Alpha Lipoic Acid (ALA).

You may see this called just lipoic acid, lipoate or thioctic acid - it is all the same thing.

ALA is a vitamin-like sulphurous fatty acid. I say vitamin-like because a vitamin is micronutrient that cannot be made by the body and has to be obtained from a different source. ALA on the other hand is made by the body in small amounts.

I will give a very brief summery of it's actions here and go into them in greater depth later.

The links below will take you directly to those sections of the page if you so wish, but we do suggest that you read down from the top on your first visit to get the complete view.

ALA and it's role in converting glucose to energy.
Alpha Lipoic Acid as an antioxidant.
To clarify what I mean by 'free radical'.
Why ALA is so important as an antioxidant.
Where do we get ALA from naturally?
Supplements and R-ALA vs S-ALA.
Where can I get R-ALA?
ALA and Diabetes.
ALA and Congestive heart failure (CHF).
ALA and Neuropathy (nerve damage).
ALA and your liver.
ALA also chelates (binds) to heavy metals.
ALA can minimise the side-effects of treatments such as x-rays and radiation.
ALA and Glaucoma.
ALA and Cataracts.
So how much ALA does one need?
Side effects of Alpha Lipoic Acid.
Some interesting websites.

It has been called unique, essential, a master nutrient and it is easy to see why. It plays a crucial role in a number of metabolic processes, such as breaking down amino acid chains for protein synthesis and the generation of energy in the form of ATP (adenosine triphosphate)

In simple terms it helps turn glucose into the energy your body needs to function.

But it has yet another property, it is an incredibly effective antioxidant, helping rid the body of those damaging free radicals and thus protecting the cells from damage.

We have a number of antioxidants in our bodies but ALA is special, as you will see later.

It also works as a liver purifier, or cleanser, maintaining a healthy liver and sometimes even rectifying liver problems. For an amazing article on this see

Be a `liver lover' with alpha-lipoic acid Better Nutrition, July, 2000 by Burt Berkson

It increase glutathione levels. Glutathione is one of the chief antioxidants produced directly by the body which help dissolve toxic substances in the liver.

It increases insulin sensitivity, the efficiency of the insulin and the uptake of glucose.

It improves diabetic polyneuropathy.

It also helps to reduce glycation; in other words, the damage that sugar does to our body, including accelerated ageing.

It can help prevent coronary heart disease.

ALA and it's role in converting glucose to energy.

First we need to understand where our energy comes from. Our body is made up of trillions of separate cells that each contain a little factory that produces energy - these factories are called mitochondria.

Glucose and fats are the raw ingredients that enter the factory, which then processes them into adenosine triphosphate (ATP), the chemical that the body uses as energy, in much the same way as coal enters a factory and is converted into electricity which we use as a source of energy in our houses.

Just as one needs the machinery involved in the process of converting coal to electricity to work, so the body needs the enzymes involved in ATP production to work properly and this is where ALA comes in - it helps by activating these enzymes, which is why it is referred to as a coenzyme, (a substance that must be available in order for another substance to work properly.

If this energy conversion does not work properly less glucose is 'burnt' so it builds up in the bloodstream, leading to hyperglycemia.


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ALA as an antioxidant.

An antioxidant is a substance that protects the body from damage caused by oxidative free radicals by binding to the free electron of the free radical and so neutralising it.

It is no wonder they are often called free radical scavengers.


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To clarify what I mean by 'free radical' -

A molecule usually contains pairs of electrons, which keeps it stable and gives it a positive charge. However chemical reactions can break the bond that holds those paired electrons together.

When that occurs a free radical is produced.

The molecule now has an odd number of electrons which makes it very reactive, extremely unstable and negatively charged.

As molecules like to be stable the free radical will steal an electron from, or donate an electron to, another molecule as soon as it can, which means that that molecule is now a free radical, and so a chain reaction is set up.

The danger here is that this can create new substances that are harmful to the body and can also affect the proper working of the immune system.

Not all free radicals are dangerous, we actually need some free radicals as they can produce vital hormones and fight bacteria and viruses.

However oxidative free radicals are not good.

The body uses oxygen when it processes our food and during this metabolic process a type of free radical is produced that is actually an oxygen molecule with unpaired electrons. This is a particularly destructive variety of free radical and the process that produces it is known as oxidation.

They are usually balanced by antioxidants which end the chain reaction before important molecules are harmed.

An imbalance between antioxidants and oxidative free radicals leads to what is known as oxidative stress.

We diabetics experience oxidative stress because high glucose levels compromise our levels of antioxidants.

When, for some reason, too many free radicals are formed, the antioxidants are overwhelmed and cell damage can occur.

