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Alpha Lipoic Acid Supplement Review and Benefits
Lipoic Acid - The Undiscovered Wonder

By Wesley James
http://www.pipeline.com/~wjames/MuscleMaker/

If I promised to tell you about the least known, most bio-active nutritional substrate that has been discussed in a bodybuilding magazine this year, would you read the rest of this article? I hope so because it could mean a 40% energy increase, a 32% improvement in your recovery capacity. It could also mean a 2% lower bodyfat percentage in a year, without changing your diet. Read on!


Catabolism

You would never know it from most bodybuilding literature but catabolism is a natural, necessary, even beneficial process. According to some sources, a healthy individual must replace every cell in their body every seven to nine years. Catabolism is an essential part of this cycle. Our bodies use multiple catabolic pathways. Bodybuilding publications most often discuss Cortisol as the agent of catabolism but it is far from the only tissue destroyer. The entire family of Glucocorticoids, of which Cortisol is only one member, are tissue wasters. There are numerous other catabolic substances at work in our bodies as well. Cumulatively they disadvantage the body's recovery capacity, which for a collection of complex reasons is already at a roughly 6:1 disadvantage.

Over the last forty years a number of anti-catabolic agents have been discovered. Some of these are drugs, like Anabolic Steroids and Clenbuterol. Others are nutritional supplements; for example, Hydroxy-Methyl-Butyrate (HMB), Ornithine Keto-Glutarate (OKG), Phosphatidyl-Serine (PS) and Keto-Iso-Caprionate (KIC). Through differing means, the form of catabolism addressed by each of these substrates is the micro-trauma and stress of exercise. While largely disregarded, some of the most significant damage to our cells is created completely apart from exercise. One form of catabolism is particularly insidious because its agent is the very fuel that allows the body to function, glucose. The process is called Glycation. It is best known for the often fatal harm it does to diabetics': retinopathy, neuropathy, nephropathy and atherosclerosis. While less recognized, the degenerative effects of glycation occur in everyone, all the time, simply because glucose circulates in our blood.


Glycation

Glycation occurs when portions of glucose molecules latch on to tissue proteins, tearing them from the tissue or leaving Advanced Glycosalation End-products (AGE) in their wake. This glycation damage sometimes ruptures the tissue, triggering still further breakdown. It frequently leaves dysfunctional or dead cells in place, albeit with reduced tissue integrity. It always increases the demand on the system for repair enzymes and protein re-synthesis. When AGE compounds are left in tissue, they compromise both the structure and function of that tissue. Since our bodies have a finite capacity for repair and re-synthesis, the result is not only catabolic but progressively debilitative.

While sometimes accepted as a natural part of the aging process, glycation is more akin to the type of oxidation that causes and produces free-radical destruction of body tissue. Increasingly in recent years, these processes are being viewed as constrainable. Just as life-extension scientists have come to realize that antioxidants can protect the body against maladies caused by free-radicals (about 80 non-germ related diseases), they have learned that a rarer breed of substrate can protect against glycation damage. Interestingly, the best protector against glycation is also a very rare, if not unique, antioxidant. Unlike Vitamin C which is normally only soluble in water or Vitamin E which is normally only soluble in oil (fat), this nutritional marvel is soluble in both. The compound to which I refer is Lipoic Acid (or Alpha Lipoic Acid). If you've never heard of it, you've been missing a truly wondrous protein sparing, anti-glycatant, anti-glycemic, antioxidant and chelating agent. Substantial research indicates it can aid in modulating metabolism, increasing energy and enhancing our effective recuperative capacity. That's a powerful lot of benefit from one nutritional supplement but there's much, much more. Stay with me.


