feb. 1; 163(1):11-6.

15. Stol S., et al. "The potent free radical scavenger alpha lipoic acid improves memory in aged mice: putative relationship to NMDA receptor deficits", Pharmacol., Biochem. & Behavior, 1993: 46:799-805.

ALPHA LIPOIC ACID
Metabolic Antioxidant Supplement

Product No. 872 Fill Size: 60 Capsules

Each capsule contains:
Alpha Lipoic Acid 100 mg.
Bioperine® 5 mg.
Other ingredients: rice flour, gelatin.

®Bioperine is a registered trademark of Sabinsa Corp. Bioperine is an extract of piperacea, used to enhance nutrient bioavailability.

Recommended Use: One or two capsules daily. Higher doses (600 mg. - 1200 mg.) daily have been safely used in clinical applications.