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Alpha Lipoic Acid

The Ideal Antioxidant

What is Alpha Lipoic Acid?

Alpha lipoic acid (a.k.a. lipoate, 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 multi-enzyme complex that catalyzes the last stage of the process called glycolysis. Glycolysis is the first step in converting blood sugar (glucose), obtained from carbohydrates and proteins, into an energy 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 and the amino acid cysteine.

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 referred to as a disulfide molecules because it contains two sulfur units occurring as thiols. A thiol 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, another thiol-containing molecules and the most important antioxidant made by the body.

Why the Universal Antioxidant?

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 phases such as blood; yet as dihydrolipoic acid, it is also effective in protecting fatty tissues and membranes, a role it shares with Vitamin E.

Thus, alpha lipoic acid and dihydrolipoic acid function together as a universal antioxidant, meaning an antioxidant that quenches free radicals in both lipid and water-soluble portions of tissues and cells.

Alpha lipoic acid and dihydrolipoic acid are extremely powerful quenchers of hydroxyl, singlet-oxygen, peroxynitrite and other free radicals. Smog and many other sources of environmental toxins either create 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 manufacture from alpha lipoic acid, functions as a powerful direct chain-breaking antioxidant halting runaway lipid peroxidation reactions. It enhances the antioxidant potency of other antioxidants (e.g. Vitamins C and E) in both the water-based (cytosol interior) and lipid (membranous) portions of the cells.

Alpha lipoic acid directly recycles Vitamin C and indirectly recycles Vitamin E. This ability is both unique and highly sufficient.

Several other distinctive properties are characteristic of alpha lipoic acid's universal antioxidant properties. ALA increases glutathione levels in cells, in part by improving the body's ability to use the amino acid L-cysteine in synthesizing its supply of glutathione.

It also maintains a normal ratio of reduced-to-oxidized coenzyme q10, which is especially important to the health of the mitochondria, the energy factories of the cells. As a further benefit, as dihydrolipoic acid, alpha lipoic acid is one of very few antioxidant molecules small enough to penetrate the mitochondria directly.

The reduction of alpha lipoic acid to dihydrolipoic acid and the role of alpha lipoic acid in the production of glutathione are two of its several vitamin-like physiologic functions.

Alpha Lipoic Acid Improves Sugar (Carbohydrate) Metabolism and Increases Muscular Energy

Alpha lipoic acid is an important component in the production of energy from carbohydrates. Lipoate is involved throughout the complex multi-enzyme 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. Lipoic acid enhances the burning of glucose in obese laboratory animals in a manner comparable to, but independent of, insulin.

One study of adult diabetic patients showed that alpha lipoic acid increases cellular uptake and oxidation (burning) of glucose by about 50%. This is important for athletes as well as those who are over-weight.

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.

The Multiple Benefits of Alpha Lipoic Acid

  • A natural antioxidant that has a high reactivity to specific free radicals, including oxygen radicals and ionizing metals such as iron.
  • Well absorbed via the stomach and is easily supplemented orally. It does not accumulate in tissue, and therefore has no toxicity in the amounts taken to support blood sugar metabolism.
  • Because it is distributed throughout all tissues, it is useful for a wide variety of tissues, particularly the protection of the brain, which is the most sensitive organ to free radical damage.
  • Synergistically interacts with other antioxidants to regenerate both Vitamins C and E and maintain the proper ratio of reduced-to-oxidized Co-Q10 in the mitochondria. Therefore, alpha lipoic acid can buffer periodic deficiencies in these and other antioxidants due to improper diet and/or elevated stress.
  • Increases tissue levels of glutathione, one of the principal antioxidants that decline with age. Protects the mitochondria; mitochondrial decay is associated with aging.
  • In addition to its benefits as an antioxidant, alpha lipoic acid functions a a co-vitamin or coenzyme by enhancing the utilization and disposal of glucose.

The Importance of Biotin

Anyone likely to be severely biotin-deficient should take supplemental biotin if alpha lipoic acid is used regularly. Since biotin (Vitamin H) and alpha lipoic acid are chemically similar and are transported into cells by the same mechanism, elevated dietary alpha lipoic acid can interfere with biotin absorption. Additionally, alpha lipoic acid may decrease the efficacy of biotin's role in the function of certain enzymes.

Source: Jarrow Formulas

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Scientific References

  • 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  inactivations by oxidized and reduced lipoic acid. FEBS Letters (1996) 379: 74-76.
  • Kagan VE., et al. Dihydrolipoic acid, a universal antioxidant both in the membrane and in the aqueous phase. Biochemical Pharmacology (1992) 44: 1637-1649.
  • Kagan VE., et al. Recycling of Vitamin E in human low density liproproteins. Journal of Lipid Research (1992) 33: 385-397.



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