• The King of Antioxidants: Unparalleled Free Radical Protection
• The Best DHLA Form Derived from a Natural Source
DHLA: The Spectacular Antioxidant
DHLA (dihydrolipoic acid) is unique as an antioxidant due to its spectacular effectiveness in quenching every known free radical that occurs
in living tissue, including both fat and water-soluble tissues. No other antioxidant has this incredible capability. DHLA is readily absorbed
orally and has very low toxicity. It has unequalled potential as a highly effective therapeutic agent in clinical conditions associated with free
radical damage such as Parkinson’s disease, Alzheimer’s disease and other neurodegenerative illnesses.(1)
Until 2003, DHLA in a stabilized form was not available. DHLA could only be obtained indirectly through consuming ALA
(alpha lipoic acid) which in turn, was converted by the body into small amounts of DHLA. However, this process did not deliver a significant
or reliable supply of DHLA. Research studies have attempted to measure the effect of DHLA on cellular tissue using indirect methods based
on ALA consumption. As a result, DHLA is known to be a powerful electron donor to other compounds. Ascorbic acid and indirectly vitamin
E are regenerated by DHLA.(2) Busse et. al. found that the oxidized form of DHLA, ALA, increased intracellular glutathione.(3) DHLA was
shown to regenerate coenzyme Q10, glutathione and NADPH or NADH and by this mechanism, increase cellular ATP production.(4) The
oxidized form of DHLA, ALA, also assists in the conversion of pyruvate to acetyl-coenzyme A, the beginning point of the Krebs cycle which
produces the high energy molecule ATP.
The Discovery of Stable DHLA
Recently, the world’s first stable form of DHLA has been created by a U.S. researcher and has been verified
by independent laboratory testing. Stable DHLA offers a significant and reliable source of DHLA, never before available.
Synthetic vs. Natural Sources
ALA, R-lipoic acid or DHLA that are derived from synthetic sources can
never match natural-source counterparts in the ability to sustain and repair
the DNA of the cell. A natural (nonsynthetic) source is comprised
of dynamic, complex living processes where each molecule contains atoms that
generate biological photons, or in other words, pure light. The photonic field around
each molecule creates a luminous field which surrounds all living substances.
Only nutrients derived from a natural source are capable
of upgrading cellular DNA, according to quantum physics researcher
and expert, Dr. Fritz-Albert Popp.(33)
On the other hand, synthetic-source nutrients may provide initial
cellular benefits, but over time, they act to accelerate the degeneration of
DNA, ending in earlier cell death. Synthetic nutrients initially stimulate
the cell to accomplish work which may appear to be beneficial, but long-term,
the DNA and cellular degradation cannot justify the initial benefits.
Consequently, using ALA derived from a synthetic source can defeat the
purpose of using an ALA supplement in order to live longer and more healthfully. Not
only has a stable form of DHLA been badly needed, but also a DHLA
source that has been derived from a natural source so it is capable
of imparting significant, long-term DNA protection and cellular benefits.
Benefits of ALA (Alpha Lipoic Acid)
Research Summary
Many research studies show the spectacular benefits from the use of
ALA, even ALA derived from synthetic sources. Although these
studies demonstrate many short-term benefits of synthetic ALA, they do not test for or warn against the long-term problems encountered in
consuming synthetically-derived agents.
Unfortunately, most research studies using ALA have used the
synthetic form which contains equal amounts of the R
and the S racemic forms. The S form occurs only in
synthetic-source ALA, never in naturally-derived
ALA, and has negative, pro-inflammatory effects.
In an attempt to enhance the effectiveness
of synthetic ALA, some manufacturers
have chemically removed the S-form,
thus producing a new form, stand-alone R-lipoic
acid. Because synthetically derived
ALA contains both R and S forms, studies
show that synthetic R-lipoic acid alone is superior
to ALA (which contains both R and S
forms).
A 1995 research study using DL-alpha-lipoic acid, a
synthetic form containing both the R and the S forms in equal
proportions, claimed that the resultant DHLA was both an antioxidant
and a pro-oxidant where hydroxyl radicals were generated.(8) However,
new research since the year 2000 has shown the S-form of lipoic acid
(which has pro-inflammatory effects) may well be the cause of this prooxidant
study finding (rather than as an effect of DHLA).
