Generality
Alpha-Lipoic Acid is a cofactor of vital importance for human body cells.
Effective in relation to diabetic pathology, in particular diabetic neuropathy, as well as in many other pro-oxidant conditions, integration with Alpha-Lipoic Acid has generally proved to be well tolerated.
brief review of organic chemistry
The carbon reported by the asterisk is a chiral center (as sp3 hybridized and bound to different atoms between them). The presence of chiral centers (or centers of asymmetry) involves the existence of 2n enantiomers (compounds, one non-superimposable mirror image of the other, which differ only in rotatory optical power). Given that n is the number of chiral centers in this case only 21 = 2 enantiomers will exist. One of these has R configuration, the other S.
Generally only one of the two enantiomers is able to react with biological receptors and carry out the desired function.
In the case of lipoic acid the biologically active natural form is R. The synthetic lipoic acid (also called alpha lipoic acid) is instead a mixture of the R and S (raceme) form. Not all drugs or food supplements with asymmetry centers can be sold in the racemic form, since in some cases the enantiomer that has no pharmacological interest has negative effects on the body (people with a few more years will remember the case of thalidomide and phocomelic children).
The antioxidant properties of lipoic acid are due to the presence of the sulfide bridge which acts as an electron acceptor.
The figure shows the two forms in which lipoic acid exists in oxidized (above) and reduced (below) nature. These two forms are easily interconvertible through redox reactions.
Indications
Why is Alpha Lipoic Acid used? What is it for?
Alpha-Lipoic Acid is an organic acid characterized by strong direct and indirect antioxidant activity.
More precisely, Alpha-Lipoic Acid is attributed:
- Direct antioxidant activity, valuable both in the aqueous (cytoplasmic) and lipid phase (typical of cell membranes). Thanks to this characteristic, Alpha-Lipoic Acid protects the body from both intracellular and extracellular free radicals, in both biologically present chemical forms.
- Indirect antioxidant activity, important in regenerating other antioxidants such as vitamin C, vitamin E, coenzyme Q10 and glutathione.
- Chelating activities against heavy metals such as mercury and lead;
- Metabolic activities, especially valuable in optimizing the oxidative metabolism of sugars.
In light of the aforementioned biological activities, Alpha-Lipoic Acid is successfully used mainly as an antioxidant.
Diabetes and its complications (such as diabetic neuropathy), dyslipidemias, atherosclerosis, neurodegenerative diseases and ischemia damage are at the moment some of the clinical conditions in which Alpha-Lipoic Acid has proved to be effective.
Experts also consider the biological potential in sports, especially useful in preventing muscle-tendon damage caused by reactive oxygen species produced in large quantities during intense training.
Property and Effectiveness
What benefit has Alpha-Lipoic Acid shown during the studies?
Studies currently published in the literature support the biological activity, especially antioxidant, of Alpha-Lipoic Acid.
From a careful examination of the literature, mostly concentrated on experimental models, some significant potentials would emerge.
Alpha-Lipoic Acid and cardiovascular function
The interesting protective action of Alpha-Lipoic Acid on cardiovascular function, derives mainly from the ability of this molecule to inhibit the oxidation of LDL cholesterol.
It is well known that oxidation of small LDL particles is one of the main risk factors for atherosclerotic diseases, and more precisely for the formation of the much feared atheromatous plaque.
Acid-Alpha-Lipoic acid and antiaging medicine
For several years now, Alpha-Lipoic Acid has been included among the most useful anti-aging remedies.
The antiaging action of Alpha-Lipoic Acid would in this case be due to the action:
- antioxidant, important in preserving the correct functional and structural integrity of tissues and certain organs such as the liver;
- metabolic, especially valuable in optimizing glucose metabolism, reducing the formation of advanced glycosylation complexes (protagonists of aging).
Alpha-Lipoic acid and diabetes
Despite the sensitive hypoglycemic action, Alpha-Lipoic Acid is successfully used in diabetic pathology especially in the management of diabetic neuropathy.
In several clinical trials it has been shown that the use of Alpha-Lipoic Acid, for several weeks, may contribute to a reduction of some typical symptoms of neuropathy, such as paresthesia, pain and the sensation of peripheral burning.
At the base of this activity there would seem to be the improvement action on the nervous vasculature.
Acid-Alpha-Lipoic acid and sport
The use of Alpha-Lipoic Acid in athletes would be justified above all for its myoprotective activity against damage caused by oxygen free radicals.
From some studies, mostly experimental, the ability of Alpha-Lipoic Acid, in association with other antioxidants, to emerge:
- Prevent the decrease of glutathione-transferase activity induced by physical exercise;
- Protect the muscle from oxidative damage;
- Counteract the lipid peroxidation of the membranes.
Doses and method of use
How to use Alpha-Lipoic Acid
The daily most used dosages of Alpha-Lipoic Acid are those of 300-600 mg, for a period of at least three weeks.
In particular, 600 mg / day is the dose to be taken when the symptoms are acute; 300 mg / day is a suitable dose for the maintenance phase.
The chemical characteristics of Alpha-Lipoic Acid allow an easy intestinal absorption, at the level of the small intestine, and an excellent biodistribution, widespread also to the central nervous system, due to the ability to cross the blood-brain barrier.
Side effects
At the above doses, the use of Alpha-Lipoic Acid is generally well tolerated and free of clinically relevant adverse reactions.
Although the potential effects of an overdose of Alpha-Lipoic Acid are not yet well characterized, there is some evidence in the literature of induced hypoglycemia and allergic skin reactions.
Contraindications
When should Alpha-Lipoic Acid not be used?
The use of Alpha-Lipoic Acid is contraindicated in case of hypersensitivity to the active ingredient, as well as during pregnancy and breastfeeding.
Pharmacological Interactions
Which drugs or foods can modify the effect of Alpha-Lipoic Acid?
The contextual use of Alpha-Lipoic Acid and hypoglycemic drugs could induce an unpredictable and unintended lowering of glycemic values. This side effect must necessarily be reported on the label of food supplements based on lipoic acid.
Precautions for use
What do you need to know before taking Alpha-Lipoic Acid?
Given the potential hypoglycemic effect of Alpha-Lipoic Acid, it would be appropriate to require close medical supervision during diabetic pathology, altered glucose metabolism and obviously in the course of drug therapy with hypoglycemic agents.