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Alpha-lipoic acid (ALA) is a unique, vitamin-like antioxidant that can combat radiation sickness, repair damaged livers, treat diabetes and diabetes-related conditions (polyneuropathy) and protect against oxidative processes that promote premature aging and degenerative diseases. ALA is becoming increasingly recognized as a ‘mitochondrial antioxidant.’ Now a more potent form of ALA – R-lipoic acid – is available to health consumers. Research shows that (R)-lipoic acid is a more biologically active form of ALA that offers greater antioxidant and neuroprotective benefits at substantially lower doses than the synthetic forms of lipoic acid currently available.
Water and Fat Soluble Antioxidant
Although lipoic acid is produced naturally in the body, researchers were virtually unaware of its existence until the 1930s. When pure samples were isolated in the 1950s, ALA was first believed to be a new vitamin. Later, researchers discovered that ALA is, in fact, an essential coenzyme with a vital role in mitochondrial electron transport reactions involved in converting glucose into ATP to produce energy. By 1988 researchers had also learned that ALA is a powerful biological antioxidant, although one with some very unique health properties. What most impressed researchers was the discovery that ALA functions as both a fat and water-soluble antioxidant that can easily cross cell membranes. Thus, ALA can confer free radical protection to both interior and exterior cellular structures.
Regenerating Vitamins E and C
Human aging is marked by a decline in the concentration, synthesis and recycling of central antioxidants, such as vitamin E, vitamin C, co-enzyme Q-10 and glutathione. This loss of antioxidant function seriously impairs the body’s ability to control free radicals. Left unchecked, free radicals – dangerous, unpaired electrons – proliferate throughout the body, damaging cell membranes and organs, impairing immune function, disrupting DNA strands and contributing to the progression of cancer and other degenerative diseases. In recent years researchers have shown how alpha-lipoic acid recycles vitamins E and C to stave off free radical damage.
One of the central components in the antioxidant cycle is vitamin E, a potent biological antioxidant that works to stabilize highly reactive free radicals in lipid (fatty) tissues and membranes (lipoproteins). In the process of quenching fatty free radicals, such as lipid peroxyl and lipid alkoxyl radicals, vitamin E becomes a free radical itself, though one that is far less reactive or damaging than the original radical.
The vitamin E radical is then regenerated by vitamin C (ascorbic acid). This process recycles vitamin E from a radical back into an antioxidant again, but results in the formation of a new free radical in the form of unstable vitamin C – a semiascorbyl radical. Vitamin C is next recycled by glutathione, a thiol (sulfur-containing compound). Up to this point vitamins E, C and glutathione work in concert to control free radicals and prevent cellular damage. But this is also an important stage where the antioxidant regeneration cycle runs into a limiting factor determined by the availability of glutathione.
Glutathione
Glutathione is the most important member of the thiol group and the body’s primary intracellular antioxidant. In addition to being an important free-radical deactivator, glutathione also plays a vital role in protecting against cataract formation, enhancing immune function, preventing liver damage, slowing the initiation of cancers and eliminating heavy metals. Glutathione is quickly depleted when the body experiences high levels of oxidative stress from causes such as illness, infection, trauma, medication or surgery. Glutathione deficiency is also associated with low protein intake, diabetes, liver disease, cataracts, HIV infection, respiratory distress syndrome, cancer, and idiopathic pulmonary fibrosis.
ALA Boosts Glutathione Levels
Dr. Lester Packer, senior scientist at Lawrence Berkeley Laboratory and head of the Packer Lab at the University of California, has spent over 35 years studying how antioxidants like vitamins C, E and glutathione interact in the body. Dr. Packer first discovered several years ago how vitamin E is ‘recycled’ by vitamin C.
Despite their detailed understanding of the antioxidant regeneration cycle, when Dr. Packer and other researchers tested methods for boosting antioxidant levels they ran into a problem when attempting to increase cellular glutathione levels. Whereas increasing one’s intake of dietary or supplemental sources can readily elevate levels of vitamins E and C, cellular glutathione is only produced in the body.
Glutathione, when taken orally, is broken down in the stomach before reaching the bloodstream. What does end up being absorbed can raise serum levels, but the effect inside of cells is minimal.
This problem was solved when Packer and his team turned to ALA. ‘Alpha-lipoic acid proved to be the missing link,’ Packer said. They discovered that in addition to being a powerful antioxidant in its own right, ALA is able to raise intracellular glutathione levels. ALA is easily absorbed when taken orally, and once inside cells it is quickly converted to its most potent form, dihydrolipoic acid, an even more potent free-radical neutralizer. Because both alpha-lipoic acid and dihydrolipoic acid are antioxidants, their combined actions give them greater antioxidant potency than any other natural antioxidant now known.
