Are Alpha Lipoic Acid Effective in Treating HIV?

Alpha lipoic acid (also known as thioctic acid, or ALA) may play an important therapeutic role for HIV-infected people. ALA has been shown to directly block NF-kappa B activation, to directly inhibit HIV replication in cell cultures, and to successfully treat peripheral neuropathy in individuals with diabetes mellitus.

Alpha Lipoic Acid and HIV

ALA, a naturally occurring disulfide-compound that acts as a cellular coenzyme, inhibits replication of HIV-1 in cultured lymphoid T-cells. Experimental results show that lipoic acid is an effective inhibitor of human immuno-deficiency virus (HIV-1) replication. In a study with HIV-infected participants, with ALA provided a variety of advantages related to antioxidant status, T-helper lymphocytes, and the T-helper/ suppressor cell ratio. In a small study conducted in Germany, scientists administered 450 mg ALA per day for 14 days and found important increases in plasma vitamin C and glutathione in a majority of the patients.

In vitro study done at “Kumamoto University” in Japan has shown that ALA significantly depresses both HIV tat gene activity and HIV infectivity, and is active in both acute and chronically infected cells. ALA blocks the activation of a substance called NF-kappa B, which is essential for the transcription of the HIV virus. Gene expression of HIV depends on a host cellular transcription factors including NF-kappaB. ALA interrupts HIV replication by completely blocking the activation of NF-kB in cell cultures at a concentration of 2 mM. Alpha lipoic acid has direct effect as an HIV-1 replication inhibitor at concentrations of 70 mg/L and has a synergistic antiviral property when combined with Zidovudine (a type of anti retroviral drug commonly known as AZT) at a concentration of 7mg/mL.

HIV patients are known to have low tissue levels of glutathione. In a study investigated the use of ALA supplementation on a group of HIV positive people. At the end of a 3 week period, participants were determined to have increased levels of plasma vitamin C and glutathione and a corresponding decrease in lipid peroxidation. Other a study was carried out in 33 HIV-infected individuals with a history of highly active antiretroviral treatment (HAART) unresponsiveness to test the hypothesis of whether supplement with alpha-lipoic acid would increase blood total glutathione and improve immune T-cell function. After six months of therapy, the mean whole blood total glutathione level in the ALA-treated group increased significantly compared with placebo. In response to the CD3 monoclonal antibody, lymphocyte proliferation decreased 66% in the placebo group over 6 months, compared with  a 3.7-fold enhancement in the anti-CD3 response in the ALA-therapy group.

Alpha Lipoic Acid for Eye Health is Important

Alpha lipoic acid (scientific name 1,2-dithiolane-3-pentanoic acid) is a vitamin-like chemical called an antioxidant. ALA (alpha lipoic acid) rapidly and easily penetrates biomembranes of cells and organelles. Studies indicate that ALA supplements hold promise for treating various health problems, including glaucoma, and cataracts.

Alpha Lipoic Acid and Eye Therapy

Alpha lipoic acid is very strong antioxidant and this antioxidant effect is beneficial in improving eye conditions like cataract and glaucoma. An antioxidant combination, which includes alpha-lipoic acid, has been shown to deter cone and rod cell death in the eyes that are associated with seeing a spectrum of colors and light. A study revealed that the combination of alpha-lipoic acid and vitamin E helped prevent retinal cell death in animals with retinitis pigmentosa. ALA inhibited aldose reductase activity in the rat lens. The enzyme aldose reductase plays an substantial role in the development of cataracts in diabetes.


Cataracts are related with reduced antioxidant activity in the lens of the eye, and ALA is known to regenerate several important lens antioxidants, including glutathione. In vitro and animal-based study has shown that ALA can increase glutathione levels, as well as prevent cataract formation. Since alpha lipoic acid is both water-soluble and fat-soluble, it can get deep into the eye tissues and destroy free radicals that cause protein changes resulting in cataracts. L-buthionine (S,R)-sulfoximine is an inhibitor of glutathione synthesis, whose administration to newborn animals leads to the development of cataracts. An animal experiment; studied the effect of ALA, on cataract formation in L-buthionine (S,R)-sulfoximine (BSO)-treated newborn rats and found that a dose of 25 mg/kg bw protected 60% of animals from cataract formation.