Lipoic Acid - Structure and Benefit

Alpha Lipoic Acid or simply Lipoic Acid was for many years called Thioctic Acid. Many still refer to it by this name. All these names are valid. "Alpha Lipoic" indicates that there is a Lipo or fat molecule in the Alpha or first position. This is true of this compound. "Thioctic" indicates that there is Sulphur (Thio) present. This is also true of this molecule. In fact, there are two Sulphur atoms attached to this eight-carbon chain, at positions six and eight. Thus, what we have is Octanoic Acid (an eight carbon version of carboxylic acid) combined with Cysteine, a protein which contributes the Sulphur atoms. Anyway, for many years its role in the body was unknown, except as a co-factor in some metabolic reactions. Along about 1951, during tests of a host of organic compounds, it was discovered that Lipoic Acid acted as a powerful in vitro antioxidant. This was considered all the more interesting because in emulsified foods, containing both water and oil, it protected both components from spoilage. It was also noted that sugar fermentation which can occur even without other breakdown processes was affected. This triple effect made Lipoic/Thioctic Acid a prime candidate as a food preservative. Unfortunately, Lipoic Acid affects the taste and mouth-feel of foods. (It creates foam and tastes, some say, like soap.) This makes it unattractive for this purpose for which it is otherwise so well suited. Food scientists, therefore, largely dismissed this interesting molecule. Argument, however, arose among biochemists about what category of substrate it was. Some scientists were ready to declare it the first fat soluble B vitamin. Others wanted to declare it an essential co-enzyme. Since it was discovered that the body could produce some Lipoic Acid, it was not, strictly speaking, essential. Moreover, no one disease could be directly linked to a deficiency of Lipoic Acid. (Although it cures scurvy in Vitamin C deficient individuals and cerebro-cortical atrophy in cases of clinical hypotonia.) In any event, status as a vitamin was denied. Science was left to view Lipoic Acid as a non-essential, or at best "conditionally essential", co-enzyme and antioxidant. This doesn't begin to describe how amazing this metabolite is, but it does help explain why it was so easily initially overlooked.

Thioctic Acid came under examination again as a protection against the effects of alcohol. It failed, however, to block alcohol's effect and actually increased the duration of alcohol intoxication by slowing the systems efforts to break it down. Although it did succeed at significantly detoxifying its by-products, it also aggravated the Vitamin B-1 deficiency frequently accompanying alcoholism. (Thiamine is a co-factor in many Lipoic Acid reactions.) Regardless, bodybuilders should celebrate its commercial availability. Lipoic Acid offers a wide variety of very significant benefits to the health minded, drug free bodybuilder. At levels as low as 30 Mg per day it can, over time, become a part of every cell in the body, protecting those cells from the ravages of oxidative damage. Once present it reduces glycation related damage as well, slowing and reducing the demand for cell replacement. Anything that reduces cell breakdown is, by definition, anti-catabolic. Since cell replacement in the presence of oxidative free-radicals increases the likelihood of cancerous mutation, Alpha Lipoic Acid is also anti-carcinogenic. Its ability to enter the nuclei of cells can also prevent oncogenic gene triggering by protecting against NF-Kappa-B reduction. If you are confused by all that, you need only retain that this makes Lipoic Acid doubly anti-carcinogenic.

In summary, for the bodybuilder, its action is anti-catabolic through its protein sparing effect and its cell replacement demand reduction. It is also powerfully anti-carcinogenic. Further, it synergistically reinforces and recycles antioxidant vitamins and glutathione. Finally, in Europe it is used to control blood sugar levels and reduce the damage associated with primary and secondary diabetes. This has extraordinary implications for bodybuilders as we will see. It can even encourage the regeneration of nerve cells destroyed by diabetic neuropathy. We will explore these functions later as well. For now you should realize, we're talking about an exceptionally beneficial substrate which in addition to all the above is helpful against Cataracts, Alzheimer's, Parkinson's and, excitingly, HIV/AIDS.


