ALPHA LIPOIC ACID
Lipoic Acid may Enhance the Function of these Substances
Carbohydrates
Lipoic Acid may act as a coenzyme in the metabolism of Carbohydrates.
Lipoic Acid may improve the body's utilization of Glucose within the Muscles.
Lipoic Acid may facilitate the conversion of Glycogen into Glucose.
Enzymes
Lipoic Acid may protect Catalase from oxidation.
Lipoic Acid (applied topically) may activate Activator Protein 1 in the Skin, which in turn may stimulate the production of Matrix Metalloproteinases.
Lipoic Acid is an essential cofactor for Pyruvate Dehydrogenase (Lipoamide).
ùùùLipoic Acid may protect Superoxide Dismutase (SOD) from oxidation.
Hormones
ùùùLipoic Acid may improve the actions of Insulin (it mimics the function of Insulin).
Krebs Cycle Chemicals
ùùùLipoic Acid may increase the body’s production of Adenosine Triphosphate (ATP) within Muscles.
Lipids
ùùùLipoic Acid may function as a coenzyme for the metabolism of Fatty Acids.
Nucleic Acids
ùùùLipoic Acid may inhibit damage to mitochondrial DNA (mtDNA).
Organic Acids
Lipoic Acid is essential for the decarboxylation of Pyruvic Acid and other Keto Acids.
Peptides
ùùùLipoic Acid may increase intracellular Glutathione levels by 30 - 70%:
Lipoic Acid (1% cream/lotion applied topically) increases the Glutathione content of the Skin.
Pharmaceutical Drugs
Lipoic Acid is synergistic with and increases the effectiveness of Zidovudine.
Proteins
Lipoic Acid (applied topically) beneficially activates Activator Protein 1 (AP-1) in the Skin.
Lipoic Acid (applied topically) may facilitate the removal of old, damaged Collagen in the Skin (via its ability to activate Activator Protein 1 which in turn stimulates the production of Matrix Metalloproteinases that “digest” old, damaged Collagen in the Extracellular Matrix). In addition, Lipoic Acid may inhibit the inflammatory Cytokine-induced destruction of normal Skin Collagen.
Lipoic Acid may function as a coenzyme in the metabolism of Proteins:
ùùùLipoic Acid may inhibit the Cross-Linking (glycosylation) of some types of endogenous Proteins (including Albumin).
\Quinones
ùùùLipoic Acid may regenerate Coenzyme Q10.
Vitamins
ùùùLipoic Acid may help to recycle Vitamin C (it facilitates the conversion of Dehydroascorbic Acid to Ascorbic Acid):
Lipoic Acid (1% cream/lotion applied topically) may increase the Vitamin C content of the Skin.
ùùùLipoic Acid may prevent the symptoms of Vitamin E deficiency (although Lipoic Acid does not spare or regenerate Vitamin E it exerts a Vitamin E-like effect and counteracts the effects of Vitamin E deficiency)
ùùùLipoic Acid (1% cream/lotion applied topically) may increase the Vitamin E content of the Skin.
Lipoic Acid may Counteract these Potentially Toxic Substances
Amino Acids
ùùùLipoic Acid may inhibit the excitotoxic effects of Glutamic Acid.
Carbohydrates
ùùùLipoic Acid may inhibit the ability of Fructose to cause Cross-Linking of the body’s endogenous Proteins.
Electromagnetic Radiation
ùùùLipoic Acid may reduce the toxic effects of exposure to Radioactivity.
Enzymes
ùùùLipoic Acid may inhibit Aldose Reductase (an enzyme implicated in Cataracts and Diabetes Mellitus).
ùùùLipoic Acid (after its conversion to DHLA) may inhibit Cyclooxygenase-2 (COX-2).
Lipoic Acid (after its conversion to DHLA) may inhibit Lipoxygenase (15-Lipoxygenase form).
Lipoic Acid may inhibit Viral Reverse Transcriptase.
Fungi
ùùùLipoic Acid may increase the survival rate of people who have consumed Amanita phalloides Mushrooms.
ùùùLipoic Acid may help to prevent and reverse the adverse effects of Mycotoxins.
Hormones
ùùùLipoic Acid may inhibit the ability of Angiotensin 2 to damage the Kidneys.
Lipopigments
ùùùLipoic Acid may facilitate the removal of Lipofuscin from the Brain. references
Minerals
ùùùLipoic Acid may help to protect the body from Arsenic poisoning.
