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Interviewed by John McKenzie on

World News Tonight in September 1997,
Lester Packer, Ph.D., of the University of
California, Berkeley, said ALA could be a
missing link in the treatment and preven-
tion of disease. He added that it is proba-
bly the most potent naturally occurring
antioxidant known to man.
1
Packer, who with his associates has pub-
lished more than 60 studies on ALA,
explained that the product has its own
antioxidant properties and is more potent
than other antioxidants, including vitamin
C and vitamin E. In addition, it increases
the effectiveness of both vitamins.
Type 2 (non-insulin-dependent) diabet-
ics may improve their insulin function and
glucose metabolism with ALA supplements.
Researchers gave 10 thin and 10 obese
patients with Type 2 diabetes 600 mg of
oral alpha-lipoic acid twice daily for four
weeks. During that time, insulin function,
A
n essential cofactor in energy metab-
olism in organisms from microbes to
human beings, alpha-lipoic acid
(ALA)also referred to as lipoic acid and
thioctic acidprovides sufficient protection
against arthritis, cataracts, diabetes, heart
disease, aging, heavy-metal poisoning, liver
cirrhosis, kidney damage, AIDS, and other
health conditions. ALA is found in spinach
and other foods, but it is unlikely that a
food source will contain enough of the
product to be effective.
Unlike other antioxidants, such as vi-
tamin C, which is water soluble, and vita-
min E, which is fat soluble, ALA is both
water and fat soluble, making it bioavail-
able in a variety of locations in the body.
ALA and dihydrolipoic acid (DHLA), its
reduced form, are effective against a vari-
ety of free radicals, those wayward mole-
cules that accelerate aging and contribute
to many health problems.
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Alpha-Lipoic Acid
McGraw-Hill's Terms of Use
glucose, and lactate and pyruvate levels were
measured to determine glucose metabolism.
The ALA supplements were found to be
beneficial to both groups. The thin diabet-
ics registered better insulin function and
decreases in fasting glucosesuggesting a
shift toward normalizationwhile the obese
patients had improvements in insulin func-
tion. In both groups, levels of lactate and
pyruvate decreased, indicating more normal
glucose metabolism. ALA seems to work
by stepping up the burning of glucose.
2
Diabetics often have an increased risk
of neuropathy, which is characterized by
reduced heart-rate variability. In a study called
Alpha-Lipoic Acid in Diabetic Neuropathy
(ALADIN), 328 patients with diabetic neu-
ropathy were given either 100, 600, or
1,200 mg of ALA or a placebo or look-alike
pill daily for three weeks. Researchers in the
Deutsche Kardiale Autonome Neuropathie
(DEKAN) Studie gave 73 patients with car-
diac autonomic neuropathy either 800 mg
of ALA or a placebo daily for four months.
In the ALADIN study, pain and other symp-
toms decreased significantly with dosages of
600 or 1,200 mg daily for 19 days. ALA also
improved heart-rate variability in the diabet-
ics with cardiac autonomic neuropathy. With
this and other confirmation, researchers
believe that ALA exerts a protective antiox-
idant effect on nerve cells.
3
ALA is being used successfully to treat
alcohol-induced liver damage, amanita mush-
room poisoning, and metal toxicity. It has
also been found useful in treating diabetic
polyneuropathy, a type of nerve damage.
ALA acts as a natural supplement, somewhat
like vitamin E, in preventing many diseases,
especially those influenced by free radicals.
4
To test the value of ALA in treating
diabetics, researchers in Germany and else-
where gave ALA and gamma-linolenic acid
(GLA) to diabetic laboratory animals in an
attempt to improve nerve function and
blood flow. Each substance was found to
cause modest improvements in the ani-
mals, and when combined, showed a
marked synergistic effect.
5
ALA assumes some of the biochemical
functions of glutathionea primary antiox-
idant containing three amino acids
including maintaining high blood levels of
vitamin C and recycling vitamin E. According
to animal experiments, ALA may prevent
cataracts, which are caused by oxidative
stress in the lens of the eye.
6
ALA and DHLA have substantial
antioxidant properties, including the abil-
ity to quench a variety of reactive oxygen
species, inhibit reactive oxygen-generators,
and spare other antioxidants. A number of
clinical studies, including some reported
here, address the use of ALA as a therapeu-
tic agent for such diverse conditions as
myocardial and cerebral ischemia-reperfusion
injury, heavy-metal poisoning, radiation
damage, diabetes, neurodegenerative dis-
eases, and AIDS.
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Burton Berkson, M.D., Ph.D., of the
Integrative Medical Center in Las Cruces,
New Mexico, has seen firsthand how ALA
can save lives. A 35-year-old woman with
severe hepatitis C was informed by her
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physicians that she probably would die
without a liver transplant. After Berkson
treated her with ALA, she was able to
avoid the transplant.
