Lipoic Acid is the Number One Super Antioxidant

One of the most formidable protectors of your brain is an antioxidant you may never have heard of. Dr. Lester Packer, professor of molecular and cell biology at the University of California at Berkeley, and one of the world’s leading researchers on antioxidants, calls alpha-lipoic acid the “superantioxidant,” closest to his vision of an “ideal” antioxidant if he were to design one. Indeed, in Dr. Packer’s hierarchy of five so-called “network antioxidants”—desig­nated as the mightiest among hundreds of antioxidants—he puts lipoic acid number one. Lipoic acid is “the most versatile and powerful” of all antioxidants, he declares. It is an incomparable brain antioxidant—the antioxidant’s antioxidant.

Several things make it unique and universal, finds Dr. Packer. Because it is a small molecule it is one of the few substances that can readily penetrate the blood-brain bar­rier and be quickly taken up by brain tissue; thus, it goes directly to the aid and rescue of target cells under attack in the brain. “It is the only antioxidant that can easily get into the brain,” he says.

Moreover, unlike any other antioxidant, it is both fat and water soluble because of its unique chemical structure, and thus able to work its miracles in both the watery and fatty portions of the cell, wherever it is most needed. No other antioxidant can do that. And there’s more. Lipoic acid is the only antioxidant that can recycle or regenerate itself as well as all four other crucial antioxidants—vitamins E anc C, glutathione, and coenzyme 010. This means that when an antioxidant like vitamin E or C is exhausted anc depleted, lipoic acid rushes in to restore it to its full antiox idant powers. It is also the only antioxidant that can rein vent itself as an antioxidant after it has expended itsel fighting off free radical assaults.

Further, lipoic acid neutralizes the very type of free rad ical most apt to injure brain cells—nitrogen radicals including nitric oxide. Most attention has been focused or defusing so-called ordinary oxygen radicals, but there is another type free radical that scientists have lately begun to focus on more intensely. It is the nitrogen free radica and it is particularly hazardous to brain cells.

Also critical, lipoic acid increases the efficiency of the energy factories of the cells—the mitochondria. With age energy production in mitochondria declines, meaning the: utilize oxygen and glucose less efficiently and product more free radical damage. Dr. Bruce Ames and colleague at the University of California, Berkeley, found that lipoi acid recharged energy levels in aged rats—in fact, i reversed the reduction of cellular energy in old rats by 51 percent! The rats’ physical activity also picked up, return ing them almost to the activity levels of young rats.

One other major talent of lipoic acid is that it helps con trol blood sugar and insulin levels and helps block forma tion of sugar-damaged proteins called AGEs (advance glycation end products) that accelerate aging and occur ii high levels in diabetics.

Lipoic acid is technically not a vitamin because you body can produce it, but production declines as you ag and by middle age is not enough for full protection.


Worried about declining memory? Lipoic acid may restore youthful memory. In dramatic experiments, German re­searchers at the Clinical Institute for Mental Health in Mannheim put lipoic acid in the drinking water of aged but otherwise healthy mice. Just like humans, animals tend to show signs of age-associated memory impairment as they grow older. And for the same probable reason: a lifetime of free-radical attacks on brain tissue. After two weeks, mice that drank both lipoic-acid-fortified water and plain drink­ing water were tested to see how well they could negotiate a maze; success depended on how well they remembered.

Sure enough, mice that got lipoic acid-spiked water did far better and displayed far better memories. In fact, some performed as well as or better than mice half their age, sug­gesting that lipoic acid’s antioxidant activity drastically slowed brain deterioration, perhaps by preventing neuron losses and/or repairing faulty transmission systems.

What’s also remarkable is how quickly lipoic acid worked its memory-restoring miracle—in only two weeks. In human terms that would be about a year-and-a-half for a seventy-five-year-old. Is it possible lipoic acid could work on human brains in such a short time—a mere year-and­a-half? “It might be possible, but it’s quite unproven,” says Dr. Packer. He also stresses that lipoic acid does not spur growth of new brain cells. It’s believed lipoic acid boosts memory by rejuvenating the functioning of specific recep­tors on nerve cell membranes that control message trans­missions throughout the brain.

Interestingly, lipoic acid did not improve memory in young animals. This suggests lipoic acid repairs and revi­talizes worn-out circuits in aged brain cells, but does not create supra-normal performance in young, healthy neu­rons.

“Lipoic acid is the most powerful antioxidant known to man.” —Lester Packer, professor of molecular and cell biology, University of California at Berkeley


Lipoic acid may keep you from having a stroke—but if you have one, it may help limit the damage and speed your recovery, according to impressive animal evidence. Labo­ratory animals given lipoic acid recover quickly from strokes, says Dr. Packer. He induced strokes in rats by block­ing the carotid artery that carries blood and oxygen to the brain. In such strokes, blood flow is disrupted, but then suddenly resumes as the blockage dissipates. That’s the dangerous part of a stroke—during so-called reperfusion, when the oxygen rushes back into the brain. That rush pro­vokes a burst of free radical formation in the brain of such magnitude that the brain’s ordinary antioxidant defenses cannot handle it and are wiped out. As a result defenseless brain cells are injured and killed (during reperfusion), resulting in temporary or permanent damage and possibly death. This is the nature of stroke damage. In Dr. Packer’s study, 80 percent of the rats died within a day after restora­tion of oxygen to the brain.