ùùùLipoic Acid may chelate (binds to and remove) accumulated Cadmium from the body and may help to prevent Cadmium from damaging the Liver.
ùùùLipoic Acid may counteract the Oxidation produced by Lead.
ùùùLipoic Acid may chelate (binds to and removes) accumulated Mercury from the body. references
ùùùLipoic Acid may inhibit the ability of Mercury to damage Neurons.
Organic Acids
Lipoic Acid may reduce the accumulation of Lactic Acid.
Pharmaceutical Drugs
Lipoic Acid may reduce the toxicity of Cyclophosphamide.
ùùùLipoic Acid may inhibit the ability of Cyclosporine to damage the Kidneys.
ùùùLipoic Acid may counteract the cardiotoxic and effects of Doxorubicin and may inhibit the ability of Doxorubicin to damage the Kidneys.
Proteins
ùùùLipoic Acid may facilitate the removal of Amyloid-Beta Protein from the Brain and may minimize the toxic effects of Amyloid-Beta Protein in the Brain.
Lipoic Acid may inhibit the activation of Nuclear Factor-Kappa B.
Recreational Drugs
ùùùLipoic Acid may help to prevent Alcohol (ethanol)-induced Brain damage.
Vitamin Byproducts
ùùùLipoic Acid may regenerate Dehydroascorbic Acid back into Ascorbic Acid (Vitamin C).
These Substances Enhance the Function of Lipoic Acid
Minerals
Sulfur is an essential component of Lipoic Acid.
Vitamins
ùùùVitamin E may enhance Lipoic Acid's Antioxidant properties.
These Factors Interfere with Lipoic Acid
Aging Process
The body’s Lipoic Acid content may decline in tandem with the progression of the Aging Process.
Lipoic Acid Interferes with these Substances
Minerals
Lipoic Acid binds to (chelates) Iron and may (as a result of this binding) cause Iron deficiency.
Dietary Sources of Lipoic Acid note
Meats: Liver
Vegetables: Potato Spinach
Broccoli
Yeasts: Brewer’s Yeast
Forms of Lipoic Acid
Alpha-Lipoic Acid (ALA) is the usual form of supplemental Lipoic Acid. Most synthetic Lipoic Acid supplements contain a 1:1 ratio of the two isomers of Alpha-Lipoic Acid (= R,S-Lipoic Acid):
R-Lipoic Acid (also known as RLA; R-ALA; R(+)-Lipoic Acid) is one of the two isomers of Alpha-Lipoic Acid. This isomer is more therapeutically potent than S-Lipoic Acid. High quality Lipoic Acid supplements contain only this isomer:
Potassium-R-Lipoic Acid is the Potassium salt of R-Lipoic Acid.
R,S-Lipoic Acid (also known as Racemate Lipoic Acid; R,S-ALA; R(+)S(-)-Lipoic Acid) is a mixture of equal proportions of R-Lipoic Acid and S-Lipoic Acid.
S-Lipoic Acid (also known as S-ALA; SLA; S(-)-Lipoic Acid) is one of the two isomers of Alpha-
Lipoic Acid. This isomer exerts little, if any, therapeutic activity.
Dihydrolipoic Acid (DHLA) is the “reduced” (= electrons added) form of Lipoic Acid with equal or superior therapeutic benefits to Lipoic Acid. Oxidation of DHLA produces Alpha-Lipoic Acid. This form is available commercially in supplemental form. Alpha-Lipoic Acid readily converts to DHLA within the body. The conversion of R-Lipoic Acid to R-DHLA is performed by the Pyruvate Dehydrogenase Complex (PDH) with the help of NADH in the Mitochondria. DHLA possesses significantly more Antioxidant activity compared with R-Lipoic Acid or S-Lipoic Acid:
R-Dihydrolipoic Acid (also known as R-DHLA) is the active (reduced) isomer of DHLA. When R-
Dihydrolipoic Acid reacts with a Free Radical it is converted (oxidized) back to R-Lipoic Acid.
S-Dihydrolipoic Acid (also known as S-DHLA) is the inactive isomer of DHLA.
Bioavailability
ùùùLipoic Acid is both water-soluble and fat-soluble.
The half-life of orally-ingested Lipoic Acid is approximately 30 minutes.
ùùùLipoic Acid is capable of penetrating the Skin when applied topically.
ùùùLipoic Acid is capable of penetrating the Blood-Brain Barrier.