The highlights of ALA research, including R-lipoic acid and S-lipoic
acid, are as follows:
Scavenger of Free Radicals. Lester Packer, PhD, of the
University of California at Berkeley, has shown that ALA is a powerful
free radical quencher and metal-chelating agent. It helps regenerate
other antioxidants and favorably affects gene expression.(1) Experts
are in general agreement that ALA can scavenge the
hydroxyl radical, hypochlorous acid radical, and singlet oxygen radical,
but not the peroxyl or superoxide anion free radical.(1, 5-7)
Kidney Protection: Research by Sandhya et. al. found that ALA
protected kidney cells in a dose-dependent manner.(8)
Arsenic Protection: Research has shown that ALA can protect
mice from poisoning by sodium arsenite, an arsenical herbicide, insecticide
and rodenticide by a ratio of ALA to arsenite of at least 8:1. The
mice were protected even if the administration of ALA was given after
onset of severe symptoms of poisoning.(9)
Mercury Protection: Further research has demonstrated that ALA
removed mercury from renal slices (kidney).(14) ALA was also shown to
dramatically increase biliary excretion of injected mercury while decreasing
cadmium, zinc, copper and methylmercury excretion.(15)
Cadmium Protection: In another study, ALA and R-lipoic acid were shown
more effective than S-lipoic acid (which occurs only in synthetic ALA) in
metal chelation.(10) In isolated hepatocytes (liver cells), ALA reduced cadmium-induced toxicity. However, DHLA was much more effective than ALA.(11)
ALA (and therefore DHLA at least as much or more) was shown to provide
significant liver protection against cadmium toxicity, even under glutathionedepleted
experimental conditions.(12) Another study showed ALA completely
prevented cadmium-induced lipid peroxidation in the brain, heart and testicles
in rats.(13)
Restoration of Metabolism and Mobility: R-lipoic acid supplementation
reversed the age-related, declining ability of rats to respond to increased
oxidative stress. The age decline was almost completely reversed on a two week
dietary supplementation of R-lipoic acid.(16) When fed to old rats, R-lipoic
acid showed complete reversal of declining levels of glutathione and
ascorbic acid in hepatocytes. In addition, the metabolic rate and mobility of
the old rats were also restored to that of youthful rats.(17, 18)
Decreased Oxidative Stress in the Heart: Another study found the
aging rat heart is under increased mitochondrial-induced oxidative stress (elevated
free radical attack). This oxidative stress in the heart was significantly
reduced by R-lipoic acid supplementation.(19)
Improvement in Type II Diabetes. Since 2000, about 80% of all
type II diabetes is now believed to be linked to infection. Type II diabetes is now
at epidemic proportions with 900,000 new cases per year in the U.S. The infectious
process produces large amounts of free radicals. One marker of free radical
damage common to Type II diabetes is AGEs (advanced glycation end products).
Glycation of protein can be caused by elevated blood and tissue glucose.
Packer and Kawabata(20) showed that non-covalent binding of ALA to albumin
protects protein from glycation.
Other studies using ALA in Type II diabetes have shown improvement in insulin
metabolism.(21, 22) Nerve damage (polyneuropathies) is common in diabetes
and has been successfully treated with ALA in Germany for more than 20 years.
Findings show that ALA administration yielded excellent results: albuminuria
decreased 50%,(23) and neuropeptide deficits, nerve blood flow and neurological
symptoms all improved.(24, 25, 26)
Glaucoma Improvement: In one glaucoma study, stage I and II OAG (open angle
glaucoma) patients were assigned to one of 3 groups: no ALA, 75mg or
150mg ALA daily for 2 months. The greatest improvement in visual function,
efficacy of liquid discharge and biochemical markers were observed in the group
receiving the higher dose of ALA.(30)
Protection Against Cataracts: Cataracts in diabetics have shown a direct
correlation with high levels of aldose reductase, which is inhibited by ALA in
the lenses of rats.(31) Other studies suggest ALA supplementation may be protective
against cataract formation by other causes.(32)
Benefits of Stable DHLA
The above clinical research studies using synthetically-derived ALA had obviously
spectacular physiological benefits. However, as has been emphasized earlier, these
benefits are not without a price to pay, namely, the eventual degradation of the cellular
DNA which occurs during long-term use of synthetic compounds.
Advantages of Natural-Source DHLA: Stable DHLA (natural-source) may
prove to be one of the most significant antioxidant compounds ever created, since
it can accomplish all the feats attributed to ALA and more, but without ALA’s
negative effects. In fact, some authors believe that the benefits ascribed to ALA are
in fact, actually due to the internal generation of DHLA (after ALA consumption).
For the very first time, stable DHLA is now available that can offer significant
and reliable amounts of DHLA, without the need to consume synthetic precursors.
DNA and Nerve Protection: Stable DHLA can provide exquisite
neuroprotection as well as superior DNA protection and repair, unmatchable by any
other antioxidant. Studies show that DHLA increases cellular energy and efficiency
by increasing ATP. At the same time, DHLA helps regenerate the production of
vitamin E, CoQ10, glutathione, NADH and NADPH to provide unparalleled DNA
protection. In addition, DHLA has the capacity to induce repair of DNA strand
breaks.(7) For long-term benefits of DHLA, only natural-source DHLA is recommended
to avoid the long-term degradation of DNA from synthetically-derived sources.
