for bulk r-ala: dnpint.com ($550/kilo) or geronova.com ($500/kilo)..but its expensive!! geronova does it right too!!
Alpha-lipoic acid occurs naturally in every cell of the body and is essential to the chemical reactions that allow our bodies to produce energy. As a supplement, it is rapidly absorbed into the blood and the cells where it can prevent free-radical damage. It is vital for the creation of energy in every organ of the body, but as we age, there is not enough of it in sufficient quantities.
Alpha-lipoic acid (ALA) has been shown to be beneficial in humans and animals as a preventive and/or treatment for many age-related diseases such as heart disease, ischemia-reperfusion injury, diabetes, cataract formation, HIV activation, multiple sclerosis, neurodegeneration, radiation injury, Parkinson’s and Alzheimer’s disease, as well as declines in energy, muscle strength, brain function and immunity. (1) (21)
ALA reverses the cellular redox status (from a more oxidized to a more reduced state) which prevents inflammation, associated with all of the chronic degenerative diseases of aging. In particular, ALA plays a crucial role in protecting the mitochondria, the energy-producing structures in cells and the genetic material, DNA. As we age, mitochondrial function is impaired, and it’s theorized that this may be an important contributor to some of the adverse effects of aging.
Alpha-lipoic acid has been called the ideal antioxidant and is a key component in the antioxidant network. This compound acts as an antioxidant, however, only when there is an excess of it, and it is in the "free" state in the cells; but there is little free ALA circulating in your body, unless you take it as a supplement. Foods contain only tiny amounts of it.
What makes ALA special as an antioxidant is its versatility—it helps deactivate an unusually wide array of cell-damaging free radicals in many bodily systems. It has potent antioxidant actions in every cell of the body, protects membranes by boosting and recycling levels of other antioxidants (vitamin C, vitamin E, Coenzyme Q10 and glutathione), thus making them much more effective. It neutralizes free radicals in both the fatty and watery regions of cells, in contrast to vitamin C (which is water soluble) and vitamin E (which is fat soluble).
ALA is actually much more than an anti-oxidant, even though it is most well-known for this use.
ALA is prescribed in Germany to treat diabetic and alcoholic neuropathies and alcoholic liver disease, thought to result in part from free-radical damage. There is also evidence that it can help decrease insulin resistance; it speeds the removal of glucose from the bloodstream by enhancing insulin function, and thus helps control blood sugar, underlying many cases of coronary heart disease and obesity.
Does your lipoic acid supplement contain
only the form found in nature?
Or does it also include a synthetic by-product that may
interfere with the natural form's beneficial effects?
ALPHA-LIPOIC ACID OCCURS IN 3 DIFFERENT FORMS
R-Lipoic Acid (the R (+) enantiomer) is the pure form found in nature and the human body that is responsible for most of alpha-lipoic acid's beneficial effects.
S-Lipoic acid (The S (-) enantiomer) is a by-product from chemical synthesis.
Alpha-lipoic acid consists of 50/50 racemic mixture of the R and S enantiomers and is the normal commercially available form of lipoic acid.
R-Lipoic Acid is the only naturally-occurring form of alpha-lipoic acid.
Within the mitochondria, R-lipoic acid is reduced to DHLA, the more potent antioxidant, 28 times faster than S-lipoic acid. (1a)
Researchers at ASTA Medica claim that R-Lipoic Acid is 10 times stronger than the racemate alpha-lipoic acid for reducing inflammation. (2)
The S-form can oppose the action of the R-form. In the aging rat heart, R-Lipoic Acid stimulated ATP production, whereas SLA inhibited it. (3)
For a definition and explanation of the meaning of R and S and + and - relative to chiral molecules, see FAQ and Chirality.