Dosage Recommendations
Antioxidant
The Antioxidant effects of Lipoic Acid occur at a dosage level of 25 - 50 mg per day.
Preventative Dosage
The most effective dosage of supplemental Lipoic Acid for healthy people for preventative purposes is in the range of 250 - 750 mg per day.
Specific Ailments
The therapeutic dosage of Lipoic Acid that has been found to increase Energy levels in Chronic Fatigue Syndrome (CFS) patients is 500 - 800 mg per day. dosage of 800 mg of Lipoic Acid per day has been shown to protect the Liver from the toxic effects of many toxins.
Clinical trials of Lipoic Acid on Diabetes Mellitus patients have illustrated that higher doses (300 - 1,200 mg per day) alleviates several aspects of Diabetes Mellitus (including Diabetic Retinopathy).
Topical Products
Although most topical Lipoic Acid products are at a strength of 1% Lipoic Acid, it is claimed that the optimal concentration should be 3% to 10%. Dermatologists commonly use 5%.
Commercial Availability of Lipoic Acid Supplements
“Singular” Oral Lipoic Acid Products
Lipoic Acid is available from health food stores and internet-based suppliers in the form of:
- 5 mg capsules (R,S-Lipoic Acid)
- 50 mg tablets (R,S-Lipoic Acid)
- 50 mg capsules (R,S-Lipoic Acid)
- 50 mg capsules (R-Lipoic Acid)
- 100 mg tablets (R,S-Lipoic Acid)
- 100 mg capsules (containing 50 mg R-Lipoic Acid + 50 mg R-Dihydrolipoic Acid)
- 100 mg capsules (R,S-Lipoic Acid)
- 100 mg capsules (R-Lipoic Acid)
- 150 mg capsules (R-Lipoic Acid)
- 150 mg capsules (R-Dihydrolipoic Acid)
- 100 mg capsules (containing 75 mg R-Lipoic Acid + 75 mg R-Dihydrolipoic Acid)
- 200 mg tablets (R,S-Lipoic Acid)
- 250 mg capsules (R,S-Lipoic Acid)
- 300 mg capsules (R,S-Lipoic Acid)
- powder/crystals (R,S-Lipoic Acid)
- powder/crystals (R-Lipoic Acid)
- liquid containing Potassium-R-Lipoic Acid (5 mg of R-Lipoic Acid per drop)
Topical Products
Lipoic Acid is an active ingredient (usually at a concentration of 1%) in some topical Skin care products (Cosmeceuticals) including:
- Face Firming Activators
- Eye Creams
- Lip Creams
- Body Lotion
Chemical Data
Chemically, Lipoic Acid is a Saturated Fatty Acid that has an unusual ring structure containing two Sulfur atoms at one of the molecule.
Lipoic Acid is a dithiol (it contains two Sulfur groups).
Chemical Names
1,2-Dithiolane-3-pentanoic acid
Dithio-Octanoic Acid
6,8-Dimercapto-Octanoic Acid
Molecular Formula
C8H14O2S2
Health Benefits of Lipoic Acid
Aging Process
ùùùLipoic Acid may retard some aspects of the Aging Process:
ùùùLipoic Acid may inhibit damage to mitochondrial DNA (mtDNA) - the principal detrimental process implicit in the Mitochondrial DNA Theory of Aging.
Lipoic Acid may possess Life Extension properties.
Cardiovascular System
ùùùLipoic Acid may help to prevent Atherosclerosis.
Lipoic Acid may lower Blood Pressure in Hypertension patients.
Lipoic Acid may protect against the toxic effects of Ischemia (i.e. it may protect against Ischemia-Reperfusion Injury).
Lipoic Acid may inhibit the ability of Peroxyl Free Radicals to damage Red Blood Cells.
ùùùLipoic Acid (when consumed prior to the occurrence of an Ischemic Stroke) may minimize the Brain damage incurred by people who experience an Ischemic Stroke (due to the Antioxidant effects of Lipoic Acid).
Cells
Lipoic Acid may help to prevent Free Radicals damage to Cell Membranes.
Lipoic Acid may help to preserve the Mitochondria of Cells.
Ears/Hearing
Lipoic Acid may retard the further progression of Age-Related Hearing Loss (by retarding damage to mitochondrial DNA in the Ears’ Cochlea).
Lipoic Acid may inhibit damage to mitochondrial DNA (mtDNA) in the Cochlea. references
ùùùLipoic Acid (25 mg per day or more) may help to reverse Noise-Induced Hearing Loss.