The Most Potent Antioxidant
According to Dr. Packer, ALA is more potent than vitamins C and E, and CoQ10, and may, in fact, be the most important antioxidant ever discovered. “The therapeutic potential of alpha-lipoic acid is just beginning to be explored,’ observed Packer, ‘but this compound holds great promise.”
ALA also is important in cell metabolism and is required for production of energy inside cells. Without ALA, cells could not metabolize sugars for energy and would just shut down. This makes alpha-lipoic acid a metabolic antioxidant, able to draw on the cell’s own metabolism to magnify its protective effects and that of other antioxidants.
Experiments carried out by Dr. Packer and colleagues suggest that ALA may also have much broader use in treating other diseases and may have general health benefits when taken as a daily supplement like other antioxidants. ‘Alpha-lipoic acid could have far-reaching consequences in the search for prevention and therapy of chronic degenerative diseases such as diabetes and cardiovascular disease,’ stated Dr. Packer. ‘And because it’s the only antioxidant that can easily get into the brain, it could be useful in preventing damage from a stroke.’
(R)-Lipoic Acid More Effective
Natural ALA, referred to as R-lipoic acid or (R)-ALA, is found in exceedingly miniscule amounts in animal and plant tissues, tightly bound to mitochondrial complexes. Because of the extreme difficulty (and high cost) of isolating natural (R)-ALA, researchers in the US and Europe originally conducted studies with synthetic lipoic acid. Unlike natural (R)-ALA, synthetic lipoic acid contains a 50/50 mixture of two forms (enantiomers) called (R)-ALA and (S)-ALA. Both (R)- and (S)- forms of ALA are isomers – essentially mirror-image molecular formulas, with the atomic arrangements reversed.
Working with synthetic ALA, researchers were able to gain valuable insights into its role as a coenzyme in mitochondrial energy production, and an antioxidant and antioxidant-recycling nutrient. They then began to map out the impressive range of protective health benefits conferred by supplemental ALA. In time researchers had access to pure samples of the natural, biological version, (R)-ALA. They quickly learned that while the body can utilize both forms of ALA, there is a strong preference for the natural, more biologically active (R) form. For example, researchers in Germany reported that, unlike the natural form, (S)-ALA does not improve ATP synthesis in isolated cells. Furthermore, the R-form increased membrane fluidity and transport, while the S-form tended to decrease fluidity.
R-lipoic acid is the biologically active form of the key ‘mitochondrial antioxidant,’ alpha lipoic acid. R-lipoic acid is directly involved in cellular metabolism and is a vital component of the intracellular antioxidant cycle, able to scavenge a variety of free radicals and reactive oxygen species (ROS) while recycling vitamins C, E and glutathione. R-lipoic readily crosses the blood brain barrier and has been shown effective for elevating intracellular glutathione levels. R-LA helps regulate neuronal calcium homeostasis, regulates pro-inflammatory cytokines, and alters the expression of ‘toxic genes.’ R-lipoic acid has been used to treat diabetes and has been recommended as a “neuroprotective agent.” Because R-lipoic is the naturally occurring form found in mitochondrial complexes it offers substantially greater antioxidant and neuroprotective benefits at substantially lower doses than the synthetic forms of lipoic acid currently available.
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Alpha Lipoic Acid: Improve Insulin Sensitivity and Fight Diabetes!
What is it about foods like broccoli and spinach that make them so healthy? There’s the fiber, vitamins and minerals, of course, but then there’s other important chemical compounds we call “antioxidants,” too — like alpha lipoic acid (ALA).
Chances are you’ve heard a lot about the many benefits of various antioxidants and high-antioxidant foods — fighting inflammation, helping beat cancer or heart disease, warding off depression and cognitive decline, and so much more — but have you ever wondered what exactly antioxidants are and how they work in the body?
Alpha lipoic acid — one kind of antioxidant — is a type of compound found in plant foods we commonly eat that scavenges free radicals, fights inflammation and slows the aging process. But perhaps its most famous use is in treating diabetes naturally.
Humans also make a small amount of ALA on their own, although the concentration in our bloodstreams goes up substantially when we eat a healthy diet. Naturally abundant in foods like green veggies, potatoes and certain types of yeast, lipoic acid is similar to a vitamin in that it can also be man-made in a lab so it can be taken as an anti-inflammatory supplement (which is then called alpha lipoic acid).
What Is Alpha Lipoic Acid?
Lipoic acid is found in the body and also synthesized by plants and animals. It’s present in every cell inside the body and helps turn glucose into “fuel” for the body to run off of. Is it “essential” that you consume a certain doseage of alpha lipoic acid every day? Not exactly.