THE BENEFITS OF R-LIPOIC ACID
R-Lipoic Acid significantly reduces inflammation, an underlying cause of the degenerative diseases of aging and is more potent by a factor of 10 over commercial ALA. (2)
R-Lipoic acid was found to be more bioavailable than S-lipoic acid when taken orally in a human study. (2a)
R-Lipoic Acid was more effective than the S form in a battery of metal chelation tests. One hypothesis of the cause of diabetic complications involves overloading by transition metals which could explain the stereospecific effect of the R-form. (4)
R-Lipoic Acid is the only form of lipoic acid found in nature and therefore the only form recognized by the critical mitochondrial enzymes. (5)
R-Lipoic acid was more effective than S-lipoic acid in enhancing insulin-stimulated glucose transport and metabolism in insulin-resistant rat skeletal muscle. (5a)
R-Lipoic acid was more effective than racemic alpha-lipoic acid and S -alpha-lipoic acid in preventing cataracts in rats. (5b).
R-Lipoic Acid increases cellular and mitochondrial antioxidant activity and prevents mitochondrial decay. This effectively attenuates the reported increase in oxidative stress with aging. (6)
R-Lipoic Acid improves memory, reverses cognitive dysfunction, and protects the brain from neurodegeneration associated with aging. (6) (7) (8) (21)
R-Lipoic Acid protects body fats against oxidative damage and reverses stress damage in the heart. (8)
R-Lipoic Acid supplementation improves metabolic activity and lowers oxidative stress and damage evident in aging. (9)
R-Lipoic Acid significantly increase insulin sensitivity, enhances glucose transport, increases metabolic rate and reduces the gain in body fat from aging. (10) ( 11)
R-Lipoic Acid has insulin-mimetic effects in glucose uptake in insulin resistant cells and may have therapeutic implications in restoring glucose availability in tissues such as the skeletal muscle. (12)
R-Lipoic Acid significantly increases or maintain levels of other antioxidants including Coenzyme Q10, vitamin C, vitamin E and glutathione. (13) (14) (15)
R-Lipoic Acid prevents depletion of the glutathione pool within the cytoplasm and mitochondria. Pre-treatment of PC12 cells with RLA leads to the preservation of mitochondrial complex I activity lost due to glutathione depletion. (14)
The R-(+) enantiomer is much more effective than the S-(-) enantiomer at enhancing insulin-stimulated glucose transport and non-oxidative and oxidative glucose metabolism. (16)
R-Lipoic Acid, through its positive effects on cellular energy metabolism, attenuates metabolic dysfunction associated with advanced glycation endproducts (AGEs). AGEs accumulate on long-lived proteins, including beta-amyloid plaques in Alzheimer's disease and contributes to neuronal dysfunction and cell death.(19) (20)
R-Lipoic Acid, a membrane permeable antioxidant, prevents the up-regulation of the AGE -induced gene expression responsible for regulating nitric oxide (NO) production. NO oxidizes and nitrates proteins which are markers of a chronic neuroinflammatory condition. This mechanism is relevant for Alzheimer's disease and for many chronic inflammatory conditions. (21)
ABOUT S-LIPOIC ACID
Until recently it was believed that S-Lipoic acid was physiologically inactive. Now there are a few reports from the patent literature suggesting this is not the case. There have been no human clinical trials to date that directly compare RLA, SLA and rac- ALA, although this will be forthcoming in the near future. In the meantime, we believe that enough evidence has been reported from in vitro and animal studies to warrant the use of pure RLA over the racemic ALA, when there is a choice.
S-Lipoic acid produces different biological actions than R-Lipoic Acid that may be undesirable. (16-22)
S-Lipoic acid is metabolized in the outer cell membrane or cytoplasm. This may interfere with R-Lipoic Acid's ability to penetrate the inner mitochondrial membrane, thus limiting energy production.
At high concentrations, S-Lipoic acid inhibits mitochondria metabolism. (7)
S-Lipoic acid cannot bind with critical mitochondrial enzymes and inhibits ATP production. (16)
S-Lipoic acid is less effective than R-Lipoic Acid as an antioxidant. (16)
R-Lipoic Acid costs more per unit than alpha-lipoic acid, but it may be 10 times more effective than racemic alpha-Lipoic acid at reducing inflammation; a primary cause of the diseases of aging.