Lipoic Acid

Lipoic acid offers powerful protection against three common ailments of aging: stroke, heart disease, and cataracts.

Lipoic acid strengthens memory and prevents brain aging.

Lipoic acid boosts the entire antioxidant defense network. By taking lipoic acid, you are in effect increasing your levels of vitamins E and C, glutathione, and Coenzyme Q10.

Lipoic acid is new to the United States. It has been used safely and effectively in Europe for more than two decades to prevent and relieve the complications of diabetes.

Lipoic acid is reported to reverse mushroom poisoning of the liver, which is usually lethal.

It has been used successfully to treat other liver diseases such as hepatitis C.

RDA: None.

The Packer Plan: 100 milligrams daily (50 milligrams in the A.M. and 50 milligrams in the P.M.).

Sources: Synthesized by the body. Present in small amounts in potatoes, spinach, and red meat.

Lipoic Acid Protects the Heart.

The damage that occurs to the brain after a stroke is similar to the damage that is inflicted on the heart muscle after a heart attack. Similar to a stroke, which is typically caused by a blockage in an artery delivering blood to the brain, a heart attack is usually the result of a blockage in an artery delivering blood to the heart. The result is a period of ischemia or oxygen deprivation followed by an explosion of free radicals when the oxygen is restored. In both cases, it is the proliferation of free radicals that exacerbates the injury.

Since lipoic acid offered significant protection against stroke, we felt that it might do the same for heart attack and devised an experiment to test our hypotheses. Based on previous experiments, we knew that if a heart is denied oxygen under these circumstances, only 20 to 25 percent of the hearts will recover and continue beating normally. The rest will suffer serious damage. When we added lipoic acid to the reperfusion solution, however, the odds were overwhelmingly tipped in favor of recovery. In fact, the recovery rate increased to almost 60 percent, more than double the rate of recovery without lipoic acid.

This is in keeping with our earlier experiment showing that lipoic acid can help protect heart tissue from free radical damage inflicted during a simulated heart attack.

The experiments performed in the Packer Lab clearly demonstrate how the antioxidant network in general, and lipoic acid in particular, can offer significant protection against the common ailments associated with aging, notably heart disease, stroke, and cataracts.

They provide the solid scientific basis for the belief that maintaining your antioxidant advantage can help preserve health and vitality well into your later decades.

Lipoic Acid and Stroke

Our next experiment produced even more amazing results that further reinforced my belief in the incredible power of lipoic acid, and its potential as a treatment for many different diseases, including stroke, the third leading cause of death in the United States.

Stroke is caused by a disruption in the delivery of blood and oxygen to the brain. If you're not worried about stroke, you should be. As many as 700,000 people in the United States suffer strokes each year, and 150,000 will die of them. Those who do survive a stroke often suffer physical or mental disabilities. Our studies show that lipoic acid may prove to be a weapon in the treatment of stroke, and in fact, it may help prevent strokes.

In our experiment, we induced a stroke in laboratory rats by blocking the carotid artery, which delivers blood and oxygen to the brain. After thirty minutes, blood flow was restored, and we monitored the animals for twenty-four hours. Once the oxygen was restored, there was a burst in the production of free radicals, which overwhelmed the brain's antioxidant defenses. This proved to be deadly. Within twenty-four hours after restoring oxygen, 80 percent of the rats had died.

We then repeated the experiment, with one important exception. This time, we injected the rats with lipoic acid right before we restored the normal flow of blood to the brain. Amazingly, after twenty-four hours, only 25 percent of the animals had died, and the survivors showed no sign of any problem. In fact, they had recovered completely. We know of no other antioxidant or drug that could have performed this feat.

Obviously, the lipoic acid injections had protected the animals against the ravages of stroke, but the question that remained was how. One of the problems in developing a treatment for stroke is that it is very difficult to design a drug that is allowed entry into the brain—that is, that can cross the so-called brain/blood barrier. We needed to know whether lipoic acid was one of the few substances that could actually cross the brain/blood barrier and work its magic right in the brain cells, where it was needed the most—whether it did so directly or through another member of the network.

Here is yet another example of how the antioxidant network can work for our benefit, and it could literally make the difference between life and death.

Lipoic Acid and Cataracts

Our next experiment is particularly relevant to humans because it concerns one of the most common ailments associated with aging— cataracts. A cataract is a cloudy or opaque covering that grows over the lens of the eye and is caused by free radical damage to proteins. Cataracts are so common among older people that the odds are if you live long enough, you will develop them. Cataracts are a result of years of exposure to sunlight, which can promote too many free radicals, thereby depleting the body of antioxidants.