Researches have shown that ALA can increase glutathione in red blood cells and lacrimal fluid of patients with glaucoma, and so, may hold some positive effect for treating glaucoma.  Some findings indicates that 150 mg of ALA, taken daily for one month, significantly improves visual function in patients with glaucoma. Forty-five patients with stage I and II open-angle glaucoma were administered either 75 mg of ALA for 2 months or 150 mg for 1 month. A control group of 31 patients were administered just local hypotensive treatment. The important improvement of biochemical parameters, visual function, and the coefficient of efficacy of liquid discharge was observed in the participants administered the higher dose of ALA.

How may Alpha Lipoic Acid Help Brain Function?

Alpha-lipoic acid  (also known as lipoic acid, thioctic acid, or ALA) is a powerful antioxidant that is capable of scavenging harmful free radicals from your tissues. Alpha-lipoic acid is one of the antioxidants that can pass the blood brain-barrier, which enables it to protect brain tissue and prevent free-radical damage. ALA may have a favorable effect on patients with Alzheimer’s disease and other types of memory dysfunction secondary to trauma or cerebral vascular accident.

Alpha Lipoic Acid Brain Benefits

ALA is a neuroprotective metabolic antioxidant that has been shown to cross the blood brain barrier. Animal studies have showed that brain functioning can be improved and that brain damage and deterioration can be lessened by therapy with ALA. Experiments have shown that ALA reduced brain damage after a stroke, and that those animals who received ALA had a survival rate three times greater than those that did not. A study in 2005 investigated whether ALA could have an effect on the antioxidant defense systems in the brains of rats fed arsenic on a daily basis. The rats were administered arsenic along with a dosage of ALA once daily for 60 days. Results demonstrated that deficits in antioxidant production and a rise in oxidation due to the ingestion of arsenic could be surmounted in rats when simultaneously treated with ALA.

Results from animal-based studies demonstrate that ALA may improve long-term memory. ALA has also been found to work synergistically with other compounds, particularly acetyl-L-carnitine to improve brain functioning in aged rats.Supplemented aged rats were found to perform as well as younger rats in memory and other tasks. Acetyl-L-Carnitine is a specific form of carnitine that has the ability to pass through the blood-brain barrier.

Alzheimer’s Disease

By decreasing oxidative damage in the central nervous system, alpha lipoic acid may reduce the severity of central nervous system disorders. ALA reduces amyloid-beta-induced inflammation and improves brain cells production of the chemical signaling molecules called neurotransmitters. A naturally occurring cofactor for the mitochondrial enzymes pyruvate dehydrogenase and alpha-ketoglutarate dehydrogenase, alpha lipoic acid has been shown to have a variety of effects which can interfere with the pathogenesis or progression of Alzheimer’s disease. For instance, alpha lipoic acid increases ACh (acetylcholine) production by activation of choline acetyltransferase and enhances glucose uptake, so supplying more acetyl-CoA for the production of acetylcholine. A 2001 small study of 9 Alzheimer’s patients found that supplement with Alpha-lipoic acid for 12 months resulted in a decrease in oxidative stress which led to a stabilization of cognitive function. A 2007 research in Journal of  Neural Transmission showed that high doses of Alpha-lipoic acid slowed Alzheimer’s progression to a greater degree than standard therapy.

