~ Alpha Lipoic Acid - The Ideal Antioxidant

Alpha Lipoic Acid: The Ideal Antioxidant

What Is Alpha Lipoic Acid?

Also known as thioctic acid, alpha lipoic acid is an antioxidant and a cofactor in the body's production of energy. It has vitamin-like roles in the body. Alpha lipoic acid is a cofactor in the multienzyme complex that catalyzes the last stage of the process called glycolysis. Glycolysis is the first step in converting blood sugar (glucose), which is obtained from carbohydrates and proteins, into energy in a form that the body can use.

Alpha lipoic acid is not considered to be a vitamin because it is assumed that it can be synthesized by the body in small amounts from essential fatty acids. Although alpha lipoic acid is found in foods, such as liver and yeast, there are no foods rich enough in alpha lipoic acid to serve as good sources.

Alpha lipoic acid is a compound that contains sulfur in the form of two thiol groups, and therefore it is called a disulfide molecule. A thiol (chemically written as -SH) consists of one sulfur and one hydrogen atom. Not only does alpha lipoic acid act as an antioxidant itself, it also stimulates the production of glutathione, the most important antioxidant made by the body.

Alpha Lipoic Acid Functions as a Universal Antioxidant and Free Radical Scavenger

Once inside cells, alpha-lipoic acid is converted to its more potent form, dihydrolipoic acid. Alpha lipoic acid is unique in that, like vitamin C, it is effective as an antioxidant in water based tissues such as the blood, and yet as clihydrolipoic acid it also is effective in protecting fatty tissues and membranes, a role it shares with vitamin E.

Thus alpha lipoic acid and clihydrolipoic acid together function as a universal antioxidant, meaning an antioxidant that quenches free radicals in both lipid and water-soluble portions of tissues and cells. Lipoic acid and clihydrolipoic acid are extremely powerful quenchers of hydroxyl, singlet-oxygen, peroxynitrite and other free radicals.'

Free radicals are associated with the development of atherosclerosis, lung disease, and neurological disorders, as well as being implicated in chronic inflammation, such as that found with rheumatoid arthritis and inflammatory bowel disease. Smog and many other sources of environmental toxins either are themselves or lead to the creation of free radicals in the body.

Alpha Lipoic Acid Recycles Both Fat-and Water-Soluble Vitamins

Dihydrolipoic acid, which the body routinely manufactures from alpha lipoic acid, functions as a powerful direct chain breaking antioxidant and it enhances the antioxidant potency of other antioxidants (e.g., vitamins C and E) in both the water-based and lipid or non-water-based portions of cells.' Alpha lipoic acid directly recycles vitamin C and indirectly recycles vitamin E. This ability is unique and highly significant.

Several other unusual properties are characteristic of alpha-lipoic acid's universal antioxidant properties. Alpha lipoic acid increases glutathione levels in cells, at least in part, by improving the body's ability to use the amino acid L-cysteine to synthesize its supply of glutathione. Supplemental lipoic acid also maintains a normal ratio of reduced-to-oxidized coenzyme Q10. Coenzyme Q10 is especially important to the health of the mitochondria, the energy factories of the cells.

As a further benefit, alpha lipoic acid as clihydrolipoic acid is one of the very few antioxidant molecules (it may be the only one) small enough to penetrate the mitochondria directly. The reduction of alpha lipoic acid to clihydrolipoic acid and the role of alpha lipoic acid in the production of glutathione appear to be normal functions of alpha lipoic acid in the body. These are two of its several vitamin-like physiologic functions.

Alpha Lipoic Acid Improves Sugar Metabolism and Increases Muscular Energy

There is no doubt that alpha lipoic acid is an important component in the production of energy from carbohydrates. It is involved throughout the complex multienzyme process which catalyzes glucose (blood sugar) into energy.

As part of the glycolytic pathway, alpha lipoic acid both stimulates insulin activity and reduces insulin resistance. It has been shown to enhance the burning of glucose in obese laboratory animals in a way that is comparable to, but independent of, insulin. One study of adult diabetic patients showed that alpha lipoic acid increased the cellular uptake and oxidation (burning) of glucose by about 50 percent. This is important for athletes as well as for the overweight. The efficient burning of glucose is essential for the normal production of energy in the muscles, and impaired muscle-energy metabolism interferes with exertion. Similar improvements in energy metabolism have been found in the brain.

Alpha Lipoic Acid May Have Special Delivery Requirements for Maximal Benefits

Alpha lipoic acid does not accumulate in tissues and, therefore, does not have any toxicity in the amounts usually taken. Because it is distributed throughout the tissues, it is useful in a wide variety of conditions. It is particularly protective of the brain, which is the most sensitive of organs to free radical damage, and the eye. However, animal experiments have shown that this protective effect is highly dependent upon the timing and the form of administration.

Alpha lipoic acid is rapidly cleared from the blood by the liver and must be transformed into dihydrolipoic acid for maximal benefits both as an antioxidant and as a glucose disposal agent. Sustained release delivery may match better the known pharmacokinetics of alpha lipoic acid than do the usual tablet and capsule delivery forms.5 Also, sustained release may be helpful to those who suffer from gastric distress from the very low pH (i.e., very acid quality) of alpha lipoic acid when taken in regular dosage forms.