Free radicals are responsible for membrane damage which plays a part in cardiovascular disease and the fragility of capillary walls. Cataracts are created when free radicals damage proteins, and we age faster (and wrinkle more!!) when they cause a breakdown of elastin and collagen.

There are a number of factors responsible for the creation of these extra free radicals.

Common ones are the exposure to environmental pollutants like tobacco smoke and car exhausts and chemical pollutants like pesticides and those found in many of our normal household cleaners. Also over exposure to the sun.

Then there are the slightly less common ones like radiation exposure.

But topping the list is our 'normal' diet, in which the word normal refers to 'usually eaten', not 'healthy'. Our modern western diet contains types of fat that significantly increase the formation of oxidative radicals - oxidation occurs more readily in fat molecules than in carbohydrates or proteins. Heating these fats increases the problem, and we do love our fried foods don't we?

Alcohol is another substance that increases free radical production. So the common meal of steak, chips and a cold beer is a recipe for disaster!


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Why ALA is so important.

Alpha lipoic acid's claim to fame, and why it is called a universal antioxidant, is it's versatility.

It is able to dissolve, and therefore work, in both fatty and aqueous (watery) parts of the body, which means it can work within and outside the cell.

Other powerful antioxidants are only soluble in fat, i.e. Vitamin E, or in water i.e. Vitamin C so where they can work is limited. Vitamin E is usually found in the fatty portion of cell membranes while vitamin C is found in the interior of cells and the watery parts of the blood.

ALA is the only known antioxidant that can easily get into the brain, so it is not surprising that it is being used to treat Alzheimer patients.

ALA is particularly protective of the DNA and mitochondria, and it is in the mitochondria that the main 'fat burning' takes place with the concurrent release of oxidative free radicals.

Most antioxidants, in their action of dealing with free radicals, have to pass onto that free radical one of their own electrons or accept an electron from the free radical and this in turn makes them free radicals themselves.

This may seem a somewhat pointless exercise but the advantage is that the free radicals formed from the antioxidants are less reactive and thus less destructive than those they have just dealt with.

However, ALA is different.

Antioxidants are either in reduced or oxidised forms. In their reduced form they have an extra electron to give. Once they have given that extra electron to a free radical they return to their oxidised form.

Most antioxidants can only function as such when in their reduced form, but ALA can work as an antioxidant in both it's oxidised and it's reduced form.

Inside the cell alpha lipoic acid is broken down by enzymes or free radicals into the reduced form, known as dihydrolipoic acid, which is an even more potent antioxidant.

And as if that was not enough it can regenerate, or recycle, and so extend the useful life of the antioxidants vitamin C, glutathione, and coenzyme Q10, and also, indirectly, vitamin E, making them available antioxidants again - it truly is an amazing substance.

Note -

I have found myself, in the attempt to discribe and understand the workings of ALA, dredging up from the depths the biochemistry I learnt while studying Microbiology.

However I also realised that this is of little interest to most folk who just want to know if taking ALA will help them or not, so I do not intend to get any more technical here. If that is where your interest lies you will need to surf the web yourselves - Lipoic Acid Basics - is a good place to start.


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Where do we get ALA from?

As I have said before the body is capable of making it's own ALA, which gives an indication of how important a substance it is. However it only makes enough for the basic metabolic processes.

This means there is none available for use as an antioxidant. To achieve the benefit of it's antioxidant properties we need to have an excess of ALA so that it can circulate freely throughout the body.

We can get a small amount from consuming foods containing ALA, such as red meat, yeast, potatoes, carrots, beetroot, yams, kohlrabi, spinach and broccoli.

Anyone on a diabetic diet will notice that most of these sources are foods we are told to eat sparingly or not at all! Broccoli and spinach of course are encouraged on all diets but just how much broccoli or spinach can any one person consume in a day (and we are not discussing POPEYE wannabe look-a-likes here)?!!!

Somewhere I read that to get the same amount of ALA via beef liver a day as you would get in a 600mg tablet you would need to eat 200 tons of the stuff - any volunteers?

I have been asked why, if ALA is so important to the body as an antioxidant, we do not produce enough for that purpose as well?

I can only give my take on this and that is in previous times, lets say the Palaeolithic era, we did not need the quantity of ALA we do now. We were not trying to deal with the highly refined, frankly toxic western diet. Rather we ate all the sorts of food that are listed as high in ALA. Also the only pollutants were the 'emissions' from the odd woolly mammoth!

The small amount of ALA we made coped fine then. It is us and our lifestyle that has increased the need and so it is up to us to help the body out by meeting that need.

 

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So that brings us to supplements.

There are a number of ALA supplements on the market but to get the best value for our money we need to know more about ALA itself. Remember that the ALA we take will have been manufactured and so is synthetic.