ACTIVITY
Anti-Glycation

To better understand how these benefits accrue it will help to have a few facts. Glucose is a relatively stable compound even in solution but in the presence of oxygen, particularly at temperatures above 70 degrees, it becomes less stable. In blood it will breakdown into shorter chains. Some of these chains are quite reactive. One in particular, hydroxyl, has a strong affinity for protein. Generally blood is too alkaline to allow these radicals to run rampant but the local release of lactic acid, an exercise by-product, can acidify tissue. Other conditions can also produce varying degrees of acidosis. Even acidic (sour tasting) foods may be sufficient. Notably, the ketosis that occurs during low carbohydrate dieting reduces pH quite enough to allow such reactions to run amuck. During these periods of acidosis, the broken glucose chains aggressively leech protein from muscle, skin, nerve and connective tissue cells, compromising their structural integrity and demanding their replacement. Some cells die but are not replaced, accelerating the aging process. Others require special enzymes to allow the repair of the damage. If the conducive environment was produced by lactic acid, glycation amplifies the catabolic effect. Glycation is one of the ways people lose muscle as they age. It is a principal cause of the progressive devastation of diabetes. Of particular concern to athletes, it weakens our connective tissue, increasing the likelihood of injury. Further, glycation does not stimulate GH release to signal the need for repair of the damage it creates. As a result, the damage is often cumulative, contributing to reduced functional efficiency of the damaged tissue and thus progressive debility. In the next section we will see how Lipoic Acid helps solve this problem.


Blood Sugar Regulation

Over the last few years, bodybuilders have become increasingly aware that the regulation of blood glucose levels is important to them in a variety of ways. This knowledge has lead to the use of Chromium Picolinate and Vanadyl Sulfate as nutritional supplements among drug-free athletes. It has also lead to the use of exogenous Insulin and Sulfonylurea drugs among other individuals in spite of the grave danger associated with such action. Somehow, in all the rush to regulate blood sugar, Lipoic Acid has been ignored. This oversight is unfortunate because Lipoic Acid is not only relatively safe but exceptionally effective in this role. Here's how it works.

As Creatine users have come to appreciate, Adenosine Tri-Phosphate (ATP) is the fuel the body uses in muscle. Less discussed is how the body converts glucose into ATP. The process is a bit complex and probably only of interest to biochemists but it occurs through a series of chemical reactions. What is relevant here is that on the way to becoming ATP, glucose becomes Pyruvate which becomes Acetyl-Co A which via further reactions, called the Krebs cycle, eventually becomes ATP. It is a multistage process. You also need to know that Lipoic Acid, while only a co-factor in many of these reactions, is regulating. Within limits, increasing the availability of Lipoic Acid increases the quantity and rate of glucose conversion to stored energy. More important for us as bodybuilders, Lipoic Acid increases the amount of ATP muscle can and will store. A muscle that stores more ATP can perform more reps before becoming depleted. Without changing any other parameter, the addition of supplementary Lipoic Acid can, like Creatine, make you stronger. Perhaps more exciting, it accomplishes this increase in strength at the expense of fat storage. Let's look at how.

In a healthy body, any glucose not used as fuel in the muscles or brain or stored as glycogen in the liver is converted to triglyceride and stored as fat. Let's assume that an average trainee consumes 3000 calories a day. On a typical bodybuilder's diet, 60% of those calories, 1800 calories, will be carbohydrate. (The other 40% will be 30% protein and 10% fat.) All 1800 carbohydrate-calories will be converted to simple sugars mostly glucose but also ribose and fructose, etc. If your muscles can currently store 1500 of those calories, they are converted to ATP and stored. The balance, 300 calories, will be converted to triglyceride and stored as fat. At that rate, in slightly less than 12 days you would add a pound of fat. Fortunately, there are other mitigating factors because such behavior would add about thirty pounds of fat a year. According to Dr. Hans Tritschler, a researcher from Munich, Germany, Lipoic Acid can increase the conversion and storage of glucose as ATP by approximately 40%. It does this through a variety of mechanisms, including the stimulation of GLUT-1 and GLUT-4 glucose transporters. Thus, the addition of Lipoic Acid to your diet could raise your capacity for conversion and storage to 2100 calories (1500 x 40% = 600 calories 1500 + 600 = 2100 calories). This creates a potential 300 calorie shortfall. Now, if you could find a way to increase your caloric demand (exercise will work nicely) you would be primed to burn a pound of fat every 12 days instead of adding a pound. Coincidentally, by increasing the energy production capacity of your muscles you should have the reserves to increase your effort by 300 calories. The only missing requirement is that you keep your heart rate in the zone where fat is burned preferentially for energy. This occurs when your heart rate is 70% of maximum +/- 5%. Further, by increasing your ATP stores you may increase your ability to store creatine phosphate and water in the muscles. As creatine users know, creatine makes your muscles larger, fuller and stronger as well. Bill Phillips and Anthony Almada take note, the research has not yet been done but Lipoic Acid may potentiate creatine monohydrate. It may increase the ability of the muscles to store creatine phosphate and it may improve the solubility of creatine monohydrate to nearly the level of creatine citrate (about ten fold).

