Alpha-Lipoic acid

Alpha-Lipoic acid:

However, they discovered that vitamin-K and, in particular, lipoic acid were highly efficient in killing colon cancer cells. Using a 10:1 ratio of vitamin C to lipoic acid had a synergistic effect and this mixture killed 50 per cent of all cancer cells at a concentration of only 4.5 mM. The researchers conclude that it would be feasible to obtain this concentration by intravenous infusion and urge further work to investigate the use of a combination of vitamin C and lipoic acid as an anti-cancer agent in humans.
Casciari, J.J., et al. Cytotoxicity of ascorbate, lipoic acid, and other antioxidants in hollow fibre in vitro tumours. British Journal of Cancer, Vol. 84, No. 11, June 1, 2001, pp. 1544-50

Quite Possibly the "Universal" Antioxidant

Copyright © 1996 by Jack Challem, The Nutrition Reporter™
All rights reserved.
This article originally appeared in the July 1996 issue of The Nutrition Reporter™ newsletter.

If it's essential role in health is any indication, alpha-lipoic acid may very well join the ranks of vitamins C and E as part of your first-line of defense against free radicals. Discovered in 1951, it serves as a coenzyme in the Krebs cycle and in the production of cellular energy. In the late 1980s, researchers realized that alpha-lipoic acid had been overlooked as a powerful antioxidant.

Over the past few years, the pace of research on lipoic acid has increased dramatically. Last year, Lester Packer, PhD, of the University of California, Berkeley, published a lengthy review article on alpha-lipoic acid in Free Radical Biology & Medicine (1995;19:227-50). In April 1996, he presented a short review of it in the same journal (FRBM;20:625-6).

Several qualities distinguish alpha-lipoic acid from other antioxidants, and Packer has described it at various times as the "universal," "ideal," and "metabolic" antioxidant. 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).

The body routinely converts some alpha-lipoic acid to dihydrolipoic acid, which appears to be an even more powerful antioxidant. Both forms of lipoic acid quench peroxynitrite radicals, an especially dangerous type consisting of both oxygen and nitrogen, according to a recent paper in FEBS Letters (Whiteman M, et al., FEBS Letters, 1996; 379:74-6). Peroxynitrite radicals play a role in the development of atherosclerosis, lung disease, chronic inflammation, and neurological disorders.

Alpha-lipoic acid also plays an important role in the synergism of antioxidants, what Packer prefers to call the body's "antioxidant network." It directly recycles and extends the metabolic lifespans of vitamin C, glutathione, and coenzyme Q10, and it indirectly renews vitamin E.

In Germany, alpha-lipoic acid is an approved medical treatment for peripheral neuropathy, a common complication of diabetes. It speeds the removal of glucose from the bloodstream, at least partly by enhancing insulin function, and it reduces insulin resistance, an underpinning of many cases of coronary heart disease and obesity. The therapeutic dose for lipoic acid is 600 mg/day. In the United States, it is sold as a dietary supplement, usually as 50 mg tablets. (The richest food source of alpha-lipoic acid is red meat.)

"From a therapeutic viewpoint, few natural antioxidants are ideal," Packer recently explained in Free Radical Biology & Medicine. "An ideal therapeutic antioxidant would fulfill several criteria. These include absorption from the diet, conversion in cells and tissues into usable form, a variety of antioxidant actions (including interactions with other antioxidants) in both membrane and aqueous phases, and low toxicity."

"Alpha-lipoic acid...is unique among natural antioxidants in its ability to fulfill all of these requirements," he continued, "making it a potentially highly effective therapeutic agent in a number of conditions in which oxidative damage has been implicated."