Note: These statements have not been evaluated by the Food and Drug Administration. This product is not intended to diagnose, treat, cure or prevent any disease.

The Alpha Lipoic Acid Benefits List
  • Lipoic acid is a natural antioxidant that has a high reactivity to specific free radicals, including oxygen radicals and ionized metals.
  • Lipoic acid is well absorbed via the stomach and can be easily supplemented orally. It does not accumulate in tissues and, therefore, does not have any toxicity in the amounts taken for preventive and therapeutic reasons. Because it is distributed throughout all of the tissues, it is useful in a wide variety of conditions, particularly the protection of the brain, which is the most sensitive of organs to free radical damage.
  • Lipoic acid interacts synergistically with other antioxidants. It regenerates both vitamins C and E and it maintains the proper ratio of reduced to oxidized coenzyme 010 in the mitochondria. Therefore, lipoic acid can buffer periodic deficiencies in these and other antioxidants due to improper diet and/or elevated stress.
  • Lipoic acid increases the tissue levels of glutathione, which is one of the principal endogenous antioxidants that decline with aging. Lipoic acid protects the mitochondria; mitochondrial decay is associated with aging.
  • In addition to its benefits as an antioxidant, lipoic acid functions as a co-vitamin or coenzyme in the enhancement of the utilization and disposal of glucose.
Usage and Safety

Neither animal nor human studies to date have any shown serious side effects with the ingestion of alpha-lipoic acid. It is prudent that any group likely to be severely thiamine-deficient, for example, alcoholics, should take supplemental thiamine if alpha-lipoic acid is used regularly. Side effects are very rare, but include allergic skin reactions and possible hypoglycemia in diabetics as a consequence of improved glucose utilization with high levels of intake.

Alpha lipoic acid is a powerful antioxidant and free radical scavenger even when ingested in relatively small amounts. One hundred milligrams supplemented once or twice per day is considered to be adequate for most purposes. Clinical studies typically have employed 300 mg taken twice per day. Jarrow Formulas' new sustained release formula is intended to match the known metabolism of alpha lipoic acid in the body and may be helpful to those who suffer from gastric distress with ordinary alpha lipoic acid supplements due to the very low pH of the compound.

Alpha Lipoic: The Ideal or Universal Antioxidant and Free Radical Scavenger
  • Active in All the Tissues of the Body and in All Cellular Compartments
  • Recycles Both Fat and Water Soluble Antioxidant Vitamins
  • Improves Sugar Metabolism and Energy Production
  • Promotes the Incorporation of Cysteine into Glutathione
  • The Antioxidant Team Player. Combines Synergistically with Other Antioxidants for Increased Benefits
  • Improved Bioavailability and Activity in New 300 mg Sustained-Release Formulation

1. Packer L, et al. Alpha lipoic acid as a biological antioxidant. Free Radical Biology& Medicine (1995) 19:227-250; Whiteman M, et al. Protection against peroxynitrite-dependent tyrosine nitration and alpha-antiproteinase inactivation by oxidized and reduced lipoic acid. FEBS Letters (1996) 379:74-76.
2. Kagan VE, et al. Dihydrolipoic acid, a universal antioxidant both in the membrane and in the aqueous phase. Biochemical Pharmacology (1992) 44:1637-1649.
3. Kagan VE, et al. Recycling of vitamin E in human low density lipoproteins. Journal of Lipid Research (1992) 33:385-397; Dusse E. et al. Influence of alpha lipoic acid on intracellular glutathione in vitro and in vivo. Arzneimittel-Forschung (1992) 42:829-831; Gotz ME, et al. Effect of lipoic acid on redox state of coenzyme Q in mice treated with 1-methyl-1-4-phenyl1,2,3,4-tetrahydropyHdine and diethyidithiocarbamete. European Journal of Pharmacology (1994) 266:291-300.
4. Haugaard N, Haugaard ES. Stimulation of glucose utilization by thioctic acid in rat diaphragm incubated in vitro. Biochimica et Biophysica Acta (1970) 222:583-586; Jacob S, et al. Enhancement of glucose disposal in patients with type 2 diabetes by alpha lipoic acid. Atzrieimittel-Forschung (1995) 45:872-874; Henriksen EJ, et al. Chronic thioctic acid treatment increases insulin stimulated glucose transport activity in skeletal muscle of obese zucker rats. Diabetes (Suppl.) (1994) 1:122A; Barbirolli B, et al. Lipoic (thloctic acid) increases brain energy availability and skeletal muscle performance as shown by in vivo 31 P-MRS in a patient with mitochondrial cytopathy. Journal of Neurology (1995) 242:472-477.
5. Wolz P, Krieglstein J. Neuroprotective effects of alpha lipoic acid and its enantiomers demonstrated in rodent models of focal cerebral ischernia. Neuropharmacology (1996) Mar, 35(3):369-75; Shih JC. Atherosclerosis in Japanese quail and the effect of lipoic acid. Fed Proc 42:2494-7 (1983, May 15).

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