As mentioned earlier, diabetics are helped by this increase in glucose uptake because reducing blood glucose levels reduces the quantity and duration of glucose' presence in the system. The greater the reduction, the less the opportunity for glycation damage. European medical doctors use Lipoic Acid to reduce the need for exogenous Insulin or Glucotrol (an Insulin sensitivity enhancing drug). It has the additional benefit of reversing the nerve damage that creates neuropathy in diabetics. We'll examine this boon further later. It would be irresponsible not to warn that diabetics should not employ this treatment without the assistance of a knowledgeable M.D. There is a significant risk of producing dangerous reactive hypoglycemia.


The Anti-Oxidant Effect

Most bodybuilders have come to accept that for all the benefits of exercise it is a form of stress. As such, it markedly increases the volume of oxidative reactions in the system. Informed bodybuilders address their concerns about this problem with supplementary Vitamin A, C and E. More conscientious athletes may add carotenoids, glutathione, selenium and other micro-nutrients. In a world full of radiation, pollution and increasing levels of ultra-violet rays, this multi-pronged protection is important to health, function and longevity. Still, if Lipoic Acid were just one more addition to the list of antioxidants, it might not merit much attention. It is far from just another free- radical scavenger. Looking like a fat on one end of its chain-like structure and carboxylic acid on the other gives it dual compatibility. Its low molecular weight (206) makes it slightly less soluble in water than Vitamin C but significantly more soluble in fat than Vitamin E. The small size of the molecule permits it to enter areas as small as the nuclei of cells. In short, Lipoic Acid can enter almost anywhere in the body with its antioxidant protection.

Most antioxidants are consumed in the process of deactivating oxidative agents. It is far better that antioxidants are consumed than that cells are damaged but it demands that they be continually replenished to be effective. The process is different with Lipoic Acid. Remember the two sulphur atoms we learned about earlier? Well, in normal state those two sulphur atoms are bound to each other. When Lipoic Acid encounters a free-radical, such as hydroxyl, or a reactive oxygen species, such as hypochlorous acid, the sulphur bond opens and each sulphur atom binds an electron. This pulls two destroyers out of the system. It also converts Lipoic Acid to Dihydrolipoic Acid. Not all free-radicals have electrons to give. Some are in need of electrons. When Dihydrolipoic Acid encounters such radicals, it happily relinquishes its two electrons, recreates the sulphur-sulphur bond and returns to being Lipoic Acid, ready to take electrons from another overloaded free-radical. Another instance when this occurs is when Ascorbic Acid has taken electrons from a free-radical to become Dihydroascorbate. When Dihydroascorbate encounters Lipoic Acid it converts back to usable Ascorbic Acid via the above described exchange method. Since Ascorbic Acid can't do this with other free-radicals, the lack of an available Lipoic Acid molecule will cause the Dihydroascorbate to be disposed of by the kidneys in urine. An opposite reaction takes place with Tocopherol (Vitamin E) and a related reaction occurs with Glutathione. This two-way behavior defines Lipoic Acid as a "Redox" agent. In effect, it recycles other antioxidants. Such substances are rare in this area of function. The net result is that beyond its own antioxidant activity it multiplies the effectiveness of other antioxidants.