8
A number of recent studies have also
shown alpha-lipoic acid to be effective in
treating diabetic neuropathy, explained
Berkson, who is principal FDA investiga-
tor for intravenous ALA treatments in
acute liver diseases and a consultant to the
National Centers for Disease Control and
Prevention. A 55-year-old man with adult-
onset diabetes was informed by his doctors
that there was practically nothing they could
do about his incapacitating burning feet and
pins and needles in his hands. After months
of treatment, including ALA, this man no
longer suffers these symptoms. Alpha-lipoic
acid should be considered in the same class
as vitamin E, based on its remarkable bene-
fits and impressive research.
Berkson became interested in ALA
after treating a patient with hepatic necro-
sis caused by eating toxic mushrooms. An
intravenous infusion of ALA 30 hours
after the patient had ingested the mush-
rooms brought an improvement within
one hour, and the patient was soon dis-
charged. Berkson prescribed ALA for two
additional patients with mushroom poi-
soning, and within a short time they were
feeling better and had almost normal liver
function.
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Since then he has prescribed
ALA, both orally and intravenously, to
more than 100 patients.
ALA acts as a coenzyme for the produc-
tion of acetyl coenzyme alpha-dihydrolipoic
acid, which in turn recycles other anti-
oxidants such as vitamin C. Like other
researchers, Berkson has found ALA to
inhibit HIV replication in cultured T cells,
prevent cataracts, protect the kidney from
amino-glycoside damage, protect islet cells
in the pancreas from inflammatory attack,
and increase helper T cells in the blood,
among other benefits. In addition, ALA
reduces the toxic side effects of some
forms of chemotherapy. ALA crosses the
blood-brain barrier easily and plays a sig-
nificant role in a variety of neural meta-
bolic processes.
Berkson has successfully treated three
patients with chronic hepatitis C who are
now thriving and did not require a liver
transplant. Most researchers report that
there are no effective treatments for chronic
hepatitis C, and that interferon and antiviral
drugs have less than a 30 percent response
rate. For those who do undergo a trans-
plant, the new liver often becomes infected,
Berkson said. One year of antioxidant ther-
apy as prescribed by Berkson costs less than
$2,000, compared to $300,000 for a liver
transplant.
10
The three patients were selected at ran-
dom from a group of about 50 chronic
hepatitis C subjects at Berksons Integrative
Medical Center. Each day they were given
600 mg of ALA in two divided doses; 900
mg of silymarin (from milk thistle) in three
divided doses; and 400 mcg of selenome-
thionine (selenium) in two divided doses.
Patient No. 1 was also treated with B com-
plex vitamins, vitamin C, vitamin E, and
A l p h a - L i p o i c A c i d
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coenzyme Q10. Patient No. 2 was also
given medication for insomnia. Patient No.
3 was also treated for other health prob-
lems. All three show no signs of hepatitis.
By helping recycle vitamin E in the
body, ALA and DHLA keep the concentra-
tion of the vitamin high so that it can per-
form its antioxidant functions adequately,
according to M. Podda and colleagues at
the University of California, Berkeley. ALA
and DHLA have also been shown in vitro
to possess potent antioxidant activity and
may even substitute for vitamin E. Research
supports the idea that the major effect of
ALA in vitamin Edeficient animals is to
replace the vitamin rather than recycle it. In
any case, it cannot be ruled out that ALA
antioxidant activity may be acting through
other antioxidantssuch as coenzyme Q10
or vitamin Cwhere in vitro recycling has
been described.
11
For athletes, ALA helps prevent muscle
and tissue damage during intense workouts
and speeds muscle recovery, according to
Dallas Clouatre, Ph.D., and Will Brink.
ALA regenerates not only vitamins C and E
but also glutathione in the cytoplasm of the
cell, and coenzyme Q10 within the mito-
chondria. ALA quenches an unmatched
variety of free radicals and also regenerates
other antioxidant and free radical quench-
ing systems.
12
If you are an endurance athlete,
Clouatre and Brink wrote, you are pump-
ing many times the amount of oxygen
through your system when you are exer-
cising than when you are at rest. Burning
glucose and fats for fuel (as we do during
exercise) generates free radicals, and push-
ing so much oxygen through your system
allows this source of oxidation and free
radicals greater access to your tissues.
Similarly, an athlete performing resis-
tance exercise such as weight training may
be causing countless small tears in the mus-
cle (microtrauma) and other forms of tissue
damage. Microtrauma leads to localized
inflammation, pain, and swelling as the
immune system attempts to clear out dam-
aged tissue by generating free radicals to
destroy both bacteria and cells that are to
be replaced.
Spinach is the richest source of lipoylly-
sine, which is protein-bound ALA. Large
amounts of the substance are also found in
broccoli, kidney, heart, and liver. There is
little or no lipoyllysine in garden peas,
Brussels sprouts, rice bran, or bananas.
Researchers do not yet know if the protein-
bound form of ALA has as much activity as
free ALA found in supplements.