In our next experiment, we gave one group of newborn rats a drug called butathione sulphoxamine (BSO) that inhibited the production of glutathione. We gave another group of newborn rats BSO, but this time, we also gave them an injection of lipoic acid.

Newborn rats do not open their eyes until the sixth week of life, but we knew from past experiments that when these glutathione-deprived rats did open their eyes, they would all have cataracts. But the question that remained was: Would lipoic acid protect against cataracts caused by glutathione deficiency?

At the end of six weeks, as predicted, the rats that had been given the glutathione-blocking drug but had not been given lipoic acid all developed cataracts. But almost all of the rats that had been given lipoic acid supplementation had remained cataract free! Further testing revealed that glutathione levels were much higher in the eye lens of the rats treated with lipoic acid, but severely depleted in the rats not treated with lipoic acid.

It was very exciting to have finally found the antioxidant that could stimulate glutathione production. But that's not all we found. Lipoic acid had the same effect on vitamins C and E. In other words, lipoic acid supplements had not only restored glutathione, they had also boosted the levels of these other important network antioxidants. From these experiments, it became obvious that lipoic acid was an antioxidant like no other.

A Cure for “Incurable” Mushroom Poisoning.

One innovative physician who has used lipoic acid in his practice for more than twenty years is Burton Berkson, M.D., Ph.D., of Las Cruces, New Mexico. Dr. Berkson can cite numerous examples of how lipoic acid has literally saved the lives of patients for whom other treatments are ineffective.Dr. Berkson's first use of lipoic acid dates to 1977 when as a medical resident at Case Western Reserve- affiliated hospitals, he was assigned to treat a husband and wife who were suffering from liver disease caused by the highly poisonous Amanita mushroom. Often fatal, Amanita poising destroys the liver in several key ways, including drastically reducing the levels of glutathione, the primary antioxidant in the liver. Critically ill, the couple was expected to die within a few days.

Fortunately, Dr. Berkson knew quite a bit more about mushroom poising than the average physician. Before going to medical school, Dr. Berkson had earned a Ph.D. in microbiology, specializing in mycology, the study of fungi. As a mycology professor at Rutgers University, he had an article in a medical journal by a Czech doctor who described his experiences using lipoic acid as a treatment for Amanita poisoning. "What was remarkable about the study is that out of forty patients with mushroom poisoning, thirty-nine had survived, a considerable improvement over the 60 to 90 percent mortality rate normally associated with mushroom poisoning. To everyone's surprise, within an hour, they reported feeling markedly better. To everyone's astonishment, within three days they were getting out of bed, and within two weeks, they were back to normal. Drs. Berkson and Barter published articles on their experiences with lipoic acid in scientific journals, but few in the medical community paid any attention to them. According to Dr. Berkson, at the time the medical establishment was enamored with organ transplantation, a new and exciting field, and naively believed that the best approach to liver disease was simply to transplant a new liver. For the past twenty years, Dr. Berkson has used lipoic acid to treat people with other forms of liver disease, such as hepatitis C, a severe infection of the liver. In fact, he notes that he has recently treated a thirty-five-year-old woman with severe hepatitis C who had been warned that she would probably die within a matter of weeks without a liver transplant. Shortly after taking lipoic acid supplements daily, she was well enough to resume her busy schedule as a working mother. Dr. Berkson's files are filled with amazing stories about "miracle cures" attributed to lipoic acid, which he describes in his new book, Alpha Lipoic Acid: The Breakthrough Antioxidant.

Lipoic Acid Suppresses Bad Genes.

I am not exaggerating when I say that one of the biggest medical stories of the century is the discovery thatantioxidants play a far greater role in health maintenance than we had ever believed possible.

In addition to quenching free radicals, antioxidants such as lipoic acid may prevent the onset of disease by blocking the activation of so-called bad genes. This knowledge greatly expands our ability not only to treat many different diseases, but simply to eradicate them.

There are many misconceptions about the way that genes work. For example, although most genes are normal, all of us carry a few defective or potentially harmful ones. Yon may believe that if you are born with a gene to develop colon cancer, heart disease, or arthritis, it automatically means that you will get that disease. That is simply not the case. Environment—lifestyle, diet, and other factors—may also play a role in determining whether we will develop a particular disease even if we are genetically programmed to do so.

Genes have to be "turned on," or activated, before they can be expressed. The body has many different signaling systems that regulate the expression of genes so that they are turned on and off at appropriate times. For example, the genes that regulate growth are more active during childhood than they are when we are fully grown adults, and that is why we stop growing at a certain point. However, if DNA is targeted by a free radical, it can activate bad genes that would have otherwise lain dormant. That is why people who are exposed to high levels of free radicals—for example, smokers—are more likely to develop particular diseases than those who are not. The free radicals in cigarette smoke may activate particular genes, which may trigger the onset of various forms of cancer and heart disease. If the person had never smoked, those genes may never have surfaced.