Chelating Agent

When I mentioned pollution earlier, I was not specific about the Lead in air from automobile exhaust. I didn't point out the Cadmium from cigarette smoke or the mercury from dental fillings and fish from polluted waters. Each of these toxins are classed as a "heavy metal". (I don't think they have anything to do with Metallica or Black Sabbath.) I'm sure you've noticed the black, purple, green and yellow colors that accumulate around bruised tissue. In large measure, these colors are the result of metals in blood escaping through broken capillaries and depositing in the tissue. These metals get trapped in the tissue when the body bathes the tissue with enzymes designed to heal the contusion. These enzymes are acids intended to dissolve scar tissue and breakdown damaged and dead cells. The higher acidity these substrates produce encourage accelerated formation of metal ions which are charged metal atoms. This is similar to the process that occurs when acids corrode metals. Here, the destruction of tissue has healing intent. The process, however, goes on at a reduced rate throughout the body all the time. While ions are not quite the same as free-radicals, they induce their own form of tissue destruction. Ions, however, leech entire molecules from tissue. When the metals involved are toxic, heavy metals, they can produce dangerous compounds in the system. These poisons can seriously damage the brain, liver and other organs, sometimes irreparably. Many are aware of the brain damage lead paint causes in young children. Aluminum has been implicated in Alzheimer's. An entire subset of the dental profession has arisen to address the issue of mercury vapor toxicity and the host of reported disorders it provokes. Each of the heavy metals has been linked to one of more serious, sometimes fatal, health risks.

The treatment for acute heavy metal poisoning is a powerful chelating agent called EDTA. Devotees of the O.J. Simpson trial will remember testimony about this chemical. Normally the levels of heavy metals in the system are low enough not to need emergency intervention. That does not mean they don't take their toll on the body. Besides the type of tissue destruction we discussed in the section on antioxidants and the potential for encouraging cancer, these toxic results of heavy metal compounds compromise various body systems. Unless we are vigilant in clearing them from the body their poisoning effect is cumulative. Chelating agents like Lipoic Acid, Superoxide Dismutase (SOD), reduced Glutathione and Selenium can prevent the build up. They can protect us from this slow death. They also free the system to address the elevated recuperative demands of heavy training. The only heavy metal you should need to concern yourself with is heavy iron.


Gene Protection

Researchers from time to time announce to the press that they have located the gene that either causes or increases susceptibility for some particular disease. They rarely explain that such genes often rest dormant for a lifetime, unless and until some free-radical, oxidative reagent, heavy metal ion or nuclear factor attacks it. Consider that the gene may never be activated if a protective substrate can keep the attacker from the gene. Let's back up a minute. A gene is really a segment of a DNA molecule that functions as a unit to control a specific type of cell by regulating the production of a specific protein. According to the research team at the Human Genome Project, there are on the order of 100,000 genes on each of the 46 chromosomes in the nucleus of each cell. Genes are capable of duplicating themselves exactly with every cell division. They divide numerous times within our life span. They are also capable of manipulating various protein formations through a process called gene expression. Anything that interacts with normal gene regulation can have profound influence on gene expression. Oxidatives can influence gene expression. So to can they be activated by a protein complex called Nuclear Factor kappa-B (NF-kappa-B). This activator can bind to DNA and change the rate of gene activation and division. Older people's genes reveal more bound NF-kappa-B. Studies have revealed that this can lead to weakening of the immune system, aging of the skin and functional impairment in all other body systems. NF-kappa-B is checked by a protein fragment identified as I-kappa-B. When these two are bound in complex, they cannot pass through our cytoplasm into the nucleus. The genes within the nuclei are thus safe. Some oxidatives, notably peroxides and UV, can break the complex and lay the genes bare to assault. Lipoic Acid, owing to its small molecular size can reside in the cytosol and act as a back-line defense. While Lipoic Acid is not the only redox agent that can do so (glutathione/reduced glutathione can also) clearly both NF-kappa-B and tumor necrosis factor (another nasty) are blocked by Lipoic Acid. In this way Lipoic Acid can keep your systems and organs, including our biggest organ, skin, healthy longer. It won't do to have created a kick ass body only to have it covered by wrinkled, sagging skin and organs that are primed to fail early. It may not be as immediately apparent but this benefit may be felt for longer because it is so close to the source of genetic diseases.