Other research on alpha-lipoic acid has shown that it might:

help people with genetic defects leading to muscle myopathies (Barbiroli B, et al., Journal of Neurology, 1995;242:472-7);

reduce ischemia/reperfusion injury to the heart and brain. (Schonheit K, et al., Biochimica et Biophysica Acta, 1995;1271:335-42; and Cao X and Phillis JW, Free Radical Research, 1995;23:365-70); and

inhibit the activation of "nuclear factor kappa-B," a protein complex involved in cancer and the progression of AIDS. (Suzuki YJ, et al., Biochemical & Biophysical Research Communications, 1992;189:1709-15).
"The therapeutic potential of alpha-lipoic acid is just beginning to be explored," observed Packer, "but this compound holds great promise."

The information provided by Jack Challem and The Nutrition Reporter™ newsletter is strictly educational and not intended as medical advice. For diagnosis and treatment, consult your physician.

Lipoic Acid

Other common name(s): Alpha-Lipoic Acid

Scientific/medical name(s): None

DESCRIPTION
Lipoic acid is an antioxidant found in certain foods, including red meat, spinach, broccoli, potatoes, yams, carrots, beets, and yeast (see Broccoli).

OVERVIEW
Lipoic acid is an antioxidant that plays an important role in metabolism. Recent research has shown that it is beneficial in treating nerve damage in diabetics. There is currently no evidence that lipoic acid prevents the development or spread of cancer.

How is it promoted for use?
Lipoic acid is an antioxidant that is promoted to protect the body against cancer and other diseases. An antioxidant is a compound that blocks the action of activated oxygen molecules, known as free radicals, that can damage cells. Oxidation may also play a role in causing poor health as people age, and some researchers claim that lipoic acid is beneficial to maintaining good health in old age. The nutrient has been used to treat diabetic polyneuropathy, a nerve disease found in many diabetics that causes pain and numbness in the hands and feet. In addition to treating nerve damage in diabetics, researchers claim lipoic acid also lowers blood sugar levels.
Promoted as the most powerful and versatile of all the antioxidants, including vitamin E and vitamin C, lipoic acid is claimed to strengthen the effects of other antioxidants and regenerate antioxidants used up in the fight against free radicals (see Vitamin C and Vitamin E). Some proponents believe that lipoic acid may inhibit the gene that triggers cancer cells to grow; however, there is no scientific evidence to support these claims.

What does it involve?
A healthy diet that includes meat and vegetables containing lipoic acid is the best source of this nutrient. The body also produces lipoic acid naturally. As a person ages, his or her body produces less lipoic acid.

Supplements are available in health food stores and on the Internet, but high doses of any antioxidant supplement may actually cause cell damage. A safe and effective dosage of this supplement has not been established.

What is the history behind it?
In 1937, scientists found certain bacteria contained a compound that was later characterized as lipoic acid. The value of lipoic acid as an antioxidant has been known and studied since 1939. In 1957, lipoic acid was isolated and characterized as a compound found in yeast extracts.

What is the evidence?
In a recent review article, researchers reported that a number of experimental studies and clinical trials over the past five years have found alpha-lipoic acid to be useful in treating nerve problems in diabetics and can improve insulin sensitivity in people with type-2 diabetes. They also suggested that it might be useful in liver disease as well. Laboratory and animal studies have found that alpha-lipoic acid is beneficial in treating stroke, cataract formation, HIV infection, nerve degeneration, and radiation injury. There are no scientific studies, however, showing that lipoic acid supplements will directly prevent the development or progression of cancer.

Are there any possible problems or complications?
Lipoic acid found naturally in foods is safe. Research has shown that 300-600 mg of lipoic acid a day may be safely taken with no side effects. Extremely high doses of lipoic acid supplements, however, may damage cells and should be avoided.

References
Ames BN. Micronutrients prevent cancer and delay aging. Toxicol Lett. 1998;102-103:5-18.

Bustamante J, Lodge JK, Marcocci L, Tritschler HJ, Packer L, Rihn BH. Alpha-lipoic acid in liver metabolism and disease. Free Radic Biol Med. 1998;24:1023-1039.

