Lipoic acid in a nutshell:
Lipoic acid can be found in various forms and are excellent antioxidants. Our bodies can make it and it is not a vitamin. It is commonly used to help treat insulin resistance.
Best source of Lipoic acid for Juicers
It has been suggested that Lipoic acid can be obtained from potatoes, but actually they contain very little. Better sources of lipoic acid are tomatoes, broccoli, spinach & Brussels sprouts.
The various forms of lipoic acid are extraordinarily versatile antioxidants. They are optimally effective, however, when they are taken with vitamins and amino acids that act as their co-factors.
Alternative names: Lipoic acid, alpha-lipoic acid; R-lipoic acid; thioctic acid.
What Is Lipoic Acid?
Every living thing that consists of at least one cell surrounded by a membrane makes lipoic acid. The energy-making centers of the cell, the mitochondria, combine sulfur with an eight-carbon (n-8) fatty acid called octanoic acid to make lipoic acid. Since our bodies can make lipoic acid, it is not a vitamin, but supplemental lipoic acid can be very useful in supporting recovery from several disease conditions.
Lipoic acid is a “chiral” molecule. This means that it has a configuration that makes it impossible for the molecule ever to fit over its mirror image, much as your physical left hand cannot be made to fit over the mirror image of your right hand. The kind of lipoic acid that occurs in nature has a “rightward” orientation. The process of making artificial lipoic acid creates both “rightward” or R-lipoic acid and “leftward” or S-lipoic acid (S- being the abbreviation for “sinister,” an older term for leftward orientation). Most industrial processes result in the formation of about 45% R-lipoic acid and about 55% S-lipoic acid.
It’s harder to make pure R-lipoic acid than it is to make a mixture of R-lipoic and S-lipoic acid. A bottle of R-lipoic acid may cost up to US $50, while a bottle of mixed R- and S-lipoic acid is almost always $10 or less.
What Does Lipoic Acid Do in the Human Body?
Some manufacturers will play on the term “sinister” and tell you that mixtures of the two different forms of lipoic acid are somehow sinister and harmful to your health and that the more expensive product is better for you. That’s not entirely correct. In fact, there is strong evidence that the less expensive product is actually more helpful for human health.
R-lipoic acid (which is actually absorbed into the body as sodium R-lipoate) is the form of the antioxidant that can enter cells and do its work at the level of the mitochondria. S-lipoic acid (which is actually absorbed into the body as sodium S-lipoate) can’t exert antioxidant action inside cells, but it is still useful as an antioxidant outside cells, in the blood plasma. Some experts have argued that since you really want lipoic acid to go inside your cells, you need to take the pure R-lipoic acid in supplements.
Antioxidant expert Dr. Lester Packer of the University of California at Berkeley and his colleagues, however, have found that pure R-lipoic acid fails to travel to its intended destinations. R-lipoic acid by itself tends to be absorbed by cells in the lining of the digestive tract and never gets into the bloodstream.
Pure R-lipoic acid is poorly dissolved in water. It tends to form stringy polymers that just get flushed away by bowel movement. R-lipoic acid that is part of a mixture of S- and R-lipoic acid is more likely to find its way into the bloodstream so it can be absorbed by tissues in the rest of the body.
In other words, when it comes to lipoic acid, the cheap stuff works better. In fact, it works a lot better. Dr. Packer and his team found that a mixture of R- and S-lipoic acid delivers 25 times more lipoic acid into the bloodstream and 3.3 times more lipoic acid into cells than R-lipoic acid alone in men. A mixture of R- and S-lipoic acid delivers 17 times more lipoic acid into the bloodstream and 2.7 times more lipoic acid into cells in women. Dr. Packer also found that obese people absorb more lipoic acid from supplements than underweight people, because the antioxidant is both fat- and water-soluble.
If you have read what nutritional product companies write about their products, chances are this is the exact opposite of what you have read. Dr. Packer and colleagues published their research in an article entitled “The Plasma Pharmacokinetics of R-(+)-Lipoic Acid Administered as R-(+)-Sodium Lipoate in Healthy Human Subjects” in the December 2007 edition of Alternative Medicine Review.
How to Take Alpha-Lipoic Acid
Since some German researchers gave their subjects intravenous lipoic acid in doses of 2,000 mg per day 20 years ago, many nutritional “experts” have been advising people to take oral lipoic acid supplements in doses of 2,000 mg once per day ever since. That’s been bad advice. The body just can’t absorb that much lipoic acid at one time. About 600 mg of lipoic acid is all the gastrointestinal tract can absorb at one time, although you might be able to take three doses of 600 mg at separate times (at least four hours apart) during the day.
It’s especially wasteful to take more than 600 mg of R-lipoic acid at one time, since it is only partially soluble in water.