Because antioxidants can help regulate dangerous genes, there are extraordinary possibilities to treat disease on the most basic level. If we can identify and suppress bad genes before they can do harm, we will be practicing the ultimate form of preventive medicine.

We don't have to wait to take advantage of this new information. By following the Packer Plan, we will be practicing this powerful form of preventive medicine right now.

Lipoic Acid, AIDS, and Immune Function.

Disease and oxidative stress are closely linked: even a disease that appears to be totally unrelated to the body's tug-of-war between free radicals and antioxidants can be profoundly affected by a shift in the antioxidant balance. Such is the case with AIDS (acquired immune deficiency syndrome), which is actually a group of diseases that result from the suppression of the immune system by the human immunodeficiency virus (HIV). A retrovirus is a virus that can alter the genetic makeup of a cell. What makes HIV so difficult to control is that this virus targets and destroys immune cells called T-helper cells, the body's first line of defense against infection. Once the T-cells are decimated, the body is left vulnerable to a host of opportunistic infections that prey on weakened immune systems. For example, people with AIDS are especially vulnerable to pneumonia and cytomegalovirus (which can cause blindness), two infections that a healthy immune system can often defeat.

Although AIDS appears to be caused solely by an infectious agent, the reality is that oxidative stress is a major factor in the progression of the virus. When the T-cells are weakened by HIV, they lose their ability to produce and transport glutathione, a major cellular antioxidant. Oncethe T-cells lose their antioxidant edge, they succumb to oxidative stress, which can cause even further destruction. Not surprisingly, the glutathione levels as well as levels of other antioxidants are significantly lower in HIV-positive patients. Although restoring antioxidants is not a cure for AIDS, researchers believe that it, along with other medications, will at least help give the body a lighting chance against the virus.

In the test tube, lipoic acid prevents the replication of HIV in cultured human cells. Although this doesn't necessarily mean that it will work in HIV-positive people, I think it might. There is also some evidence that lipoic acid bolsters the antioxidant defenses in HIV-positive people, which presumably will help them fight infections better. In one study, lipoic acid (150 milligrams three times daily) was given orally to twelve HIV-positive patients. At the end of the two weeks, all of the patients had an increase in blood glutathione levels, and nine of the patients had an increase in the number of T-helper cells—a sign that their immune systems were stronger. More studies are needed to determine if lipoic acid should be included in the treatment of HIV infection, but it seems obvious that restoring the antioxidant balance can help. If you are HIV-positive, I recommend that you find a knowledgeable physician who can help determine if lipoic acid supplements should be added to your treatment regimen.

Lipoic Acid is a Memory Enhancer

As we age, there is a subtle but very real decline in mental function that begins during midlife. The most common symptom is the deterioration of short-term memory, known as age-associated memory impairment (AAMI). A name forgotten, a missed appointment, even the loss of mental stamina are all signs of AAMI. I want to stress that these temporary lapses are not signs of senility or Alzheimer's disease; they are a normal part of the aging process. The good news is, antioxidants may play a role in helping to preserve mental function.

As the regulator of all body functions, the brain is one of our hardest Working organs. In fact, it is a virtual hotbed of activity, and it requires a tremendous amount of energy to carry on its work. This 1-pound organ coordinates all of the body's nervous activity, processes incoming sensory impulses, and is the repository of reasoning, intellect, memory, consciousness, and emotions. As a result, the brain consumes a vast mount of energy. To accommodate its insatiable need for energy, brain tissue is rich in mitochondria, the cellular powerhouses that reduce ATP, the fuel that runs the body. Since the burning of oxygen is required to make energy, the brain is also a major producer of free radicals and is particularly vulnerable to oxidative stress.

Over time, the constant assault of free radicals can exact a steep toll on mental function.

Since free radical damage has been implicated in age-related changes in memory, researchers have, investigated whether supplemental antioxidants can help slow down this damage—and perhaps even reverse it.

A recent study performed at the Clinical Institute for Mental Health in Mannheim, Germany, examined the effect of lipoic acid on memory loss in aging mice, which experience similar age-related memory problems as humans. Older but otherwise healthy mice were given lipoic acid in their drinking water. After fourteen days of treatment, the mice had to negotiate their way through a maze. Mice treated with lipoic acid performed significantly better than untreated mice. Many did as well and some even better than mice half their age. Interestingly, lipoic acid did not improve performance in younger animals that presumably still have strong antioxidant defenses.