There are two forms of alpha lipoic acid.

There is the biologically active form that is found naturally in the body, called R-ALA and there is the synthetic by-product of ALA production, known as S-ALA.

It is possible to remove the S-ALA from the end product but it is an expensive and complicated process so many manufacturers do not bother.

Most commercially available tablets are a 50/50, or sometimes even a 70/30 mix of S-ALA and R-ALA.

The problem with this is that S-ALA does not do what R-ALA does, in fact it can sometimes do the exact opposite. It inhibits mitochondrial metabolism by it's inability to bind to the key enzymes and it is far less effective as an antioxidant.

S-ALA can also inhibit glucose entry into cells and decrease their insulin sensitivity.

The benefit you get from the R-ALA can well be cancelled by the S-ALA and you are pouring your money down the drain, never mind the frustration of having 'nothing happening'.

 

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I would personally rather pay that little bit more for a supplement that contains only R-ALA and get the full benefit for my money.

There are such supplements out there. Most can be bought online. Below are some of the websites:-

1. R-Isomer Alpha Lipoic Acid made by Bio-Health.

2. SAN R-ALA sold by Wholesale Suppliment Store in the US.
Or by their UK agent.

3. R+ Alpha Lipoic Acid from Discountsupplements LTD UK

4. RalaPure.com

 

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ALA and diabetes.

It is this that really interests us of course and there are a number of benefits to be had.

For Type 2 diabetics getting the glucose into the cell is of primary importance as our insulin resistance hampers that process no end. ALA appears to be an insulin mimetic (mimics the way insulin works) and works alongside insulin to make the process happen. Basically ALA appears to help the cell to mobilise its glucose transporters.

It also seems to increase the permeability of cell membranes, something that is decreased if you have high sugar levels.

It has been shown to improve glucose utilisation in many tissues but especially in muscle tissue, apparently by causing an increase in the number of glut-4 transporters on the outside of the myocites (muscle cells), sometimes by as much as 50%.

This is particularly important because muscle is responsible for the greatest uptake of glucose after a meal.

So basically ALA increases the glucose stored in muscle by channelling more of the glucose from the bloodstream to the muscle instead of to the adipose (fat) tissue - an important issue for the overweight Type 2 diabetic.

Studies done in 2001 in Toronto, Canada, concluded that ALA stimulated glucose uptake and stated

"Collectively, these results further support a role of alpha-lipoic-acid as an antidiabetic agent in the treatment of diabetes"

see the full study at DiabetesJournals.

Diabetics also suffer from increased glycation, which is where glucose tends to bind with proteins and in the process damages them. Glycated proteins produce vastly greater numbers of free radicals than nonglycated ones This can, in the long run, have damaging effects on most organs of the body and lead to diabetic complications.

ALA helps reduce this glycation and rids the body if the free radicals.

 

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Congestive heart failure (CHF)

is a common cause of death in diabetics. It happens when the heart is, for any number of reasons, unable to pump sufficient blood for the body's needs.

One reason for this occurs when LDL cholesterol is oxidised by free radicals.

Deposits of cholesterol, known as atherosclerotic plaques, build up on the walls of the arteries, restricting their size and thus the blood flow through them. This leads to hypertension and also the increased chance of a stroke or heart attack if a bit of this plaque becomes dislodged and travels to where it totally blocks the blood flow in a smaller vessel.

ALA inhibits the oxidation of proteins, of cellular DNA and protects against the oxidation of LDL. Inhibiting these greatly decreases the problems of CHF.

 

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Neuropathy (nerve damage)

is one of the most frequent seen complications of diabetes. It is a degenerative nerve condition that can cause numbness, tingling and sometimes burning pain in the extremities.

A number of studies have been done that show ALA to be very effective in partially restoring the nerve function and lessening the pain associated with this complication.

Peripheral neuropathy is aggravated by abnormal protein glycation and ALA, as we have stated before, helps prevent this glycation.

In Germany Alpha lipoic acid is an approved treatment for neuropathy, is available by prescription and has been successfully used for the past 30 years.

See www.PubMed.gov

The Mayo clinic, together with a Russian medical centre also did a study on the use of ALA in neuropathy and came up with this conclusion -

"There appears to be a rather large effect on the pain of diabetic neuropathy with ALA,"

says Peter Dyck, M.D., Mayo Clinic neurologist and peripheral nerve specialist.

"The magnitude of the change is considerable. We also found some improvement in neurologic signs and nerve conduction. We were surprised by the magnitude and the rapidity of the response."

MayoClinic.org

For other studies see:-

DiabetesJournals.org
FindArticles.com


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Diabetics also stand a risk of developing liver disease,

especially us Type 2's who are overweight, because this puts extra stress on the liver and together with high blood sugars can lead to a condition known as 'fatty liver', or if you want it's fancy name, nonalcoholic steatohepatitis.