Carper J. The 5 most important antioxidants. Start taking these supplements when you're young and healthy-and stay that way! USA Weekend (Final Edition). April 4, 1999;8.

Fremerman S. Alpha-lipoic acid. Natural Health. 1998;27:151.

Han D, Sen CK, Roy S, Kobayashi MS, Tritschler HJ, Packer L. Protection against glutamate-induced cytotoxicity in C6 glial cells by thiol antioxidants. Am J Physiol. 1997;273:R1771-1778.

Packer L, Witt EH, Tritschler HJ. alpha-Lipoic acid as a biological antioxidant. Free Radic Biol Med. 1995;19:227-250.

Note: This information was reprinted from the American Cancer Society's Guide to Complementary and Alternative Methods. Copyright(c)2000, American Cancer Society. This information may not cover all possible claims, uses, actions, precautions, side effects or interactions, is not intended as medical advice, and should not be relied upon as a substitute for consultation with your doctor who is familiar with your medical needs.

What Is It?
Health Benefits
Forms
Dosage Information
Guidelines for Use
General Interaction
Possible Side Effects
Cautions

What Is It?

In the late 1980s, scientists realized that alpha-lipoic acid, a compound initially classified as a vitamin when it was discovered three decades earlier, possessed potent antioxidant properties that could prevent healthy cells from getting damaged by unstable oxygen molecules called free radicals. In fact, this vitaminlike compound has proved to be many times more potent than such old guard antioxidants as vitamins C and E. As a perk, it even recycles C and E (as well as other antioxidants), enhancing their effectiveness.

Because it dissolves in both water and fat, this so-called "universal antioxidant" is able to scavenge more wayward free-radical cells than most antioxidants, the majority of which tend to dissolve in either fat or water but not both. Alpha-lipoic acid can reach tissues composed mainly of fat, such as the nervous system, as well as those made mainly of water, such as the heart.

Also known as lipoic acid or thioctic acid, alpha-lipoic acid is mainly derived from dietary sources (spinach, liver, brewer's yeast), although scientists have discovered that the body does manufacture small supplies of its own. In order to get the concentrated doses needed to treat specific ailments, however, many experts recommend supplements.

Health Benefits

In addition to functioning as an antioxidant, this hard-working nutrient assists the B vitamins in producing energy from the proteins, carbohydrates, and fats consumed through foods.

Intravenous forms of alpha-lipoic acid are administered in hospitals to treat cases of acute mushroom poisoning and for other cases of acute poisoning that affect the liver.

Studies indicate that alpha-lipoic acid supplements hold promise for treating various disorders, including HIV infection, liver ailments, and glaucoma. But it has been most intensively studied for preventing complications from diabetes.

Specifically, alpha-lipoic acid may help to:

Treat symptoms of nerve damage in people with diabetes. Alpha-lipoic acid has been used for decades in Europe to counter nerve damage in people with diabetes (types 1 and 2). Known as diabetic neuropathy, this often very painful condition tends to develop in people who have had uncontrolled diabetes for a long time. The neuropathy may be caused in part by free-radical damage to nerves resulting from poorly regulated blood sugar (glucose). As an antioxidant, alpha-lipoic acid helps to block such damage. In addition, because of its effect on glucose metabolism, lipoic acid my improve the glucose-lowering action of insulin (the hormone that regulates blood sugar).
In one clinical trial, 328 people with diabetic neuropathy received either 100 mg, 600 mg, or 1,200 mg a day of alpha-lipoic acid for three weeks. Participants who took 600 mg daily had the greatest reduction in pain and numbness. And in a separate study, blood sugar levels dropped in 74 people with type 2 diabetes who took 600 mg or more of alpha-lipoic acid daily.

Alpha-lipoic acid may also aid the large percentage (approximately 25%) of people with diabetes who risk sudden death from nerve-related heart damage. In one study, improved heart function was observed in people at risk for this complication who took 800 mg of alpha-lipoic acid daily for four months.