13
According to a number of studies,
patients with HIV have a compromised
antioxidant defense system. Therefore,
blood antioxidants are decreased and per-
oxidation products of fats and proteins are
increased in these patients, reported
Michael Murray, N.D. This blood profile
may contribute to the progression of AIDS,
since antioxidants such as glutathione pre-
vent viral replication while reactive oxidants
tend to stimulate the virus.
14
A small pilot study was designed to
determine the short-term effect of ALA
1 0 0 S U P E R S U P P L E ME N T S F O R A L O N G E R L I F E
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supplementation (150 mg three times daily)
in HIV positive patients, Murray said. The
supplementation increased plasma ascorbate
(vitamin C) in 9 of 10 patients, total glu-
tathione in 7 of 7 patients, total plasma sul-
fur groups in 8 of 9 patients, T-helper
lymphocytes and T-helper/suppressor cell
ratio in 6 of 10 patients; while the level of
free radical damage decreased in 8 of 9
patients. This pilot study indicated that
lipoic acid supplementation led to signifi-
cant beneficial changes in the blood of
HIV infected patients.
For general antioxidant support, the
recommended dosage is 20 to 50 mg/day,
Murray wrote. In the treatment of diabetic
neuropathy, the recommended dose is now
400 to 800 mg/day. For the treatment of
AIDS, the recommended amount is 150
mg three times a day.
Lipoic acid supplementation appears
to be very safe as there have not been any
reports of adverse effects in over three
decades of use in the treatment of diabetic
neuropathy, Murray said. In addition,
animal studies have shown it to be of very
low toxicity.
In addition to sparing vitamins C and
E and other antioxidants, ALA works syn-
ergistically with two B vitaminsB
1
and
B
3
in cellular energy production. ALA also
may improve blood sugar control in dia-
betes, resulting in a reduction in the dosage
of insulin or oral blood sugarlowering
drugs.
ALA is available in tablets and capsules.
According to Dr. Packer, it is probably the
most potent naturally occurring antioxi-
dant known to humankind.
References
1. McKenzie, John, Health Report,
World News Tonight with Peter Jennings,
Sept. 29, 1997.
2. Konrad, T., et al., Alpha-Lipoic Acid
Treatment Decreases Serum Lactate and
Pyruvate Concentrations and Improves
Glucose Effectiveness in Lean and Obese
Patients with Type 2 Diabetes, Diabetes
Care 22: 28087, 1999.
3. Ziegler, D., and F. A. Gries, Alpha-
Lipoic Acid in the Treatment of
Peripheral and Cardiac Autonomic
Neuropathy, Diabetes 46 (Suppl. 2):
S62S66, 1997.
4. Bustamante, J., et al., Alpha-Lipoic
Acid in Liver Metabolism and Disease,
Free Radical Biology and Medicine 24:
102339, 1998.
5. Cameron, N. E., et al., Effects of
Alpha-Lipoic Acid in Neurovascular
Function in Diabetic Rats; Interaction
with Essential Fatty Acids, Diabetologia
41: 39099, 1998.
6. Maitra, I., et al., Alpha-Lipoic Acid
Prevents Buthionine Sulfoxamine-
Induced Cataract Formation in Newborn
Rats, Free Radical Biology and Medicine
18: 82329, 1995.
7. Packer, Lester, et al., Alpha-Lipoic
Acid as a Biological Antioxidant, Free
Radical Biology and Medicine 19(2):
22750, 1995.
A l p h a - L i p o i c A c i d
5
8. Berkson, Burton M., The Remarkable
Benefits of Alpha-Lipoic Acid, Paper
presented at 1998 World Congress,
Oxygen Club of California, Santa
Barbara, 1998.
9. Berkson, Burton M., Alpha-Lipoic Acid
(Thioctic Acid): My Experience with
This Outstanding Therapeutic Agent,
Journal of Orthomolecular Medicine
13(1): 4448, 1998.
10. Berkson, Burton M., A Conservative
Triple Antioxidant Approach to the
Treatment of Hepatitis C, Medizinische
Klinik 94 (Suppl. III): 8489, Oct. 15,
1999.
11. Podda, M., et al., Alpha-Lipoic Acid
Supplementation Prevents Symptoms of
Vitamin E Deficiency, Biochemical and
Biophysical Research Communications
204(1): 98104, Oct. 14, 1994.
12. Clouatre, Dallas, and Will Brink, Alpha-
Lipoic Acid for Total Performance,
Lets Live, Oct. 1997, 6567.
13. Lodge, J. K., et al., Natural Sources
of Lipoic Acid: Determination of
Lipoyllysine Released from Protease-
Digested Tissues by High Performance
Liquid Chromatography Incorporating
Electrochemical Detection, Journal of
Applied Nutrition 49: 311, 1997.
14. Murray, Michael, Lipoic AcidA
New Breed of Antioxidant, Natural
Medicine Journal 1(3): 2021, April
1998.
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