Some of the drugs we are given, such as those to treat high cholesterol, may themselves cause liver damage.

ALA can with good reason be termed a universal detoxifier. It boosts the level of glutathione, a cellular, water soluble antioxidant which helps dissolve toxic substances in the liver, such as those we ingest from medications or chemicals in our food.

As glutathione is broken down in the digestive tract taking it as a supplement does not result in an increase within the cells and therefore ALA's ability to boosts the levels of glutathione is very important.

 

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ALA also chelates (binds) to heavy metals

like mercury, lead, cadmium and arsenic, pulling them out of circulation within the body and facilitating their removal. This helps prevent damage to many organs but especially the liver, which is one of the body's main filters.

 

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ALA can also minimise the side-effects of treatments such as x-rays and radiation for cancer,

probably by neutralising the enormous numbers of free radicals these treatments produce.

An interesting study into the effects of ALA on irradiated humans has been done following the Chernobyl disaster.

Children living in the contaminated areas, who were given 400mg a day of ALA or a combination of 400mg of ALA and 200mg of vitamin E over a 4 week period, had less oxidative damage, normal leukocyte levels and normal kidney and liver functions than those not receiving the supplements.

Vitamin E on it's own did not have any effect so it was the ALA that did the trick.

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Glaucoma

is an eye problem caused by an increase in the pressure of the fluid within the eye - known as the intraocular pressure (IOP). This excess fluid presses on the optic nerve at the back of the eye and eventually damages it, resulting in a gradual loss of peripheral vision. It is ALA's ability to boost glutathione levels that may make it of benefit in glaucoma treatment.

It has been suggested that 150 mg of alpha lipoic acid, taken daily for one month, improves visual function in people with glaucoma.

 

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Another, much more common, eye problem in diabetics are cataracts.

Cataracts are clumps of protein that collect on the lens of an eye and stop the light passing through it to the retina behind.

High sugar levels increase the chance of one getting cataracts. The cells of the eye are very susceptible to damage by glucose and the free radicals generated can cause damage to the proteins of the lens of the eye. These proteins are not renewable, they cannot be replaced and so permanent 'cloudy' areas develop in the eye.

The eye is protected from free radical damage by the antioxidant glutathione which is found in the fluid within the eye. ALA, as said before, boosts the levels of this.

Dr. Lester Packer, who heads the Department of Molecular & Cell Biology at the University of California, Berkley and his team, studying the effects of ALA on cataracts, suggested that about 60% of diabetes related cataracts could be prevented with ALA.

 

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So how much ALA does one need?

This really depends on what you are trying to get out of taking it.

Below are some guidelines:-

100-300mg a day as a general antioxidant
150-200mg a day for cataracts and glaucoma
400-600mg per day for diabetes and reduction of oxidative stress
600-800mg per day for neuropathy

As ALA is absorbed, metabolised and cleared rapidly it works best as a number of smaller divided doses taken throughout the day rather than one large single dose.

This is assuming, of course, that you are not taking a 'time release' version.

It has been suggested that ALA has better bioavailability if taken on an empty stomach but there have been mentions in the forums that large quantities taken like that have caused hypos so you will need to try this out for yourself.

Be careful and make sure you do not try it unless there is someone there with you who knows what to do if you do crash


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Side effects.

The obvious one is the one mentioned above - it may make your blood glucose levels go to low, leading to a hypo. As a type 2 battling to get her BG levels down this sounds like a one way ticket to heaven but I suppose we all have our cross to bear. If yours is hypo's then be careful.

Some people are allergic to ALA and come out in skin rashes, have headaches or upset stomachs. I am afraid that if these symptoms occur you will have to stop taking the ALA.

People who may be deficient in vitamin B1 (such as alcoholics) should supplement it if taking ALA.

 

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Some interesting websites:-

RalaPure.com
Benefits for Cataracts/Glaucoma.

Vitamin Reasearch Products
has an interesting article dealing with all aspects of ALA.

ALAUpdate.com
Alpha Lipoic Acid assists in diabetes related glucose uptake.

ALAUpdate.com
Lipoic Acid Effects on Blood Pressure, Glucose Tolerance, and Insulin Sensitivity.

ALAUpdate.com
Effects of ALA on free fatty acid oxidation.

ALAUpdate.com
Alpha Lipoic Acids effects in the treatment of diabetic autonomic neuropathy.

ALAUpdate.com
Alpha Lipoic Acid improves insulin sensitivity in patients with type II diabetes.

ALAUpdate.com
Alpha Lipoic Acid aids in the prevention of diabetes complications.

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