Arterial and Heart Protection: Research has shown that DHLA can accelerate
recovery of the aortic blood flow during reperfusion (resumption of blood flow)
and increase ATP synthesis in the rat heart.(27) ALA forms were not helpful — only
internally generated DHLA was able to reduce the infarct or necrotic tissue size in
middle cerebral artery occlusion in mice.(28) Wolz et. al. believe ALA must be reduced
to the DHLA form in order to provide neuroprotection.(29) Natural-source,
stable DHLA (now available) can provide exquisite neuroprotection as well as
superior DNA repair and protection without compromise.
DHLA: Safety and Effectiveness
Clinical research has shown that the newly available
natural-source, stable DHLA is both safe and effective for general use, including
those with chronic illness and neurodegenerative disease. If high dosages (over
300 mg/day) of stable DHLA are used, to get maximum benefits the concurrent
use of additional nutrients such as nutritional yeast which contains naturalsource
B vitamins, sulphur-based amino acids and reduced glutathione, is an excellent
adjunct.
Brief Clinical Observations. Researchers have observed various immediate, spectacular effects of
oral administration of stable DHLA.
One 44-year woman presented with a history of bilateral, maxillary sinus infection
with extreme pain even to the touch. She had used oral antiobiotics for
more than a year with no relief and was unable to breathe through her sinuses
for at least 10 months. Further, she had begun to experience pain at her liver,
chronic fatigue, loose stool and severe brain fog. After consuming only 1/2 tsp.
of stable DHLA, within less than one minute, she remarked,
“I can breathe through my nose! My head feels clear for the first time in 10
months.”
A 60 year-old male complaining of recent brain fog, diminished short-term memory
and a general sense of malaise remarked that within one day of taking
stable DHLA, these symptoms were gone. He had a renewed
sense of mental acuity and a significant improvement in short-term
memory.
A medical doctor has remarked that in many clinical cases,
stable DHLA reduced the amount of time and number of nutritional supplements
needed to restore healthy nerve function in his patients. It became
one of his most used supplement “aces”, especially in his neurodegenerative cases.
References
- Packer L, Witt EH, Tritschler HJ. Alpha-lipoic acid as biological antioxidant. Free Rad Biol Med 1995;19:227-250.
- Scholich H, Murphy ME, Sies H. Antioxidant activity of dihydrolipoate against microsomal lipid peroxidation and
its dependence on a-tocopherol. Biochem Biophys Acta 1989;1001:256-261.
- Busse E, Zimmer G, Schopohl B, etal. Influence of alpha-lipoic acid on intracellular glutathione in vitro and in vivo.
Arzneimittel-Forschung 1992;42:829-831.
- Kagan v, Serbinova E, Parker L. Antioxidant effects of ubiquinones in microsomes and mitochondria are mediated
by tocopherol recycling. Biochem Biophys Res Comm 1990;169:851-857.
- Passwater RA. Lipoic Acid: The Metabolic Antioxidant. New Canaan, CT: Keats Publishing, Inc; 1995:1-47.
- Scott BC, Arouma OI, Evans PJ, et al. Lipoic and dihydrolipoic acid as antioxidants: a critical evaluation. Free
Rad Res 1994;20:119-133.
- Suzuki Yj, Tsuchiya M, Packer L. Thioctic acid and dihydrolipoic acid are novel antioxidants which interact with
reactive oxygen species. Free Rad Res Comms 1991;15:255-263.
- Sandhya P, Mohandass S, Varalakshmi P. Role of DL alpha-lipoic acid in gentamicin induced nephrotoxicity. Mol
Cell Biochem 1995;145:11-17.
- MGrunert RR. The effect of DL Alpha-lipoic acid on heavy-metal intoxication in mice and dogs. Arch Biochem
Biophys 1960;86:190-194.
- Ou P, Tritschler Hj, Wolff SP. Thioctic (lipoic) acid: a therapeutic metal-chelating antioxidant? Biochem Pharmacol
1995;50:123-126.
- Muller L, Menzel H. Studies on the efficacy of lipoate and dihydrolipoate in the alteration of cadmium toxicity
in isolated hepatocytes. Biochem Biophys Acta 1990;10523:386-391.
- Sumathi R, Baskaran G, Varalakshmi P. Relationship between glutathione and DL alpha-lipoic acid against
cadmium-induced hepatotoxicity. Jpn J Med Sci Biol 1996;49:39-48.
- Sumathi R, Devi VK, Varalakshmi P. DL alpha-lipoic acid protection against cadmium-induced tissue lipid
peroxidation. Med Sci Res 1994;22:23-25.
- Keith RL, Setiarahardjo I, Fernando Q, et al. Utilization of renal slices to evaluate the efficacy of chelating agents
for removing mercury from the kidney. Toxicology 1997;116:67-75.