Excretory System
Lipoic Acid may prevent the damage to the Kidneys (Diabetic Nephropathy) that is a common side effect of Diabetes Mellitus and Lipoic Acid may inhibit Angiotensin 2-induced Kidney damage.
Eyes/Vision
Lipoic Acid may help to prevent Age-Related Macular Degeneration (ARMD) (due to the Antioxidant properties of Lipoic Acid; Lipoic Acid may penetrate Eye tissue and protect both the Lens and the Retina from degeneration).
Lipoic Acid may reduce the risk of Cataracts in Diabetes Mellitus patients and in normal, healthy persons.
Lipoic Acid may inhibit the activation of Aldose Reductase (an enzyme that is implicated in Cataracts due to its ability to catalyze the production of Galacticol and Sorbitol from Galactose and Glucose).
ùùùLipoic Acid may alleviate Glaucoma.
Lipoic Acid may protect the Lens of the Eye from degeneration.
Lipoic Acid (600 mg per day) improves (the chronic progressive external form of) Opththalmoplegia.
Lipoic Acid may protect the Retina of the Eye from degeneration.
Immune System
Lipoic Acid (450 mg per day) may improve the overall health of Acquired Immune Deficiency Syndrome (AIDS) patients.
Lipoic Acid may increase the plasma Glutathione levels of AIDS patients.
Lipoic Acid may increase the plasma Vitamin C levels of AIDS patients.
ùùùLipoic Acid may retard the replication of the HIV Virus (by inhibiting the HIV Viral Transcriptase enzyme that participates in the replication of HIV, and by inhibiting Nuclear Factor Kappa B (NF-Kappa B) that activates HIV replication).
ùùùLipoic Acid may help to prevent Cancer (damage to the body’s Deoxyribonucleic Acid (DNA) is one of the underlying mechanisms for the initiation of Cancer - Lipoic Acid inhibits the ability of Free Radicals to damage DNA).
Lipoic Acid may stimulate various aspects of the Immune System.
Lipoic Acid may reduce Inflammation (primarily by inhibiting Nuclear Factor Kappa-B)
Liver
ùùùLipoic Acid (600 mg per day) may be useful for the treatment of Hepatitis C (especially when it is combined with Selenium and Milk Thistle).
Lipoic Acid has been used therapeutically to treat Liver ailments and it may protect the Liver from the toxic effects of many Pharmaceutical Drugs and Toxins:
ùùùLipoic Acid is an effective therapy in the treatment of Liver damage caused by toxic Mushrooms, Alcohol (ethanol), Carbon Tetrachloride and toxic Minerals.
Metabolism
Lipoic Acid possesses Antioxidant properties (it functions as both a water-soluble and a fat-soluble Antioxidant).
Lipoic Acid is a potent scavenger of Hydroxyl Free Radicals.
Lipoic Acid may inhibit the ability of Peroxyl Free Radicals to damage Red Blood Cells.
Lipoic Acid may increase the body’s Basal Metabolic Rate (BMR).
Lipoic Acid may normalize Blood Sugar levels.
Lipoic Acid (500 - 800 mg per day) may increase Energy levels in some Chronic Fatigue Syndrome (CFS) patients.
ùùùLipoic Acid may inhibit the Cross-Linking of the body’s endogenous Proteins (including Cross-Linking caused by Glucose).
Lipoic Acid (Dihydrolipoic Acid form) may be useful for the treatment of Cystic Fibrosis (due to its ability to inhibit Elastase and to exert anti-mucolytic actions).
Lipoic Acid may prevent and alleviates many of the detrimental side effects that occur as a result of Diabetes Mellitus (both Type 1 and Type 2)
ùùùLipoic Acid may prevent the onset of Diabetes Mellitus Type 1.
Lipoic Acid may improve Glucose utilization and disposal in Diabetes Mellitus Type 2 patients.
Lipoic Acid may reduce the incidence of Cataracts in Diabetes Mellitus patients (by inhibiting the Aldose Reductase enzyme that is implicated in Cataracts).
Lipoic Acid prevents the damage to the Kidneys (Diabetic Nephropathy) that is a common side effect of Diabetes Mellitus.
Lipoic Acid may prevent the (diabetic) Neuropathy that is a common side effect of Diabetes Mellitus.
Lipoic Acid may increase Brain and Muscle Energy levels.