Alpha Lipoic Acid and Multiple Sclerosis

Multiple sclerosis is an autoimmune disease of the central nervous system that has its symptom onset primarily in young and middle-aged adults. Damage to nerve cells as a result of free radicals is thought to be a important trigger for the autoimmune process. In multiple sclerosis, tests reveal the specific antibodies attacking the myelin cover of the nerve fibers. According to Dr. Lester Packer at the University of California in Berkeley, ALA may have a role in amyotrophic lateral sclerosis, multiple sclerosis, head injuries, and spinal cord damage.  Alpha-lipoic acid has been examined as an effective treatment in a rat model of multiple sclerosis and experimental autoimmune encephalomyelitis. Alpha-lipoic acid dose dependently prevented the development of clinical signs in this model.

Alpha-lipoic acid  has shown the ability to suppress and treat the animal model of multiple sclerosis, EAE (experimental autoimmune encephalomyelitis). MMP-9, is associated with disease activity in Multiple sclerosis. Alpha-lipoic acid  inhibits MMP-9 activity directly and at the level of transcription. In vitro , immunohistochemical staining of spinal cords from mice treated with alpha-lipoic acid revealed a decreased in the expression of adhesion molecules VCAM-1 and ICAM-1 from the surface of endothelial cells. In a study, 37 multiple sclerosis participants were given ALA 1200 mg a day for 14 days. Alpha lipoic acid  was able to lower levels of two markers for multiple sclerosis called  CAMP-1 and MMP-9. The scientists say, “ALA may prove useful in treating multiple sclerosis by inhibiting MMP-9 activity and interfering with T-cell migration into the CNS (central nervous system).

Alpha Lipoic Acid as an Liver Diseases Treatment

Alpha lipoic acid (ALA or thioctic acid), is a sulfur-containing fatty acid. ALA is frequently used in conjunction with milk thistle (silymarin) and selenium to help treat hepatitis. Also, along with milk thistle, ALA has  been used for therapy of Amanita phalloides poisoning. In Europe, it has long been used in the therapy of hepatic disorders because of its liver-sparing properties which can help the liver repair.

Alpha Lipoic Acid Liver Benefits

ALA has proved to help with fatty liver disease, hepatitis, cirrhosis and elevated liver enzymes. Intravenous forms of ALA are administered in hospitals to treat cases of acute mushroom poisoning and for other conditions of acute poisoning that affect the liver. Its combined usefulness in repairing the liver and working as an antioxidant has led to its extensive use in Europe for radiation sickness, medication poisonings, and chemical overdoses.

Alpha lipoic acid was used in the 1970s as a therapy for various forms of hepatitis. The scientists administered ALA intravenously to 79 people with acute and serious liver damage at medical centers across the United States, and 75 recovered full liver function. In a study, published in a 2008 issue of “Hepatology“, determined that Alpha-lipoic acid prevented fatty liver disease and may be used to prevent nonalcoholic fatty liver disease in insulin-resistant patients. Amanita is a extremely poisonous mushroom that causes liver damage. In the Amanita phalloides, amatoxins block the production of  DNA, which causes cell necrosis particularly in those areas that first interact with the toxins and have a high rate of degeneration, like the liver and kidneys. The first symptoms of Amanita posioning appear 6 to 24 hours after ingestion. For 12 to 24 hours, the patient will have abdominal pain, nausea, vomiting, and diarrhea. ALA infusions were used in the therapy of amanita mushroom poisoning in 75 patients between 1974 and 1978. Normally, up to 50% of patients recover without intervention; but, 89 % recovered after ALA infusion.

This combination of alpha lipoic acid, silymarin, and selenium replenishes glutathione stores, promotes liver cell regeneration, and puts the brakes on viral replication. One study by Dr. Bert Berkson has shown efficacy for ALA as part of a combination “triple antioxidant” treatment for hepatitis C with liver failure. Dr. Berkson has utilized an antioxidant protocol consisting of alpha-lipoic acid 300mg, twice a day; oral selenium, 200 mcg, twice a day; and oral silymarin, 300 mg per day. Dr. Berkson reported his triple-antioxidant protocol in 1999, in the content of a pilot study involving 3 patients with cirrhosis, portal hypertension, and esophageal varies related to HCV. All 3 were candidates for liver transplant. After a year on Alpha lipoic acid, silymarin, and selenium, all were healthy, demonstrated improved hepatic function. (Also to the alpha-lipoic acid, selenium and silymarin, Dr. Berkson recommends a B vitamin complex because high dose alpha-lipoic acid will deplete thiamine, niacin and riboflavin.)

