ALPHA-LIPOIC ACID
AntiO
Composition:
Each hard gelatin capsule contains :
Alpha lipoic acid 100 mg
AntiO (Alpha-lipoic acid) is a naturally occurring antioxidant.
AntiO (Alpha-lipoic acid) is found as a prosthetic group in
alpha-kelo acid dehydrogenase complexes of the
mitochondria, and as such plays a fundamental role in
metabolism. It is also known as thioclic acid. 11 is
synthesized inside the body and available in every tissue
of the body system. AntiO (Alpha-lipoic acid) has been
found lo affect cellular metabolic processes in vitro, as it
has the ability lo alter the redox status of cells and interact
with thiols and other antioxidants. Therefore, it appears
that this compound has important therapeutic potential in
conditions where oxidative stress is involved.
Mechanism of action:
In vitro, the final antioxidant activity of lipoic acid is
determined by its concentration and by its antioxidant
properties. Four antioxidant properties of lipoic acid have
been studied;
β’ It has a metal chelating capacity
β’ It has ability lo scavenge reactive oxygen species (ROS)
β’ It has ability to regenerate endogenous antioxidants
β’ It has ability to repair oxidative damage.
Clinical pharmacology:
I. Lipoic acid is an example of a drug whose therapeutic
effect has been related to ilsantioxidant activity.
2 Antioxidant activity is a relative concept', it depends on
the kind of oxidative stress and the kind of oxidizable
sut)strate(e.g., DMA, lipid, protein).
3. Dihydrolipoic acid (DHLA), formed by reduction of lipoic
acid, has more antioxidant properties than does lipoic
acid. Both DHLA and lipoic acid have metal-chelating
capacity and scavenge ROS. whereas only DHLA is
able to regenerate endogenous antioxidants and to
repair oxidative damage.
4. As a metal chelator, lipoic acid was shown to provide
antioxidant activity by chelating Fe2+ anctCu2+; DHLA
can do so by chelating Cd2+.
5. As scavengers of ROS, lipoic acid and DHLA display
antioxidant activity in most experiments. whereas, in
particular cases, pro-oxidant activity has been
observed. However, lipoic acid can act as an
antioxidant against the pro-oxidant activity produced
by DHLA.
6. DHLA has the capacity to regenerate the endogenous
antioxidants vitamin E, vitamin C and glutathione
7. DHLA can provide peptide methionine sulfoxide
reductase with reducing equivalents. This enhances
the repair of oxidatively damaged proteins such as
alpha-1 antiprotease. 8. Through the lipoamide
dehydrogenase-dependent reduction of lipoic acid, the
cell can draw on its NADH pool for antioxidant activity
additionally to its NADPH pool, which is usually
consumed during oxidative stress.
9. Within drug-related antioxidant pharmacology, lipoic
acid is a model compound that enhances
understanding of the mode of action of antioxidants in
drug therapy.
AntiO (Alpha-lipoic acid) as a unique antioxidant :
Reactive oxygen species are thought to be involved in a
number of types of acute and chronic pathologic conditions
in the brain and neural tissue. The metabolic antioxidant
alpha-lipoate is a low molecular weight substance that is
absorbed from the diet and crosses the blood-brain barrier.
alpha-lipoate is taken up and reduced in cells and tissues
to dihydrolipoate, which is also exported to the extracellular
medium: hence, protection is afforded to both intracellular
and extracellular environments. Both alpha-lipoate and
especially dihydrolipoate have been shown to be potent
antioxidants, to regenerate through redox cycling, it
enhances the action of other antioxidants like vitamin C
and vitamin E, and to raise intracellular glutathione levels.
Thus. it would seem an ideal substance in the treatment of
oxidative brain and neural disorders involving free radical
processes.
Many studies on humans and/or animals reveals protective
effects of these compounds in cerebral ischemic
reperfusion, excitoloxic airiino acid brain injury.
mitochondrial dysfunction, diabetes and diabetic
neuropathy, inborn errors of metabolism, and other causes
of acute or chronic damage to brain or neural tissue.
Clinical significance:
Alpha lipoic acid is used for the treatment of diabetic neuropathy;
AntiO (Alpha-lipoic acid) reduces process of glycation
Glycation is a process in which blood sugar act
spontaneously with body proteins such as coNagen and
other tissue to form sugar damaged proteins Glycation is
a more serious problem in diabetics because of high blood
sugar level and it may lead lo kidney damage, damage to
retina and and also nerve damage.
AntiO (Aipha-lipoic add) in prevention of coronary artery
disease.
As an antioxidant AntiO (Alpha-lipoic acid) protects low
density lipoprotein (LDL) from oxidation and free radicals
thus prevent the probability of a CAD.
AntiO (A!pha-iip0ic acid) improves neurological function
AntiO (Alpha-lipoic acid) prevents the peroxidation of nerve
cell membranes by inhibiting glycation and scavenging free
radicals Thus it slow down the progression of diabetic
neuropathy which it unchecked may lead to numbness of
feet, infection and this may lead to amputation. AntiO (Alpha-
lipoic acid) also prevents damage of the brain tissue by
free radicals.
AntiO (Alpha-lipoic acid) in liver metabolism and disease
AntiO (Alpha-lipoic acid) was also used as a therapeutic
agent in a number of conditions relating to liver disease
including alcohol-induced damage, mushroom poisoning.
metal intoxication, and carbon tetrachloride poisoning
AntiO (Alpha-lipoic acid) supplementation was successful
in the treatment for these conditions m many cases.
AntiO (Alpha-lipoic acid) in HIV (AIDS) Scientists have also
found that lipoic acid can inhibit replication of HIV-1 arid
other viruses through its ability to bind directly to DNA
Cataracts The interior of the eye is an aqueous
environment, and fat-soluble antioxidants like vitamin E and
beta-carotene don't offer much protection Given the dual
water and fat soluble antioxidant properties of ALA.
scientists are investigating the effects of alpha-lipoic on
AntiO in cataracts . Researchers have found that AntiO
(Alpha-lipoic acid) is of potential therapeutic use in
preventing cataracts and their complications, noting that
biochemical) changes in the lens showed major increases
in levels of glutathione, ascorbate, vitamin E and other
protective enzymes.
Side effects;
AntiO (Alpha-lipoic acid) as a natural body constituent is
very safe to use. It is available in many countries like
Australia, Germany, Italy and Japan and used by many
individuals without reported side effects. However some
patients may experience minor side effects like diarrhea or
skin rash while tacking higher dosage than recommended
Drug interaction;
The absorption of iron and other minerals may be reduced
if coadministered.
Pregnancy:
There are no reports of contraindication of AntiO (Alpha
lipoic acid) during pregnancy, but if should be avoided
during first trimester '
Dosage:
AntiO (Alpha-lipoic acid) is advised as an extra dietary-
supplement in the dosage of 100-200 mg. per day.
Indications:
To counteract the oxidative stress caused by superoxide
generation.
As an antioxidant in free radical mediated disorders like
diabetes, coronary artery diseases etc. Also in treatment
of liver dysfunctions including alcohol induced damage.
It is recommended for the people who are prone for above
conditions because of their family history or their current
lifestyle.