It also doesn’t make sense to take lipoic acid without its cofactors. In the mitochondria, the antioxidant action of lipoic acid requires the B vitamin biotin, the B vitamin niacin (in the form of nicotinamide), and the amino acid L-carnitine for optimum activity. If you take 600 mg of lipoic acid, you need at least 100 mg of biotin, 100 mg of nicotinamide, and 1200 mg of L-carnitine. You don’t have to take these nutrients at exactly the same time or in exactly the 1 to 6 or 2 to 1 ratios listed here, as long as you take all the nutrients in at least these amounts the same day. Since lipoic acid can chelate, or tie up, manganese, zinc, and copper, it also is a good idea to take a mineral supplement that contains trace minerals once or twice a week.
You shouldn’t take lipoic acid in any form if you are deficient in thiamin (vitamin B1). Thiamin deficiencies are very rare, but they sometimes occur in:
- People who have celiac disease,
- People who have a condition called small intestine bacterial overgrowth or who have poor circulation to the small intestine (both common in people who have had type 2 diabetes for 10 years or more),
- Diabetics who use the maximum amount of the medication metformin (2550 mg per day) and
- People who eat lots of sugar.
It’s very simple to take care of any thiamin deficiency with an inexpensive daily supplement that is available over-the-counter even in the highly regulated European Union.
If you use the right (cheaper) form of lipoic acid with the right complementary nutrients, however, some amazing results are possible.
Can You Really Get Your Lipoic Acid from Potatoes?
In the United States, a story originating with Natural Health News claiming that potatoes are a good source of lipoic acid has been spreading across the Internet. Potatoes in fact do contain small amounts of lipoic acid, but there is far more in organ meats, tomatoes, broccoli, spinach, Brussels sprouts, and brown rice. Diabetics who eat potatoes for their lipoic acid content may notice that their blood sugar levels don’t go up as much as otherwise expected, but potatoes will not make blood sugar levels go down.
Using Lipoic Acid in Type 2 Diabetes
By far the most common application of lipoic acid supplements is in treating insulin resistance, the underlying cause of type 2 diabetes. Insulin resistance tends to get defined as “resisting insulin,” but what happens in insulin resistance is a progressive “switching off” of insulin receptor ports on liver and muscle cells.
When cells sense high blood sugar levels, they reduce their ability to use insulin so they are not flooded with sugar. Keeping sugar out of the cell prevents burning more sugar than the cell’s antioxidant systems can manage safely. Burning large amounts of sugar would produce large amounts of free radicals that could damage the DNA and outer membrane of the cell, causing dysfunction or death.
As cells become insulin resistant, blood sugar levels rise. The pancreas also senses blood sugar levels and responds by producing still more insulin. For a short time, the additional insulin forces sugar out of the bloodstream and into cells. When this happens, however, cells switch off still more insulin receptor sites to protect themselves.
The pancreas releases still more insulin. Cells over almost all of the body become even more insulin resistant. Eventually the pancreas cannot keep up and diabetes sets in.
As an antioxidant, lipoic acid makes it safer for cells to burn sugar. They reverse their insulin insensitivity and blood sugar levels fall. Actually, when lipoic acid is administered intravenously, “plummet” would be a better way to describe the change in blood sugar levels. In one experiment, intravenous dose of just 1000 mg of lipoic acid resulted in a 50% increase in the rate at which sugar is cleared out of the bloodstream. An intravenous dose of 500 mg of lipoic acid resulted in a 30% increase in the rate at which sugar was cleared out of the bloodstream.
No medication other than insulin itself comes even close to this. And because insulin stores fats as well as sugar, lipoic acid has the enormous advantage of not causing weight gain.
The problem with lipoic acid therapy for diabetes is that it is almost impossible to persuade doctors to give intravenous lipoic acid and diabetics have to rely on over the counter supplements. Oral lipoic acid does not produce equally dramatic results. But it does produce results.
Medical scientists at the University Hospital of Endocrinology in Sofia, Bulgaria recruited 12 men who had type 2 diabetes to be treated with 600 mg of oral lipoic acid taken twice a day, for a total dosage of 1,200 mg per day. In lean diabetics, lipoic acid significantly reduced insulin resistance. In overweight diabetics, it did not.
The reason isn’t hard to understand. Lipoic acid is soluble in fat and accumulates in fat cells. In diabetics who are overweight, lipoic acid goes to fat rather than to muscle. Since muscles use up to 50 times more sugar than other kinds of tissue during exercise, the benefits of lipoic acid are greatest in lean diabetics who exercise. Of course, by the time a diabetic has lost a lot of weight by exercise, he or she probably does not have as great a need for lipoic acid.
But that doesn’t mean that lipoic acid isn’t helpful for diabetics who are overweight. It just has to be combined with the biotin, nicotinamide, and L-acetyl-carnitine mentioned above to increase fat burning in fat cells—and fat cells don’t burn fat when they are storing it. Lipoic acid won’t work when diabetics overeat.