Preserve brain function in aging adults. Results from animal studies indicate that alpha-lipoic acid may improve long-term memory. Much remains to be learned about whether this occurs in humans, but it may be worth trying this powerful antioxidant when a disease such as Alzheimer's starts to erode memory. In addition, alpha-lipoic acid holds promise for preserving brain cells following a stroke or other type of trauma that restricts blood flow to the brain.

Prevent cancer. As an antioxidant, alpha-lipoic acid holds promise for protecting the body against changes in healthy cells that lead to cancer. The evidence for this cancer-preventive effect is still preliminary, however.

Lessen numbness and tingling. Alpha-lipoic acid may benefit anyone whose limbs tend to tingle or become numb, or "fall asleep" due to nerve compression. In animal studies, alpha-lipoic acid increased blood flow to the nerves and improved transmission of nerve impulses.

Protect the liver in cases of hepatitis and other types of liver disease. As an antioxidant, alpha-lipoic acid shields the liver from potentially harmful cell changes and assists it in flushing toxins from the body. This makes it useful in treating such liver disorders as chronic hepatitis and cirrhosis. Alpha-lipoic acid supplements have also proved effective in minimizing liver toxicity following exposure to poisons such as heavy metals (including lead) and toxic industrial chemicals such as carbon tetrachloride.

Combat chronic fatigue syndrome. Because it plays a part in cellular energy production, some nutritionally oriented physicians recommend alpha-lipoic acid for the treatment of chronic fatigue syndrome. While evidence of its effectiveness for this condition is anecdotal, alpha-lipoic acid is a broad-spectrum antioxidant and immune system booster. This means it may be able to play a valuable role in increasing energy and maintaining overall health in chronic fatigue syndrome sufferers.

Reduce the incidence of cataracts. Alpha-lipoic acid has kept cataracts from forming in animals, an effect that may occur in humans, too, but still requires more investigation. The compound also increases the potency of vitamins C and E, both nutrients that protect the eye's lens from harmful ultraviolet light.

Forms

tablet
capsule
Dosage Information

Special tip:

You can buy alpha-lipoic acid either as a single supplement or in combination products with other antioxidants, such as vitamins C and E.

For general antioxidant protection: Take 100 mg twice a day.

To preserve brain function in aging adults: Take 100 mg twice a day.

To prevent complications of diabetes: Take 200 mg twice a day to guard against related conditions such as cataracts, macular degeneration, and heart disease. In addition, make sure to get 1,000 mg vitamin C and 400 IU vitamin E daily.

For diabetic neuropathy: Take 200 mg three times a day.

For numbness and tingling: Take 200 mg twice a day.

For hepatitis: Take 100 mg twice a day. In addition, take 1,000 mg vitamin C and 400 IU vitamin E daily.

For preventing cataracts: Take 100 mg twice a day.
Be sure to check our Dosage Recommendations Chart for Alpha-lipoic Acid, which lists therapeutic dosages for specific ailments at a glance.

Guidelines for Use

Alpha-lipoic acid can be taken either with or without food.

General Interaction

If you have diabetes, taking alpha-lipoic acid for long periods may require an adjustment in your dosage of insulin or other diabetes medications. Consult your doctor for guidance.
Note: For information on interactions with specific generic drugs, see our WholeHealthMD Drug/Nutrient Interactions Chart.

Possible Side Effects

Alpha-lipoic acid is very safe at commonly recommended dosages, although occasionally it causes mild stomach upset and in rare cases it can trigger an allergic skin rash. If you experience any of these reactions, reduce the dose or stop taking the supplement.

Cautions

If you suffer from any type of medical condition, consult your doctor before trying alpha-lipoic acid supplements.

Don't take alpha-lipoic acid if you are pregnant

Alpha-Lipoic acid

20mg/hour 300-600mg/day

Alpha Lipoic Acid 200mg 60t SN 0395 $NZ24.05

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