Description
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Alpha-lipoic acid (ALA) is a sulfur-containing fatty acid compound that acts as a co-enzyme and antioxidant

(substances that neutralize harmful compounds known as free radicals). Being both water- and lipid-soluble

allows it to permeate all compartments of cells. As it can be synthesized in small quantities within the body, ALA

is not considered a vitamin.

Pharmacological Action
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Most of the biochemical activity of ALA occurs in the mitochondria.  ALA, thiamine, and niacin are co-factors of the

 enzyme complex that metabolizes pyruvate (under aerobic conditions) in order to generate ATP via the citric acid

 (Krebs) cycle and the electron transport cascade (Champe P and Harvey R, Lippincott’s Illustrated Reviews:

Biochemistry, 2nd ed. Philadelphia: J. B. Lippincott Company, 1994, p107).

ALA and DHLA (dihydrolipoic acid, its reduced metabolite) serve as an oxidation-reduction couplet that

neutralizes a broad range of free radicals within aqueous and lipid regions of cells, as well as intra- and

extra-cellular environments (Gurer H, et al, Antioxidant role of alpha-lipoic acid in lead toxicity. Free Radic Biol

Med 27(1-2):75-81, July 1999).  ALA may assist the functioning of other antioxidants (vitamins C and E,

coenzyme Q10, glutathione) (Hendler SS, et al, PDR for Nutritional Supplements. Montvale, NJ: Medical

Economics Co,, 2001, pp17-20).  ALA increases the intracellular antioxidant glutathione in vitro (Sen CK, et al,

Regulation of cellular thiols in human lymphocytes by alpha-lipoic acid: a flow cytometric analysis. Free Radic

Biol Med 1997;22(7):1241-57).

In rats with diabetic peripheral neuropathy, ALA improves digital sensory (but not sciatic-tibial) motor nerve

conduction velocity. In addition, ALA corrects endo-neural nutritive, but not composite, nerve blood flow (Stevens

MJ, et al, Effects of DL-alpha-lipoic acid on peripheral nerve conduction, blood flow, energy metabolism, and

oxidative stress in experimental diabetic neuropathy. Diabetes 49(6):1006-1015, June 2000.).

ALA inhibits HIV replication in cultured T-lymphocytes. (Baur A, er al, Alpha-lipoic acid is an effective inhibitor of

hyman immuno-deficiency virus (HIV-1) replication. Klin Wochensehr 1991 Oct 2;69(15):722-4). The mechanism

 involves, in part, the inhibition of DNA transcription factor NF-kappa B. (Suzuki YJ and Packer L, Inhibition of

NF-kappa B DNA binding by alpha-lipoic acid. Int Conf AIDS 1994 Aug 7-12;10(2):27 (abstract number 401A).

Possible Effects of Deficiency
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According to animal studies, deficiency signs include muscle atrophy, failure to thrive, brain atrophy, and lactic

acidosis. Although these states have not been replicated in humans, lower than normal levels of ALA have been

observed in diabetes mellitus, liver cirrhosis, and heart disease (Murray M, Encyclopedia of Nutritional

Supplements. Rocklin, CA: Prima Publishing, 1996, p343).

Clinical Applications/Research
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* Antioxidant

* AIDS

* Viral Hepatitis

* Diabetes Mellitus

* Diabetic Neuropathy

* Glaucoma

Antioxidant

ALA can be taken as an antioxidant to slow the aging process. It remains controversial whether its benefits for

this purpose are worth the price relative to the cost of vitamins C and E (Murray M, Encyclopedia of Nutritional

Supplements. Rocklin, CA: Prima Publishing, 1996, pp345).

AIDS

ALA has increased plasma ascorbate, total glutathione, T-helper cells and helper / suppressor ratio in

HIV-positive patients (Fuchs J, et al, Studies on lipoate effects on blood redox state in human immunodeficiency

virus infected patients. Arzneimittelforschung. 1993 Dec;43(12):1359).

Viral hepatitis

As hepatitis viral load increases, glutathione decreases. ALA, in combination with milk thistle and N-acetyl

cysteine, may be quite helpful for chronic hepatitis B and C. This approach may support the liver’s ability to

handle the pathologic effects of viral infestation (Bustamante J, et al, Rihn BH: Alpha-lipoic acid in liver

metabolism and disease. Free Radic Biol Med 24(6):1023-1039, April 1998).

Diabetes mellitus

ALA is approved in Germany for preventing and treating diabetic neuropathy. The effect may result from the

antioxidant activity. ALA may also help reduce blood glucose, cataract risk, and damaging glycosylation of

proteins. It also increases blood flow to peripheral nerves (Packer L, Antioxidant properties of lipoic acid and its

therapeutic effects in prevention of diabetes complications and cataracts. Annals NY Acad Sci 1994;738:257-64;

Nagamatsu M, et al, Lipoic acid improves nerve blood flow, reduces oxidative stress, and improves distal nerve

conduction in experimental diabetic neuropathy. Diabetes Care 1995;18:1160-67; Jacob S, et al, Enhancement

of glucose disposal in patients with Type 2 diabetes by alpha-lipoic acid. Arzneimittel Forschung

1995;45:872-74; Kawabata T and Packer L, Alpha-lipoate can protect against of serum albumin, but not

low-density lipoprotein. Biochem Biophys Res Comm 1994;203:99-104)  In a four-week, randomized,

multi-centered trial, 74 patients with type 2 diabetes received either placebo or ALA at 600 mg once, twice, or

three times daily. The results indicated that oral ALA may improve insulin sensitivity in type 2 diabetics (Jacob S,

et al, Oral administration of RAC-alpha lipoic acid modulates insulin sensitivity in patients with type 2 diabetes

mellitus: a placebo-controlled pilot trial. Free Radic Biol Med 27(3-4):309-314, August 1999).

Glaucoma

Preliminary evidence indicates that a daily dose of 150 mg of alpha lipoic acid for one month improves visual

function in people with glaucoma (Filina AA, Davydova NG, Endrikhovskii SN, et al. Lipoic acid as a means of

metabolic therapy of open-angle glaucoma. Vestn Oftalmol 1995;111:6–8.).

Commonly Suggested Therapeutic Dosage
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- Antioxidant support: 20 – 50 mg. daily

- Diabetes: 300 – 600 mg. daily

- AIDS: 150 mg. three times daily (Hendler, Murray)

- Glaucoma:  150 mg daily

Sources
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The best sources are believed to be those foods rich in mitochondria – red meat (skeletal muscle, heart, liver,

kidney). Other sources are yeast, spinach, and broccoli.

Contraindications/Toxicology
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No adverse effects have been reported in 30 years of clinical use in diabetes. Dosage up to 600 mg daily is

non-problematic. Very low toxicity has been observed in animal studies. Safety in pregnant and nursing women

has not been proven. Because ALA lowers glucose in diabetics, blood sugar monitoring is crucial in this

condition. Sugar-lowering medicines should be adjusted accordingly to avoid hypoglycemic crises. ALA may

reduce the metabolic consumption of other antioxidants (vitamins C and E). ALA works with vitamins B1 and B3

in cellular energy production.

The statements above have not been evaluated by the FDA.  The nutritional suggestions and research provided are not intended to diagnose, treat, cure or prevent disease and should not be used as a substitute for sound medical advice.  Please see your health care professional in all matters pertaining to your physical health.  The Professional Description, Professional Notes, Patient Instructions, and items marked with an astrisk (*) are provided by the practitioner and are the sole responsibility of the practitioner.Copyright © 1998-2002 Standard in Natural Solutions, LLC.