Using Lipoic Acid to Treat Diabetic Neuropathy
Neuropathy is a common complication in diabetes that has been poorly controlled for 5 years or more. Neuropathy is a condition of nerve cell destruction caused by the accumulation of free radicals in the mitochondria, the energy-making centers, of nerves.
Diabetic neuropathy can cause numbness, tingling, burning, and poor reflexes that are especially noticeable at the ends of nerves that extend from the spine to the hands and feet. This is because these nerves, which can be over a meter/3 feet long, suffer damage to their mitochondria caused by high blood sugar levels. The nerve makes new mitochondria at its end closest to the spine, and it can take several years for them to migrate to the tips of the fingers or the toes. In the meantime, high blood sugar levels can kill the mitochondria on the way to their distant destinations.
Since alpha-lipoic acid protects mitochondria, it is used to treat diabetic neuropathy. Most clinical studies have used 600 mg of lipoic acid per day. The usual finding is that using lipoic acid stops the progression of the disease and reduces symptoms slightly. It usually does not cure diabetic neuropathy—but careful control of blood sugar levels can do that in a year or so even when diabetics don’t take any supplements. Very few diabetics, however, actually manage to control their blood sugar levels with taking care to stick to their diets every day of the year.
Using Lipoic Acid to Prevent Diabetic Cataracts
Diabetics are especially susceptible to the formation of cataracts, clouding of the lens of the eye. High blood sugar levels cause the proteins in the lens to link to each other in a star pattern, allowing light through but distorting images.
Lipoic acid prevents this kind of damage to the lens of the eye by recharging vitamins C and E, which in turn recharge a naturally occurring antioxidant known as glutathione peroxidase. It inhibits an enzyme called aldose reductase, which converts glucose into a tissue-damaging sugar known as sorbitol, which can harm not only the lens but the retina.
Lipoic acid also acts as a natural chelation therapy, removing excess copper and iron from the eye, keeping them from generating free radicals that can “cook” the proteins in the lens of the eye.
Using lipoic acid is not a guarantee against developing cataracts, and it won’t treat them once they occur. Including lipoic acid as part of a program of controlling blood sugar levels, however, may also reduce the risk of eventually needing cataract surgery.
Using Lipoic Acid to Treat Glaucoma
Russian scientists have conducted about a dozen studies of lipoic acid as a treatment for chronic or open-angle glaucoma. (Acute or closed-angle glaucoma is a medical emergency you should not attempt to treat on your own.) Most studies have found that using at least 150 mg of lipoic acid per day lowered ocular pressure—but not enough to make other treatments unnecessary.
Using Lipoic Acid to Treat Lead Exposure
In Europe, Australia, New Zealand, Canada, and the United States, leaded gasoline and lead-based paints were banned long ago. Once a common problem for children growing up in inner cities, lead poisoning has become a thing of the past in most of these countries.
In China, India, and much of the Middle East, Africa, and Latin America, however, lead exposure is still a common feature of everyday life. Even people who live in unpainted houses in remote locations are often exposed to lead in pottery, cosmetics, and, bizarre as it may seem, over the counter medications. Most of the people living on the planet today are still exposed to toxic amounts of lead.
Lipoic acid in small doses, 100 to 200 mg per day, can offset some of the pro-oxidant effects of lead. One of several ways that lead causes tissue damage is by the production of free radicals of oxygen. Lipoic acid recharges vitamins C and E which in turn recharge glutathione, which quenches free radicals of oxygen and converts them into harmless forms. A comprehensive antioxidant support program for lead exposure would include 100 to 200 mg of lipoic acid, 5000 IU of beta-carotene, just 100 to 200 mg of vitamin E, 100 IU of vitamin E, and 25 mg of zinc daily. These nutrients counteract the effects of lead but they do not chelate and remove lead from the body. This is done with EDTA chelation.
Lipoic Acid in Skin Care
Skin care products containing lipoic acid were heavily promoted in the 1990’s in the United States on the Oprah show. Lipoic acid in skin creams really does help shrink sags and bags of skin and can even reduce outward-protruding acne scars. Alpha-lipoic acid is included in products for fading age spots and it is used to treat a precancerous condition known as actinic keratosis.
The right kind of packaging is critical for skin care products that contain any kind of antioxidant. Skin care products that come in jars begin to degrade just as soon as the jar is opened. Skin care products that come in tubes don’t lose their antioxidant potency as the product is used up.
Unlike retinoic acid (vitamin A), lipoic acid is almost always safe on sensitive or allergy-prone skin. Just be sure to test a small dot of any skin care product on the back of your arm, leaving it there for several hours, to make sure it does not cause any kind of adverse skin reaction, before putting the product on your face.
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