- Gregus Z, Stein AF, Varga F. Effect of lipoic acid on biliary excretion of glutathione and metals. Toxicol Appl
Pharmacol 1992;114:88-96.
- Lykkesfeldt J, Hagen TM, Vinarsky V, Ames BN. Age-associated decline in ascorbic acid concentration, recycling,
and biosynthesis in rat hepatocytes—reversal with (R)-alpha-lipoic acid supplementation. FASEB J 1998
Sep;12(12):1183-9.
- Hagen TM, Ingersoll RT, Lykkesfeldt J, Liu J, Wehr CM, Vinarsky V, Bartholomew JC, Ames AB. (R)-alpha-lipoic
acid-supplemented old rats have improved mitochondrial function, decreased oxidative damage, and increased metabolic
rate. FASEB J 1999 Feb;13(2):411-8.
- Hagen TM, Vinarsky V, Wehr CM, Ames BN. (R)-alpha-lipoic acid reverses the age-associated increase in susceptibility
of hepatocytes to tert-butylhydroperoxide both in vitro and in vivo. Antioxid Redox Signal 2000 Fall;2(3):473-
83.
- Suh JH, Shigeno ET, Morrow JD, Cox B, Rocha AE, Frei B, Hagen TM. Oxidative stress in the aging rat heart
is reversed by dietary supplementation with (R)-(alpha)-lipoic acid. FASEB J 2001 Mar;15(3):700-6.
- Kawabata T, Packer L. Alpha-lipoate can protect against glycation of serum albumin, but not low density lipoprotein.
Biochem Biophys Res Comms 1994;203:99-104.
- Jacob S, Henriksen EJ, Schiemann AL, et al. Enhancement of glucose disposal in patients with type 2 diabetes
by alpha-lipoic acid. Arzneimittel-Forschung 1995;45:872-874.
- Jacob S, Henriksen EJ, Tritschler HJ, et al. Improvement of insulin-stimulated glucose-disposal in type 2 diabetes
after repeated parenteral administration of thioctic acid. Exp Clin Endocrinol Diabetes 1996;104:284-288.
- Kehler W, Kuklinski B, Ruhlmann C, Plotz C. Diabetes mellitus-a free radical associated disease: Effects of
adjuvant supplementation of antioxidants. In: Gries FA, Wessel K, eds. The role of antioxidants in diabetes mellitus:
Oxygen radicals and antioxidants in diabetes. Frankfurt am Maine: pmi. Verl-Gruppe;1993:33-35.
- Garrett NE, Malcangio M, Dewhurst M, Tomlinson DR. Alpha-lipoic acid corrects neuropeptide deficits in diabetic
rats via induction of trophic support. Neurosci Lett 1997;222:191-194.
- Nagamatsu M, Nickander KK, Schmelzer JD. Lipoic acid improves nerve blood flow, reduces oxidative stress, and
improves distal nerve conduction in experimental diabetic neuropathy. Diabetic Care 1995;18:1160-1166.
- Ziegler D, Hanefield M, Ruhnau KJ, et al. Treatment of symptomatic diabetic peripheral neuropathy with the antioxidant
alpha-lipoic acid. A 3-week multicenter randomized controlled trial (ALADIN Study). Diabetologia
1995;38:1425-1433.
- Assadnazari H, Zimmer G, Freisleben HJ, et al. Cardioprotective efficiency of dihydrolipoic acid in working rat hearts
during hypoxia and reoxygenation. P nuclear magnetic resonance investigations. Arzneimittel-Forschung 1993;43:425-
432.
- Prehn JH, Karkoutly C, Nuglisch J, et al. Dihydrolipoate reduces neuronal injury after cerebral ischemia. J Cereb
Blood Flow Metab 1992;12:78-87.
- Wolz P, Krieglstein J. Neuroprotective effects of alpha-lipoic acid and its enantiomers demonstrated in rodent
models of focal cerebral ischemia. Neuropharmacology 1996;35:369-375.
- Filina AA, Davydova NG, Endrikhovskii SN, et al. Lipoic Acid as a means of metabolic therapy of open-angle
glaucoma. Vestn Oftalmol 1995;111:6-8.
- Ou P, Nourooz-Zadeh J, Tritschler HJ, Wolff SP. Activation of aldose reductase in rat lens and metal-ion chelation
by aldose reductase inhibitors and lipoic acid. Free Radic Res 1996;25:337-346.
- Maitra I, Serbinova E, Tritschler HJ, Packer L. Alpha-lipoic acid prevents buthionine sulfoximine-induced cataract
formation in newborn rats. Free Radic Biol Med 1995;18:823-829.
- Durr HP, Popp FA, Schommers W, eds. What Is Life: Scientific Approaches and Philophical Positions. World
Scientific CO USA River Edge NJ 2002:307-328.
|