Role of Alpha Lipoic Acid in the Treatment of Neuropathy

Alpha lipoic acid (ALA or thioctic acid), is a sulfur-containing molecule that is synthesized in body from a fatty acid called octanoic acid. The primary established use for alpha-lipoic acid is the therapy of diabetic neuropathy. Nerve damage from diabetes is called diabetic neuropathy. There are 4 types of diabetic neuropathy: peripheral, autonomic, focal, and proximal. When occurring in the extremities, neuropathy can lead to pain, tingling, and numbness. Diabetic neuropathy results as a consequence of harm to nerves caused by periods of high blood sugar. High blood sugar can injure nerve fibers throughout your body, however diabetic neuropathy typically damages nerves in your legs and feet.

Alpha Lipoic Acid Diabetic Peripheral Neuropathy Treatment and Studies

ALA is a strong lipophilic free radical scavenger of peripheral nerve both in vitro and in vivo. ALA protects nerves through its antioxidant properties, which improve blood flow to nerves and helps maintain rapid nerve conduction speed. Diabetic peripheral neuropathy is one of the most common and painful complications of diabetes. For patients suffering from peripheral neuropathy, alpha-lipoic acid may help to alleviate pain, itching and numbness. Generally, the available research demonstrates that therapy with 600 mg/day of intravenous alpha lipoic acid for 3 weeks significantly reduces the symptoms of diabetic peripheral neuropathy. Oral and Intravenous (IV) alpha-lipoic acid has been used for years to treat peripheral neuropathy in Germany.

A review in the Apr 2010 edition of  The Netherlands Journal of Medicine showed that ALA, when administered either intravenously or orally at a dosage of 600 mg daily, led to important diminution in pain among people suffering from diabetic neuropathy. A Romanian study of 26 participants found symptomatic healing with oral alpha lipoic acid (600mg daily) after 3 months. In a study, oral with 1,200 mg/day of Alpha-lipoic acid for 6 weeks improved a measure of capillary perfusion in the fingers of eight diabetic patients with peripheral neuropathy.

A randomized, double-blind, placebo-controlled study in 181 patients with diabetic neuropathy found that oral with 600 mg/day, 1,200 mg/day, or 1,800 mg/day of alpha-lipoic acid for 5 weeks significantly improved neuropathic symptoms. In this study, the 600 mg/day dose was as effective as the higher doses. Taking alpha-lipoic acid may help other diabetes-related problem called autonomic neuropathy. One study found that seventy-three people with cardiac autonomic neuropathy, which affects the heart, demonstrated fewer signs of the condition when taking 800 mg of ALA orally compared to placebo.

ALA provided significant symptom improvement and delay in the progression of neurologic deficit in patients with diabetic neuropathy in the 4-year NATHAN study. Scientists have suggested that a decrease in the symptoms of diabetic neuropathy secondary to a reduction in oxidative stress may be a potential mechanism of action consistent with the antioxidant effect of ALA. In the Feb 2004 edition of Diabetic Medicine, scientists explain their meta-analysis of clinical findings on the intravenous therapy of diabetic neuropathy with thioctic acid. Their examination shows that a therapy regimen consisting of an intravenous dose of 600 mg of lipoic acid per day for 3 weeks significantly reduces the symptoms of diabetic neuropathy. Dr. Dan Ziegler’s team at the German Diabetes Clinic has performed a number of trials in people with type 2 diabetes trying to determine optimal doses of alpha lipoic acid for diabetic neuropathy. The Alpha-Lipoic Acid in Diabetic Neuropathy Study found important effect in using intravenous alpha lipoic acid for a period of 3 weeks, with an therapeutic dose of 600 or 1200mg daily.