What is Alpha Lipoic Acid?

Alpha lipoic acid, also known as thioctic acid, is a disulfide compound that is a co-factor in vital energy-producing reactions in the body.  It is also a potent biological anti-oxidant.  The body needs alpha lipoic acid to produce energy, where it plays a crucial role in the mitochondria (the energy-producing structures in the cells),  The body normally makes sufficient alpha lipoic acid for basic metabolic functions, but alpha lipoic acid acts as an anti-oxidant only when it is present in excess amounts and it is present in the “free” state in the cells. 

Since there is little free alpha lipoic acid circulating in the body, alpha lipoic acid must be consumed or injected to exert an anti-oxidant effect.  Since foods contain only tiny amounts of alpha lipoic acid, oral supplementation is the preferred method to achieve adequate distribution of free alpha lipoic acid throughout the body to exert its biological anti-oxidant effect.  Because alpha lipoic acid is a regenerator of vitamins E and C, is soluble in the aqueous and fatty phases of cells, and has been reported to raise glutathione levels, it has often been referred to as the “universal” anti-oxidant.

Energy, Oxidative Stress, and Declining Natural Protection.

The Body´s Engine Room

Humans derive energy from the mitochondria found in all cells, through the complex process of cellular respiration.  The process uses the oxygen we breathe to "burn" or "convert" glucose and fatty acids (from food) to chemical energy.  This chemical energy is stored in the form of ATP (adenosine triphosphate) molecules, which subsequently give up that energy when required.  During the respiration process, reactive oxygen species, or free radicals are formed that would be highly destructive to the cell structures if they were not neutralized by natural cellular anti-oxidants, most notably glutathione.  This natural process works effectively under normal conditions, but begins to break-down with aging and with abnormal metabolic conditions.  This break-down is reflected by a decline in the ability of natural anti-oxidants like glutathione to neutralize the free radicals produced in the cell.  This condition is called "oxidative stress" and is believed to be a major contributor to cellular aging and the degenerative diseases that accompany aging, such as cancer, cardiovascular disease, immune system decline, brain dysfunction, and cataracts.

Glutathione:  Alpha Lipoic Acid’s Best Friend

Glutathione is the body's primary defender against free radicals, but it cannot be taken in oral supplement form to counteract oxidative stress.  Naturally occurring anti-oxidants in fruits and vegetables can be of great benefit in counteracting oxidative stress, but are generally not consumed in sufficient quantities by the average individual.  Alpha lipoic acid supplementation provides a powerful, convenient and inexpensive means of augmenting the body's natural anti-oxidant defense system.    The alpha lipoic acid molecule is soluble in aqueous and lipid compartments of the body (unlike Vitamin C and Vitamin E), crosses the blood brain barrier, and regenerates oxidized glutathione, Vitamins C & E, and Coenzyme Q10.   Unlike drugs that are designed to alter metabolic functions, alpha lipoic acid helps to restore normal oxidative balance, and positively impacts overall well-being through its other beneficial biological properties.


How Is Alpha Lipoic Acid Being Used?

Pertinent Reports From Credible Sources.

Since it became widely available to the general public in the late 1990's, alpha lipoic acid has been used by millions of consumers to deal with conditions ranging from simple cosmetic embellishments, to counter-acting serious chronic degenerative conditions.   Because the remarkable biological properties of alpha lipoic acid have made it one of the most widely recommended nutritional supplements, a great deal of research-based and marketing-based information has been disseminated about the effectiveness of alpha lipoic acid for dealing with many diverse health concerns.  As supplement marketers become more "sophisticated", it is often difficult to distinguish between marketing hype and unbiased research reports.  There are many credible sources of information about the effectiveness of natural substances, including government agencies, universities, natural product associations, and private endeavors.  These sources tend to be conservative with respect to the level of proof they require to deem a substance effective, but generally add needed balance to the pseudoscientific extrapolation techniques employed by most supplement marketers.  There are too many credible sources to provide a comprehensive list, but some that stand out are "Natural Medicines" Comprehensive Database,  The PDR for Nutritional Supplements, and The Linus Pauling Institute.  These sources are in general agreement that alpha lipoic acid is effective for use in diabetic neuropathy, insulin resistance, and relief of oxidative stress. 

Mayo Clinic Study

Alpha lipoic acid is an approved drug in Germany for the treatment of diabetic neuropathy, but such a claim is not permissible in the United States without submission of substantiating clinical data and approval of the claim by the FDA.  Numerous clinical studies have been conducted on alpha lipoic acid for diabetic polyneuropathy, with most studies confirming that intravenous alpha lipoic acid improves neuropathic symptoms, with less clear-cut data reported on the use of oral alpha lipoic acid.  A study conducted by Peter Dyck, M.D. at the Mayo Clinic showed a large and rapid response in alleviating the pain of diabetic neuropathy when alpha lipoic acid was administered intravenously, but oral dosing had not been evaluated.

The difference in treatment effectiveness between intravenous and oral alpha lipoic acid is not unexpected, considering the poor solubility and absorption of alpha lipoic acid crystals, and underscores the importance of enhanced absorption and bioavailability formulations.  A recent article in the Netherlands Journal of Medicine reviewed all clinical studies with alpha lipoic acid for diabetic neuropathy and found that neuropathy symptoms were reduced by 50%.  They found that taking alpha lipoic acid by mouth was beneficial, and there was significant improvement with neuropathy pain with intravenous infusions.