Even though we can make some of it on our own without supplements or outside food sources (which is why it’s not considered an “essential nutrient”), eating an antioxidant-packed diet plus potentially using ALA supplements can increase the amount circulating in the body, with studies show has far-reaching benefits.
ALA’s most valuable role in the body is fighting the effects of free radicals, which are dangerous chemical-reaction byproducts that form during the process of oxidation. Within our cells, ALA is converted into dihydrolipoic acid, which has protective effects over normal cellular reactions.
As oxidation takes place in the body over time — due to normal chemical reactions like eating or moving, but also from exposure to environmental pollutants and toxins — certain compounds can become very reactive and damage cells. At times, this causes abnormal cells to grow and multiply, or it can have other effects like slowing metabolic efficiency and changing neuron signaling.
Like other antioxidants, alpha lipoic acid can help slow down cellular damage that is one of the root causes of diseases like cancer, heart disease and diabetes. It also works in the body to restore essential vitamin levels, such as vitamin E and vitamin C, along with helping the body digest and utilize carbohydrate molecules while turning them into usable energy.
In addition, alpha lipoic acid works like a synergist with B vitamins, which are needed for turning all macronutrients from food into energy. And it’s synthesized and bound to protein molecules, making it act as a cofactor for several important mitochondrial enzymes.
Something that makes ALA unique is that it’s both water-soluble and fat-soluble, unlike other nutrients (like B vitamins or vitamin A, C, D or E), which can only be properly absorbed with either one or the other.
There’s some evidence that ALA is acts as a “heavy metal chelator,” binding to metals (also called “toxins”) in the body, including mercury, arsenic, iron and other forms of free radicals that make their way into the bloodstream through water, air, chemical products and the food supply.
Finally (as if this wasn’t enough!), alpha lipoic acid can increase how the body uses a very important antioxidant known as glutathione, and it might increase energy metabolism too — which is why some athletes use ALA supplements for enhanced physical performance.
Health Benefits
Because it acts like an antidote to oxidative stress and inflammation, alpha lipoic acid seems to fight damage done to the blood vessels, brain, neurons, and organs like the heart or liver. This mean it offers numerous benefits throughout the whole body, from naturally treating Alzheimer’s disease to controlling liver disease.
Because ALA isn’t an official essential nutrient, there hasn’t been an established daily recommendation needed to prevent a deficiency. However, being low in antioxidants in general can speed up in the aging process, resulting in symptoms like a weakened immune function, decreased muscle mass, cardiovascular problems and memory problems.
Here are five ways that including more alpha lipoic acid in your diet (and for some people taking supplements too) can help keep you feeling young and healthy:
1. Fights Diabetes and Diabetic Complications
Because alpha lipoic acid can protect cells and neurons involved in hormone production, one benefit is it offers protection against diabetes. ALA is considered an effective drug in the treatment of diabetic distal sensory-motor neuropathy, which affects about 50 percent of people with diabetes.
In dietary supplement form, ALA seems to help improve insulin sensitivity and might also offer protection against metabolic syndrome — a term given to a cluster of conditions like high blood pressure, cholesterol and body weight. Some evidence also shows that it can help lower blood sugar levels.
ALA is used to help relieve complications and symptoms of diabetes caused by nerve damage, including numbness in the legs and arms, cardiovascular problems, eye-related disorders, pain, and swelling. That’s why it should be part of any diabetic diet plan to treat this common disorder. People who experience peripheral neuropathy as a side effect of diabetes can find relief from pain, burning, itching, tingling and numbness using ALA, although most studies show that high doses in IV form are most effective as opposed to eating ALA-rich foods.
A major benefit of alpha lipoic supplementation in diabetics is the lowered risk for neuropathic complications that affect the heart, since around 25 percent of people with diabetes develop cardiovascular autonomic neuropathy (CAN). CAN is characterized by reduced heart rate variability and is associated with an increased risk of mortality in people with diabetes.
Research suggests that supplementing with 600 milligrams a day of ALA (or “LA” as it is sometimes called) for three weeks significantly reduces the symptoms of diabetic peripheral neuropathy, although some doctors choose to use doses up to 1,800 milligrams a day safely in their patients under supervision.
2. Preserves Eye Health
Oxidative stress can damage nerves in the eyes and cause vision problems, especially in people with diabetes or older adults. Alpha lipoic acid has been used successfully to help control symptoms of eye-related disorders, including vision loss, macular degeneration, retina damage, cataracts, glaucoma and Wilson’s disease.
Results from certain studies demonstrate that long-term use of alphalipoic acid has beneficial effects on the development of retinopathy since it halts oxidative damage that can result in modified DNA in the retina. As people age, their vision becomes much more compromised, which is why it’s important to eat a nutrient-dense diet well before old age to prevent degeneration of eye tissue or vision loss early on.