But what happens to such rats if you give them a shot of lipoic acid just before the blood and oxygen begin to flow normally back into the brain? “It’s amazing, incredi­ble,” says Dr. Packer. In such an experiment, only 25 per­cent of the stroke animals given lipoic acid died and all the survivors fully recovered without a trace of damage. “There’s no other antioxidant or drug that could perform such a feat of preventing stroke-related brain injury,” says Dr. Packer.

Further, Dr. Packer’s research proved that lipoic acid per­formed the magic by preventing free radical damage to vulnerable parts of the brain. An examination of the rats’ brains revealed that those denied lipoic acid had extensive free-radical induced brain damage. Those given lipoic acid had normal brains devoid of the free radical damage usu­ally seen after a stroke. Other researchers have found nearly identical rates of increased stroke survival due to treatment with lipoic acid.

So what can you make of this? Dr. Packer and other researchers suggest that lipoic acid might be used by physi­cians to treat stroke victims, lessening the reperfusion in­jury to the brain. There’s also the likelihood that keeping your brain cells supplied with high amounts of lipoic acid might protect them from damage in case of stroke, because their antioxidant defenses are much stronger.

Lipoic acid, Antioxidant, Stroke, Neurological Disorders, alpha lipoic acid, glutathione, vitamin e, coenzyme,


High blood sugar and insulin levels are not kind to nerve cells. In fact, these two villains can attack and destroy nerve cells in diabetics. Such disturbance of the peripheral ner­vous system, known as diabetic neuropathy, is a major and painful complication for many with diabetes. Yet, lipoic acid has been used successfully for twenty-five years in Europe to treat diabetic neuropathy. High doses of lipoic acid-200 to 600 milligrams daily—have relieved symp­toms markedly within two or three weeks, German inves­tigators report. Indeed, lipoic acid can even stimulate regeneration of nerve fibers in those with diabetic neu­ropathy.

Further, lipoic acid improves insulin function or “sensi­tivity” and lowers blood sugar in Type 2 (adult-onset) dia­betics, according to several studies by German researchers. The dose: 600 milligrams twice a day for four weeks. Promi­nent physicians in this country are now planning tests of lipoic acid to treat diabetes. It also seems likely, says Dr. Packer, that taking lipoic acid prevents the onset of Type 2 diabetes by helping stabilize blood sugar and insulin levels.


There’s another crucial way lipoic acid indirectly protects your brain. Lipoic acid is strongly connected to another important antioxidant called glutathione. This antioxidant is synthesized by the body, but it is extremely difficult to raise levels of glutathione in brain cells or even in blood cells. Taking glutathione orally won’t do it, because most of it is destroyed by enzymes in the digestive tract before it can be absorbed and delivered to cells. Even if you inject glutathione into the bloodstream, it does not reach the brain.

However, there is one sure way to raise blood and brain levels of glutathione: Take lipoic acid. Lipoic acid in the bloodstream causes glutathione to soar in the brain, stud­ies show. The lipoic acid molecule is small enough to slip through the blood-brain barrier, and once inside the brain, it mysteriously regenerates glutathione, something no other antioxidant can do.

In experiments, Dr. Packer found that adding lipoic acid to various types of animal and human cells in test tubes boosted production of glutathione by an astonishing 30 to 70 percent! Feeding lipoic acid to laboratory animals also quickly and significantly raised levels of glutathione in their organs and blood.

It’s impossible to estimate how critical glutathione is in protecting cells from free radicals. Some have called it the “master antioxidant.” Mainly it detoxifies the body. Stud­ies show people with high levels of glutathione stay younger longer in all ways. Low levels of glutathione predict chronic diseases, including degenerative brain disorders and early death.

BOTTOM LINE: The best way to make sure you have ultra-protective glutathione in brain cells is to take lipoic acid.


You get little alpha lipoic acid in food. Of sixteen foods ana­lyzed by Dr. Packer, spinach was the richest source by far. Next in line: beef kidney and heart, broccoli, beef liver, tomatoes, garden peas, Brussels sprouts, and rice bran. Bananas, orange peel, soybeans, and horseradish had none. Still, Dr. Packer says, you would have to eat more than fif­teen pounds of spinach to get a mere two milligrams of lipoic acid, a tiny amount.


Many experts favor a dose of 10 to 50 milligrams of lipoic acid a day for healthy people. Dr. Packer takes 100 mil­ligrams daily, half in the morning and half in the late after­noon or evening. If you are diabetic, you may need more-200 to 600 milligrams daily. Consult your doctor. Lipoic acid is available over the counter in health food stores. The major distributor is the well-regarded Henkel Corporation, which is funding many double-blind studies on lipoic acid in this country. Lipoic acid is sold under sev­eral different brands.

Toxicity? None reported, even in high doses. However, doses over 100 milligrams could conceivably lower blood sugar too much in normal nondiabetic individuals.

Jean-Paul Marat

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