Heart Disease

I'm about sick of hearing from the American Medical Association, the American Heart Association and every food company with a product to hawk. They may be well-meaning but they are wrong about cholesterol. There is more nonsense out there on this subject than almost any other area of health. Cholesterol is not an inherently bad thing. Neither serum cholesterol nor dietary cholesterol, neither HDL nor LDL are harmful. What is potentially harmful is an oxidized form of LDL referred to as Ox-LDL. It is, more specifically, the immune system's reaction to this oxidization damaged lipoprotein that forms the build up on arterial walls. This build up is the beginning of the problem with cholesterol. Even if you had a diet completely devoid of cholesterol, you could still develop atherosclerosis and heart disease. Your liver manufactures more than enough cholesterol, both HDL and LDL to cause trouble if free-radical activity is high in the body. Cholesterol is made as a way to carry fatty substrates through the bloodstream. Blood is mostly water and fatty substances aren't readily carried in it. Cholesterol provides a more compatible shell for these fats to travel in. LDLs carry fats to their target sites. HDLs return unused or waste fatty compounds for removal. This is admittedly a simplified view. It makes clear, however, that if a means were available to protect LDL from becoming Ox-LDL, the potential for atherosclerosis and its related form of heart disease could be stopped at its root. Lipoic Acid comes to the rescue. As we've already pointed out, Lipoic Acid is a rare antioxidant that is soluble both in fat and water. If it were available to be bound into every LDL cholesterol molecule, it would do the job nicely. In separate research Drs. Dojama, Anisimov, Koziov and Ivanov have each validated this hypothesis. As early as 1960, Dr. Dojama had found Lipoic Acid to be an antiatherogenic that also activated oxioreductive enzymes involved in fat breakdown. In 1974 Dr. Ivanov reported that Lipoic Acid reduced cholesterol in aortic tissue by 45 percent, raising oxygen uptake in the heart by 72 percent, 148 percent in the aorta and 128 percent in the liver. This may seem a remote concern to us as bodybuilders but it strikes closer to home for Steroid users. One major concern for long-term steroid users is the causal link to atherosclerotic heart disease. The exact mechanism that causes this link is in dispute. Whatever the mechanism, supplementary Lipoic Acid is a very smart addition to a steroid stack.


Nerve Regeneration

Nerves regenerate more slowly than any other type of tissue. New growth also takes a long time and considerable system resources. Moreover, functional impairment, when it can be repaired, is usually a long gradual process. As bodybuilders we place exceptional demand on our bodies' abilities to grow nerve tissue to carry messages within our muscles. Every square inch of new muscle requires more than four yards of nerve growth. Inadequate nerve growth can slow new muscle growth to a crawl. Fair argument can be made that nerve and capillary insufficiency are the two principle factors limiting growth in "overtrained" athletes. They are also the most severely demanding factors in the recuperative process. If animal studies were extrapolated to humans, skeletal muscle mass could be doubled in twelve weeks but building the neural and capillary network to support the new tissue would take nearly four years (196 months). Since the body won't add new tissue any faster than it can build the support network to maintain it, the bottleneck is clear.