3. Prevents Memory Loss and Cognitive Decline
We know that a nutrient-dense diet filled with various colorful “brain foods” helps protect memory. Some health care professionals use alpha lipoic acid supplements to further help prevent their patients from experiencing neuron damage, memory loss, motor impairment and changes in cognitive functioning because of it antioxidant activity.
ALA seems to easily make its way into the brain by passing the blood-brain barrier, where it can protect delicate brain and nerve tissue. It’s also used to prevent strokes and other brain problems, including dementia in older adults.
Recent experiments using rats have shown that ALA can help reverse the damage in aging cells of the brain, improve performance in memory tasks, lower oxidative damage and improve mitochondrial function, although we still don’t know how well these benefits can apply to aging humans.
4. Helps Boost Glutathione
Glutathione is considered the “master antioxidant” by many experts, since it’s crucial for immunity, cellular health and disease prevention. Some studies have found that 300–1,200 milligrams of alpha lipoic acid helps increase the ability of glutathione to regulate the body’s immune response and fight off diseases like diabetes/insulin resistance or even HIV/AIDS.
In adults, supplementation with alpha lipoic acid seems to positively impact patients with immune deficiency syndromes and serious viruses by restoring blood total glutathione levels and improving functional reactivity of lymphocytes to T-cell mitogens.
5. Might Help Protect Skin from Damage
When it comes to battling physical signs of aging on the skin, certain studies have found that topical treatment creams containing 5 percent alpha lipoic acid can help reduce fine lines caused by exposure to sun ways. Skin damage is one side effect of high amounts of free radicals, which is why antioxidant-packed fruits and veggies are said to keep you looking young.
Best Sources
The best way to get any nutrients is ideally through real food sources, since this is how your body knows how to absorb and use various chemicals best. ALA is found in many different plant and animal sources, since it’s bound to protein molecules (especially lysine).
The concentration of ALA in different foods can vary widely depending on where they’re grown, the quality of the soil, how fresh they are and how they’re prepared, so it’s hard to quantify how much is in each type of food. There hasn’t been much research done to draw conclusions about how much ALA is found in particular foods, although we know vegetables and certain organ meats seem to be highest.
That being said, when you eat a whole food-based diet and vary the types of things you eat, chances are you consume a decent amount in addition to what your body already makes on its own.
Here are some of the best food sources of alpha lipoic acid:
- • Broccoli
- • Spinach
- • Red meat
- • Organ meat (sch as liver, hearts, kidneys from beef or chicken)
- • Brussel sprouts
- • Tomatoes
- • Peas
- • Brewer’s yeast
- • Beets
- • Carrots
Dosage
If you do choose to take ALA supplements, keep in mind that taking more won’t always offer better results. While side effects and risks of taking more seem to be very rare (considering it’s a natural chemical found in the body at all times), as little as 20–50 milligrams per day seems to be beneficial for general preventative health. Larger doses up to 600–800 milligrams per day are sometimes used in patients with diabetes or cognitive disorders but not recommended for the general public.
Dosage recommendations differ depending on who you ask, but below are some general guidelines that are within the safe range:
- • 50–100 milligrams for antioxidant purposes in generally healthy adults
- • 600–800 milligrams for patients with diabetes (divided into two doses, usually tablets are 30–50 milligrams each)
- • 600–1,800 milligrams for patients with neuropathy and diabetic neuropathy (dosages this high should only be taken with supervision from a doctor)
According to researchers from Oregon State University, the amounts of lipoic acid available in dietary supplements (ranging in dosage from 200–600 milligrams) can be as much as 1,000 times greater than the amounts that could be obtained through someone’s diet alone! Taking ALA supplements with a meal is believed to decrease its bioavailability, so most experts recommend taking it on an empty stomach (or at least one hour before or after) for the best results.
Side Effects
Alpha lipoic acid supplements haven’t been studied in children or women who are pregnant or breastfeeding, so right now it’s intended for use in adults only.
Side effects of ALA in supplement form are generally rare but for some people can include: insomnia, fatigue, diarrhea, skin rash or low blood sugar levels (especially in people with diabetes or low blood sugar who are taking medications).
Drug Interactions
Some potential interactions, or circumstances where you want to speak to your doctor before taking extra alpha lipoic supplements, include:
- • if you have a thiamine deficiency (vitamin B1), which is associated with liver disease/alcohol abuse
- • if you’re taking any medications for diabetes for insulin control, since this can raise the risk for hypoglycemia and low blood sugar
- • if you’re recovering from chemotherapy treatment or taking cancer medications
- • if you have a history of a thyroid disorder
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