A Healthy Lifespan

Dr. Tory Hagen from the Linus Pauling Institute has studied the wide range of beneficial functions of alpha lipoic acid and concluded that “it is a remarkable compound that in animal experiments appears to slow down the process of aging”.  Dr, Hagen found evidence that alpha lipoic acid was a low-level stressor that turns on the basic cellular defenses of the body, including some that naturally decline with age.  In particular, alpha lipoic acid tends to restore levels of glutathione to those of a young animal.  In light of our aging epidemic, along with skyrocketing diabetes, high blood pressure, and heart disease, the diverse beneficial effects of alpha lipoic acid make the molecule a compelling interventional option.  Dr. Hagen’s studies have shown that mice supplemented with alpha lipoic acid have a cognitive ability, behavior, and genetic expression of almost 100 detoxification and anti-oxidant genes that are comparable to that of young animals. Dr. Hagen commented that “We never really expected such a surprising range of benefits from one compound. This is really unprecedented and we’re pretty excited about it”.  Dr. Hagen's anti-aging interest is focused more on the potential use of alpha lipoic acid to make the later years in life healthier, than on the extension of life.

Protecting Your Liver

Our modern world has become an inhospitable environment for the overall well-being of the human liver.  In addition to infectious agents like the hepatitis c virus, the liver is exposed to a wide array of herbicides, pesticides, preservatives, mycotoxins, pollutants, and all-nature of chemicals that are used in food-processing and packaging and most other elements of our daily existence.  If that weren’t a big enough job for this critical detoxifying organ, the liver is also under attack from fat cells that accumulate in the liver of obese individuals.

Liver disease starts with inflammation, and if left untreated over time, inflamed liver tissue starts to scar or becomes fibrous.  If fibrosis is not treated or healed, irreversible damage can occur, called cirrhosis, which in turn can lead to liver cancer.  If the liver loses most or all of its functioning cells, a life-threatening condition called liver failure can occur.

Dr. Burton Berkson was an early pioneer in the use of alpha lipoic acid in liver disease, using intravenous alpha lipoic acid to treat acute liver failure associated with mushroom poisoning.  These early studies sparked Dr. Berkson’s interest in the remarkable alpha lipoic acid molecule, and he has continued to study the compound over the past 30 years, most notably exploring it’s use in treating hepatitis c in a triple antioxidant regimen.  Dr. Berkson’s successful use of alpha lipoic acid to treat three hepatitis c patients was first reported in 1999, and has since been updated in 2007 in an article in the Townsend Letter.  Two of the three patients still see Dr. Berkson and continue to improve after almost 10 years of treatment. 

The key consideration in the use of alpha lipoic acid in hepatitis c and other liver diseases is protection and regeneration of the liver cells.  Alpha lipoic acid does not eradicate the hepatitis c virus in patients who are unresponsive to interferon therapy, but protects the liver cells from progression to liver fibrosis and liver failure.  It is generally believed that alpha lipoic acid exerts this effect through anti-oxidant protection of lipid structures in the cell, but just published research suggests that alpha lipoic acid also inhibits the progression to liver fibrosis by inhibiting hepatic plasminogen activator inhibitor (PAI-1) expression by inhibition of the signaling pathway.  If this study is confirmed in further research, alpha lipoic acid will add another profoundly important biological property to its already impressive portfolio.

What the leading authority on Alpha Lipoic Acid has said about "The Miracle Molecule."

Alpha Lipoic Acid Is More Than An Anti-Oxidant

The anti-oxidant properties of alpha lipoic acid have been extensively detailed in the scientific literature, based on laboratory, animal, and human clinical studies. Most researchers attribute the many beneficial effects of alpha lipoic acid to the neutralization of free radicals associated with oxidative stress, but as the studies have become more sophisticated, other mechanisms of action are being uncovered. The discovery of unique biological activities associated with natural substances is a murky area that leads many supplement suppliers to the dangerous ground of "pseudoscientific extrapolation". Because a natural substance demonstrates a biological activity in a laboratory beaker, a laboratory animal, or even in a human trial, is not adequate proof that the substance will favorably impact a disease state or overall well-being.

Recognizing the need to avoid premature speculation on the importance of a specific property of a natural substance, it is important to obtain unbiased assessments from credible sources. One of the most credible sources on the usefulness of natural substances is The Linus Pauling Institute at Oregon State University http://lpi.oregonstate.edu), where alpha lipoic acid is a major focus of their research program. Below is a summary of what is known about alpha lipoic acid, as reported by the Linus Pauling Institute:

LPI Summary

  • Alpha-lipoic acid (LA), also known as thioctic acid, is a naturally occurring compound that is synthesized in small amounts by humans.

  • Endogenously synthesized LA is bound to protein and functions as a cofactor for several important mitochondrial enzymes.

  • Supplementation with high doses of LA transiently increases plasma and cellular levels of free LA.

  • Although LA is a potent antioxidant in the test tube, LA supplementation may affect health by stimulating glutathione synthesis, enhancing insulin signaling and modulating the activity of other cell signaling molecules and transcription factors.

  • Overall, the available research indicates that treatment with 600 mg/day of intravenous racemic LA for 3 weeks significantly reduces the symptoms of diabetic peripheral neuropathy.

  • Although the benefit of long-term oral LA supplementation for diabetic peripheral neuropathy is less clear, there is some evidence that oral supplementation with at least 600 mg/day of racemic LA may be beneficial.

Alpha Lipoic Acid and Non-Alcoholic Fatty Liver Disease Video by Dr.Harper