Monday, June 4, 2007

Alpha-Lipoic Acid - Anti-aging with a Big Asterisk

At the recent “Diet and Optimum Health” conference sponsored by the Linus Pauling Institute (LPI) at Oregon State University, scientists presented research discussing some of the underlying mechanisms behind lipoic acid’s many beneficial effects.
“The evidence suggests that lipoic acid is actually a low-level stressor that turns on the basic cellular defenses of the body, including some of those that naturally decline with age,” said Tory Hagen, an LPI researcher and associate professor of biochemistry and biophysics at OSU. “In particular, it tends to restore levels of glutathione, a protective antioxidant and detoxification compound, to those of a young animal. It also acts as a strong anti-inflammatory agent, which is relevant to many degenerative diseases.” …
… “Our studies have shown that mice supplemented with lipoic acid have a cognitive ability, behavior, and genetic expression of almost 100 detoxification and antioxidant genes that are comparable to that of young animals,” Hagen said. “They aren’t just living longer, they are living better — and that’s the goal we’re after.”
Sound promising? Sure.
But there are a few things you should know about lipoic acid before running out and buying it. In fact, without a proper dosing protocol, some people may want to avoid supplementing with it entirely.
What is Lipoic Acid
Lipoic acid is a compound that contains two sulfur, or thiol, groups. The oxidized form is referred to as lipoic acid (LA), while the reduced form is called dihydrolipoic acid (DHPLA).

Sources of Lipoic Acid
Lipoic acid (LA) is generated in small amounts inside the body, specifically in mitochondria, the energy production factories inside cells. It can also be obtained from plant and animal food sources. For example, spinach, broccoli, kidney, heart, and liver are all relatively high in LA. Supplements, however, provide LA in amounts much greater (as much as 1000 times or more) than those that can be obtained via food.
Functions of Lipoic Acid
LA appears to have many important biological functions in the body, including:
Serving as an enzyme cofactor in many important chemical reactions in the body. For example, LA is one of the cofactors in the pyruvate dehydrogenase complex, which converts pyruvate into acetyl-CoA to be used in the body’s primary energy production pathway, the Krebs (citric acid) cycle.
Acting as an antioxidant. Both LA and DHLA appear to neutralize oxygen and nitrogen free-radicals (unstable molecules that can cause damage to cells and tissues). Importantly and unlike most other antioxidants, LA is both fat- and water-soluble, which means it can help to reduce free-radical damage in fatty structures (e.g., cell membranes, mitochondria) and in aqueous areas (e.g., cell cytosols, extracellular spaces).
Regenerating other antioxidants. DHLA can restore important antioxidants, including vitamin C and glutathione, to their reduced forms. It also helps restore vitamin E in the body, possibly directly, and definitely indirectly by restoring vitamin C, which can in turn restore vitamin E.
Boosting glutathione levels. Glutathione, made from the three amino acids cysteine, glycine, and glutamic acid, is the body’s primary internally generated antioxidant and a key detoxification compound.
Metal chelation. Because of its di-thiol (two sulfhydryl group) structure, LA has a very high affinity for certain metals in the body, especially toxic metals such as mercury, arsenic, and possibly lead. LA chelates (binds to) these metals, and if a proper chelation protocol is used, can help to reduce the overall level of them in the body.
Regulating a variety of insulin and cell signaling processes that help to control insulin sensitivity, metabolism, and stress response. Also regulates expression of genes related to physiologic processes, such as inflammation and cell cycle control, which may, in turn, affect the risk for many conditions, including diabetes, heart disease, and cancer.
Conditions Treated with Lipoic Acid
As the research discussed at the LPI conference suggests, there are many conditions that may benefit from lipoic acid (LA), including:
Diabetes - may help to improve insulin sensitivity and reduce blood glucose levels
Heart disease - may improve blood vessel condition and function
Neuropathy - may reduce diabetic peripheral neuropathy symptoms and complications
Cognitive decline & dementia - may help to prevent and/or slow the development of these conditions
There’s a good overview of the LA research linked to these different conditions in this LPI Micronutrient Center LA review article.
Caveats, Including A Big One
Some research suggests that lipoic acid (LA) may compete with biotin for transport across cell membranes and reduce the activity of biotin-dependent enzymes. Thus, biotin supplementation may be a good idea if supplementing with LA.
But by far the biggest potential caution with LA usage relates to its potential for interacting with heavy metals in the body. As mentioned above, LA contains two sulfur groups that help LA to chelate (bind to) toxic metals, such as mercury. Although LA is naturally present in all cells of the body, if you added it all up, the total amount in your body would actually be quite small (a few milligrams).
The risk with taking large supplement doses of LA infrequently (e.g., 50 to 200 mg, or more, 2 or 3 times a day) is that such a dosing protocol doesn’t take into account the metabolism of LA in the body. Specifically, LA has an average half-life in the body of 3 hours, which means half of it is still present 3 hours after taking a dose. That means that in order to keep LA levels relatively constant in the bloodstream, you need to take it every 3 hours.
Why would you want to keep LA blood levels constant?
Because if you have had any significant exposure to toxic metals (e.g., mercury via amalgams*, vaccines, or high fish consumption), by taking LA in doses spaced farther apart than 3 hours, the toxic metals will be repeatedly picked up and dropped as the LA blood levels rise and fall. In turn, the metals will be redistributed in the body and continue to cause damage to cells and tissues in new locations. Not good. Instead of getting the beneficial effects of LA mentioned earlier in this post, you may cause much more damage.
And since LA can cross the blood-brain barrier, if you use it in large doses with an infrequent dosing schedule, you run the risk of carrying toxic metals into the brain.
*You certainly would never want to take LA supplements if you currently have mercury fillings, as that would accelerate the movement of mercury from the fillings into the body.
Bottom Line
If you haven’t been exposed to significant amounts of toxic metals and your overall body levels are low, then using LA will likely cause no problems and may have considerable benefits.
However, if you have had significant toxic metal exposure (e.g., amalgam fillings in place for many years, multiple mercury-containing vaccines, high fish consumption), you want to avoid high/infrequent LA doses and only use LA as part of a careful low/frequent-dose chelation protocol.
LA can be an effective chelator if used in the latter way. Unlike other chelators DMSA and DMPS, LA can go both inside cells and into the brain to chelate and remove toxic metals.
The concept of low/frequent-dose chelation using DMSA, DMPS, and LA was pioneered by Andrew Cutler, PhD, and is described in detail in his book, Amalgam Illness: Diagnosis & Treatment.
In my nutritional consulting practice, I help people to implement this safe and effective chelation approach (and successfully used it myself to recover from mercury poisoning). If you’d like help, you can find out more here.
Related Posts
Advisory Panel Rejects FDA Safety Report on Mercury Fillings
3/4 of Public Unaware that Flu Shots Contain Mercury
Dementia and Alzheimer’s Disease Affecting More People at Younger Ages
Date: June 4, 2007
By: Marc Joseph

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