More studies are required lo determine whether lipoic acid will enhance mental function in humans, but there is strong evidence that many antioxidants (specifically vitamin E, ginkgo biloba, and the pine bark extract supplement Pycnogenol) certainly can play a role in keeping us smart and sharp at any age.

Lipoic acid and radiation poisoning

Exposure to radiation produces a cascade of free radicals that causes severe damage and can be fatal. Radiation decimates the body's supply of glutathione, which allows free radicals to severely damage the body's tissues and organs. Several antioxidant compounds have been used to treat radiation damage, with varying degrees of effectiveness. In fact, virtually every army in the world equips its soldiers with antiradiation drugs that are similar in molecular structure to two antioxidants— glutathione and lipoic acid. Recently, researchers al the Russian Institute of Pediatric Hematology and the Vitamin Research Institute in Moscow have found that lipoic acid may prove to be one of most effective antiradiation treatments to date.

Radiation is so deadly that when animals are exposed lo high levels of radiation, only 35 percent of them will survive. Lipoic acid is so powerful that if the animals are treated with lipoic acid before exposure, the survival rate increases to 90 percent. Although we don't know precisely why more mice survive, I suspect it is because of lipoic acid's ability to boost the immune system, enhancing the body's ability to fight against diseases generated by free radicals.

Fortunately, most of us have never been exposed to lethal levels of radiation, but accidents do happen. The near meltdown of a nuclear power plant in Chernobyl, Ukraine, in 1986 led to radioactive fallout and massive soil contamination in the surrounding area. People who continued to live in Chernobyl were exposed to constant low levels of radiation. As a result, the incidence of cancer is much higher than normal, particularly among children.

Researchers examined the effects of lipoic acid treatment on the level of oxidative damage in children living in areas affected by the Chernobyl accident. The higher the level of blood peroxidation, the greater the sign of damage caused by free radicals. After twenty-eight days of lipoic acid supplements, researchers had some extraordinarily good news to report. They found that in children treated with lipoic acid, blood peroxidation levels had fallen to those seen in normal children. Even better, the children's liver and kidney functions were normalized. Even against the powerful free radicals generated by radiation exposure, lipoic acid was able to hold its own.

Lipoic Acid: The Smoker’s Rescue Formula.

I am delighted to report that along with three colleagues—Gladys Block, Ph.D.; Maret Traber, Ph.D.; and Carol Cross, M.D.—I have recently undertaken a unique clinical study that could ultimately benefit the tens of millions of Americans who smoke. Before I begin, let me make my position on smoking perfectly clear. If you smoke, quitting smoking is the single most important thing you can do to safeguard your health and ultimately save your life. Smoking is a leading cause of death in the Western world, and on average, it will rob you of about eight years of life.

I think most smokers know these dismal facts, and that is why out of the 40 million smokers in the United States, at any given time 30 million would like to quit. Unfortunately, smoking is a highly addictive habit, and quitting is very difficult, so difficult in fact that 90 percent of those who give up smoking start smoking again within five years. Until people do stop smoking, they can try to protect their health the best way they can.

Here are the facts: Smokers have elevated risks of developing heart disease, diabetes, stroke, and some forms of cancer, and to a lesser extent, so do people who are exposed to secondhand smoke. There is no doubt that oxidative stress contributes to the onset and progression of these diseases. Each puff of cigarette smoke contains thousands of different free radicals that can overwhelm the body's antioxidant defenses. Smokers have lower plasma levels of vitamins E and C and glutathione. I think that it is obvious that the constant drain on the body's antioxidant system puts smokers at great risk of disease.

In our study, we will be recruiting 500 subjects from the Kaiser Foundation in Oakland, California. This group will include smokers, nonsmokers, and passive smokers—people who live or work with smokers but do not smoke themselves. From this study, we hope to learn whether the antioxidant cocktail will reduce oxidative stress injury in both smokers and passive smokers. This would be the first step in determining whether the antioxidant network can actually protect smokers against the free radical damage inflicted by cigarette smoke.

It could be years before we publish our results, and many smokers may want to know if they should begin the antioxidant cocktail right now. My answer is a strong yes. I feel that boosting the antioxidant network will prove to have a positive effect on the health of smokers and, next to quitting, is an important way you can protect your body from some of the damage inflicted by cigarette smoke.

Above is an excerpt from the book “The Antioxidant Miracle” by Lester Packer, PH.D. Director of the Packer Lab, University of California at Berkley and Carol Colman – New York Times best-selling co-author of “The Melatonin Miracles and Stop Depression Now”.

Dr Packer is one of the world’s foremost authorities on Antioxidants and probably the most recognized scientist amongst his peers for the research on how they relate to Anti-Aging.