In the section on blood sugar regulation I mentioned the neuropathy associated with diabetes. High blood sugar levels destroy nerves. As I also mentioned earlier, European M.D.s have been using Lipoic Acid to help control diabetes. Some of those doctors noticed that the symptoms of neuropathy showed signs of abatement in their patients. It was initially theorized that this might be the result of Lipoic Acid reducing the progressive nerve destruction, allowing the body to catch up somewhat with cell replacement. Research by Reschke, Zeugen and Rosak, et al. proved the news was even better. In both diabetics and normal individuals, Lipoic Acid improves membrane fluidity (probably due to its ready solubility). Dr. Ziegler at Heinrich-Heine University showed that long-term treatment induced "sprouting", the growth of new fibers, in as little as three weeks. This is a significant acceleration of the normal process. It can not be said with certainty that this effect occurs in bodybuilders but the protective effect alone should be sufficient incentive for the use of this wonder nutrient.


Cataracts, Parkinson's and Alzheimer's

I've grouped these three disorders together because none of them seem to have any relevance to physically fit bodybuilders. Their common feature is that physical fitness does not protect one from any of them. Each is a degenerative disease. Each can destroy the quality of ones life. Cataracts are degeneration of the lenses of the eyes. The two principal causes being glycation and the UV energy in sunlight. Both glucose and sunlight create free-radicals in any tissue on which they impinge. The lenses of the eyes don't receive much protection from anti-oxidants in blood. Without the help of anti-oxidants the lenses are at the mercy of oxidative and glucatatant damage. For too many this means a progressive deterioration of vision, sometimes leading to blindness.

Parkinson's may have its cause in the adrenal glands but its damage occurs through degeneration of the Central Nervous System (CNS). Neurodegenerative disease is more common in the CNS due to its higher oxygen consumption and consequently higher oxygen radical and oxygen singlet production. The mitochondrial damage thus created produces additional radicals, etc.

Alzheimer's is believed to be caused by high concentrations of Aluminum (a heavy metal) depositing in the neural synapses of the brain. In theory, if these deposits could be prevented so could the disease.

Lipoic Acid has been shown to help with all three diseases. In 1994, Dr. Lester Packer and his group showed that Lipoic Acid increased the levels of glutathione, vitamin C and vitamin E in the eye lens tissue of animals. Cell culture studies reveal that Lipoic Acid blocks cataract formation in lenses from diabetic rats. Epidemiological studies confirm that people with higher dietary intake of anti-oxidants have lower incidence of cataracts. This doesn't quite prove that Lipoic Acid prevents cataracts in humans but it is strong argument for the thesis. Since cataracts form over many years, the confirmatory research will take time. Considering the low toxicity and multiple benefits it bestows, everyone except diabetics and pregnant women can safely take supplements and should. Diabetics should find a doctor with experience using Lipoic Acid in the treatment of their disease. There is no research on the teratogenic (birth defect) effects of supplementation. Wisdom dictates not adding any supplement to the diet of pregnant women for which adequate research does not exist.

I am among those who lament the toll Parkinson's has taken on Muhammad Ali. What we have witnessed in his deterioration demonstrates that fitness is not protection against this scourge. I know of no research that indicates that Thioctic Acid can block the impairment of adrenal function that leads to Parkinson's symptoms. Both Tritschler et al. and Grenamyre et al. have shown Lipoic Acid to be neuroprotective. Combined with other treatment, Lipoic Acid could therefore significantly slow the progressive degenerative effects of the disease.

It is too early to become excited about the use of Lipoic Acid in the prevention and treatment of Alzheimer's. There is, however, some important evidence to recommend it. In animal studies, 100 milligrams of Lipoic Acid per kilogram of body weight improved memory to a point better than that of young animals not given supplements. This 1993 research by Stoll et al. has not been duplicated but as we've seen Lipoic Acid's chelating action and nerve generation effect we can reasonably propose a pathway for this effect. Keeping in mind, prinum non nocere: first, do no harm, we can enthusiastically recommend the use of supplemental Lipoic Acid. We will discuss the quantity and safety considerations at the end of the article.


