| ALA Information |
| By David Tolson |
1. What is ALA?
ALA (alpha lipoic acid) is an enzyme found throughout the body and a key
component of mitochondria, which produce energy for cells. It is involved
in a variety of reactions, such as the conversion of pyruvate and other
alpha-keto acids in the Krebs cycle. It is also a potent antioxidant that
has been used to treat a variety of conditions, including diabetes, AIDS,
cancer, hypertension, neurological degeneration, cataracts, kidney and liver
disorders, and coronary heart disease.
2. What application does ALA have?
ALA has a variety of applications for the athlete, as it will enhance both
performance and general health. In addition to its antioxidant properties,
it may also increase eNOS activity, stabilize blood sugar, chelate heavy
metals, and improve cognitive function.
Exercise can increase mitochondrial superoxide production, ischaemia-reperfusion,
and auto-oxidation of catecholamines (1). Research has found that exercise
may result in a 10- to 20-fold increase in whole-body oxygen uptake, with
oxygen flux increasing by a magnitude of 100-200 in muscle fibers. According
to a recent article in Sports Medicine, "Studies during the past 2 decades
suggest that during strenuous exercise, generation of reactive oxygen species
(ROS) is elevated to a level that overwhelms tissue antioxidant defence
systems. The result is oxidative stress. The magnitude of the stress depends
on the ability of the tissues to detoxify ROS, that is, antioxidant defences....
Efforts to determine individual needs of athletes and a balanced diet rich
in antioxidant supplements are highly recommended (2)." Studies have shown
orally supplemented ALA to specifically protect against exercise-induced
oxidative stress, and shown it to be superior to other antioxidants in this
respect (8, 9).
3. How does ALA work?
Many have called ALA the "perfect antioxidant." This is because ALA does
not exhibit many of the weaknesses found in many common antioxidants, such
as Vitamin C, Vitamin E, beta carotene, cartenoids, and others, and has
many added advantages.
First of all, most antioxidants only defend against one or a few varieties
of ROS. ALA removes peroxyl, peroxynitrite, hydroxyl, alkoxyl, and superoxide
radicals, among many others. Secondly, most antioxidants are tissue specific.
For example, many are either fat soluble (such as Vitamin E) or water soluble
(such as Vitamin C). Alpha lipoic acid is fat soluble, and it's metabolite,
dihydrolipoic acid - which is another potent antioxidant - is water soluble.
Third, the small size of the ALA molecule allows it to prevent oxidation
in areas where others cannot, such as oxidation within the cell nucleus.
Fourth, research has shown ALA to be readily absorped (3), whereas many other
antioxidants are readily excreted or have low bioavailability. Fifth, ALA
recycles itself, while many other antioxidants are rapidly oxidized (4).
Finally, ALA operates synergistically with three other important antioxidants,
glutathione, Vitamin C, and Vitamin E. It allows Vitamin C to be recycled
(4), a synergistic effect has been shown with Vitamin E (5), and both Vitamin
E and Vitamin C recycle ALA by donating electrons to ALA cations (6). The
fact that ALA increases production of glutathione (7) is especially important.
Glutathione is one of the body's primary antioxidants. However, exogenously
administered glutathione does not cross cell membranes, but ALA does.
4. What are some further benefits of ALA use?
- Stabilizes blood sugar - ALA has been used in the treatment
of diabetes and the prevention of Type 2 diabetes (10). It modulates glucose
uptake by changing the intracellular redox status, thus improving insulin
sensitivity (11, 12). Insulin resistance decreases blood flow, oxygen availability,
and glucose uptake in muscle during exercise (14, 15). Additionally, ALA
may have an additive effect on improving insulin sensitivity when combined
with exercise (13).
- Hemodilation - A new line of supplements known as "hemodilators,"
which usually contain arginine alpha-ketoglutarate (A-AKG), increase the
levels of nitric oxide (NO) in the bloodstream, thus causing vasodilation,
lowering blood pressure, and increasing blood flow to the muscles. Unfortunately,
there are issues which these products do not address, the first being that
increasing NO levels often causes an increase in free radical (namely, peroxynitrite)
formation (16), and the second being that excesses of arginine will cause
methionine deficiency (17).
It has been shown that ALA directly stimulates the production of NO by increasing
the activity of eNOS (endothelial nitric oxide synthase) (4, 18). Also, ALA
does this while simultaneously increasing the antioxidant defenses of endothelial
cells (4). In other words, it has all of the good properties of A-AKG with
none of the bad. This is why many users of ALA report increased pumps both
in and out of the gym.
- Improves cognitive function - ALA has been shown to improve
cognitive function in many ways, some of which may be independent of it's
antioxidant properties. It exhibits a concentration-dependant upregulation
of Phase II detoxification enzymes, especially NAD(P)H:quinone oxidoreductase
(NQO1) and glutathione-S-transferase (GST), both of which are potent neuroprotectants
(19). It decreases all three indices of oxidative stress in the brain, which
in turn reverses memory impairment and improves cognition (20). It also improves
nerve conduction and neural blood flow (21), and improves mitochondrial function
and decreases DNA/RNA oxidation in the brain, both of which prevent memory
loss (22). Because of this, it has been used to treat a variety of ailments,
including Alzheimer's (23).
- Other benefits - ALA is highly concentrated in the eye and
can prevent visual impairment. It reduces advanced glycation end products
(AGEs) (24), which may play a role in macular degeneration and diabetic retinopathy
(25). It also protects the retina against ischemia-reperfusion injury (26).
Because of its effect on NO production, ALA can also aid in the prevention
of hypertension (12). In addition, ALA protects the heart by increasing
mitochondrial function and decreasing superoxide anion production, as well
as reducing plasma lipid levels, reduces the risk of coronary heart disease
(27).
As a general antioxidant, ALA has also been used in the treatment of many
other ailments, including impaired kidney function, impaired liver function,
and cancer.
5. Are there any side effects?
ALA has no serious side effects. Some users are allergic and have a mild
rash; if this happens you should discontinue use or consult a doctor. Also,
some users report nausea with high doses. If you have low blood pressure
or are hypoglycemic, you should consult a doctor before taking ALA as it
may possibly exacerbate these conditions.
6. What form of ALA is best?
There are two forms of ALA in popular usage. ALA is a mixture of 50% R-ALA
and 50% S-ALA while R-ALA is the stereoisomer that naturally occurs in the
body, hence supplemental R-ALA is much more potent (30). In some areas,
such as prevention of cataracts, R-ALA works while S-ALA has no effect at
all (29). In addition, there is evidence that S-ALA may negate some of the
beneficial effects of R-ALA (28). R-ALA is clearly a better choice, although
one can get some of the beneficial effects from regular ALA.
7. How should I take ALA?
As a general antioxidant, dosages of 100 mg a day are effective. For increased
pumps or increased insulin response, 100-200 mg 2-3 times daily with food
are recommended. Keep in mind that the effects of ALA are largely dose-dependent,
but long-term studies with dosages over 600 mg/day (of R-ALA) have not been
done. Also, the dosage one requires for R-ALA will be significantly lower
than with regular ALA.
8. What are some good supplements to take along with ALA?
Although ALA functions excellently on its own, taking some supplements
in conjunction may increase its benefits. It works well in tandem with many
other antioxidants, such as vitamin C, vitamin E, and N-acetyl cysteine.
It also has an additive effect with acetyl-L-carnitine in improving brain
function (22).
If you have any questions or comments regarding this article, please email
dvdtlsn@bulknutrition.com. No part of this article may be reproduced in any form without the permission of David Tolson or Mike McCandless. |
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