HIV/AIDS

I hope this section will be irrelevant to everyone who reads it. AIDS is a tragic disease. Realistically, every one of us knows someone who has been struck by this modern-day plague. During HIV infection, key cells of the immune system called CD lymphocytes lose their ability to make and transport glutathione. Glutathione is a major cellular anti-oxidant. Without glutathione these immune cells succumb to oxidative stress and fail. As the immune system becomes increasingly compromised, the HIV-positive individual develops opportunistic infections that are normally defeated by a healthy immune system. Ultimately, they enter a stage considered clinical AIDS.

There is no evidence that Lipoic Acid is anti-viral. Nevertheless, for those infected with the virus, the decline may be prevented if the immune cells can be kept sufficiently high in anti-oxidants. We know that Lipoic Acid is a powerful anti-oxidant and a facilitator of glutathione production. Researchers conducted a small clinical trial that produced such encouraging results that larger studies are being planned.

Dr. Fuchs and colleagues gave 150 milligrams of Lipoic Acid three times a day for two weeks. They found that plasma glutathione levels rose in all patients. Further the number of T-helper cells increased in two thirds of the patients and the ratio of T-helper/T-suppressor cells improved in 60% of the patients. Finally, a cell culture study found that Lipoic Acid prevented the replication of the HIV virus. The HIV virus replicates when NF-kappa-B is activated. We have already examined the ability of Lipoic Acid to block NF-kappa-B activation of gene replication.

When this research is coupled with the experience of Dr. Richard Cathcart at San Francisco General Hospital and vitamin C it becomes clear that non-drug nutritional supplements can be of significant benefit to those who have become infected. Until there is a cure, our best hope is to slow the proliferation of the virus and boost the health of the immune system. Lipoic Acid may be an important agent in that effort.


Dosage and Safety

The many miracles of Lipoic Acid would be of little value unless its use were safe. Often with drugs it is a balance of risk against reward. As stated earlier, Lipoic Acid is made in the body. It is also present in our diet. These facts alone argue for the general safety of its use but not the levels that are safe. Since Lipoic Acid is used in the mitochondria, foods rich in mitochondria are sources of Lipoic Acid. The most prevalent of these is red meat. Increasingly people are choosing to eliminate or at least reduce their consumption of red meat. For such individuals, yeast is an alternative source. The easiest way to increase your Lipoic Acid levels is through the use of supplements. Some of these are derived from non-animal sources.

Clinical and toxicological studies have revealed no serious adverse effect from Lipoic Acid supplementation. Since it has been used for more than thirty years at dosages of 300 to 600 milligrams per day to treat diabetic neuropathy, the number of individuals using it represents a significant sampling.

As mentioned earlier, there is insufficient data to permit recommending supplementation to pregnant women. There is, however, no evidence of teratogenic effect. There is also no evidence of carcinogenic effect at any dosage. Alcoholics or even heavy drinkers probably shouldn't use supplementary Lipoic Acid without also supplementing vitamin B-1. A few individuals will have bad reactions to anything. These would include allergic response or skin eruptions. Like any acidic compound, an upset stomach is possible, particularly if it is taken on an empty stomach. Ulcer patients should be particularly careful.

The acute toxic dose is extremely high, 400-500 milligrams per kilogram of bodyweight. This is the equivalent of 30 grams or more for a 165-pound person. A typical, conservative daily supplement range for a healthy adult would be 30-50 milligrams. This is the typical label recommendation on the bottled supplement. I have personally used 150 milligrams per day (50 mg. per meal) for an extended period of time at a bodyweight of 220 pounds. I have noticed only positive effects from this dosage.

I've found Lipoic Acid to be an exciting, unique metabolite that boosts and recharges energy levels, raises the body's defenses against a host of maladies and is protective against a collection of age related deteriorations. Smart bodybuilders will start taking this miracle metabolic enhancer and gaining strength and muscle from its enhancement of their recuperative abilities.

Copyright © 1996 Physique Tools and Wesley James


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