Nutritional Drugs that Work
Alpha Lipoic Acid
International Medical Verities Association
Finding new medicines is crucial for pharmaceutical companies because over time, they gradually lose patent protection on drugs. So imagine the disappointment when Pfizer had to pull the plug on its potential wonder drug, torcetrapib. Pfizer, the world's largest pharmaceutical company, announced last week that it had abandoned all clinical trials, turning the company's nearly $1 billion investment into a total loss. The drug, which has been in development since the early 1990s, was supposed to raise so-called good cholesterol, and cardiologists had hoped it would reduce buildup of the plaque in blood vessels that can cause heart attacks. But as is often the case with an ever-expanding list of pharmaceuticals, this one kills too many people, meaning it just does not work. In clinical trials with torcetrapib there were 60 per cent more deaths in those who took the drug compared with those who took a placebo.
This drug, if it worked, would probably have been
the largest-selling pharmaceutical in history.
Dr. Steven E. Nissen
Magnesium chloride, on the other hand, does a good job of regulating cholesterol, and when combined with alpha lipoic acid (ALA)[i] yields a superb formula for combating heart disease.[ii] ALA[iii] and magnesium, as we shall see, are crucial substances for the treatment of diabetes that we all need to become much more familiar with. Together they are the ideal protocol for treating diabetic neuropathy,[iv] retinopathy, and other diabetic complications.[v] Dr. Andrew Cutler Hall pairs ALA with DMSA for chelation of heavy metals but we will find that pairing it with magnesium (and some other natural agents) is superior.
Also known as thioctic acid, ALA is a naturally occurring compound that is synthesized in small amounts by plants and animals, including humans. Alpha Lipoic Acid is a sulfurous fatty acid and was first discovered in the 1950s, and recognized it as an antioxidant in 1988. ALA would have been classified as a vitamin except for the fact that it can be synthesized within the human body. In foods it occurs as lipolylysine and not actual lipoic acid itself. This is then converted to dihydrolipoic acid during digestion. Early in life our bodies produce amounts sufficient to do its work, but as we age the amounts synthesized decreases. It is not easily obtained from foods in the amounts our bodies need.[vi] You'll never get any realistic amount out of food as broccoli (one of the best sources), for example, contains a mere 100 micrograms per 100 gram serving. This means you would have to eat over two pounds of broccoli to get one single milligram of lipolylysine to convert into alpha lipoic acid. But the ALA in foods and supplement form is easily absorbed and transported across cell membranes.
ALA is a rate-limiting coenzyme for ATP production
via the Krebs cycle; sensitizes cells to insulin.
ALA works on the cellular level to help produce energy. It acts as a coenzyme-a helper of enzymes-in the cell's major energy cycle, the Krebs cycle.[vii] As a coenzyme, ALA takes part in a multi-enzyme process preparing the fuel for the mitochondrion, the powerhouse of the cell. Without alpha lipoic acid, cells cannot utilize sugar to produce energy and they shut down. This makes alpha-lipoic acid a metabolic antioxidant, able to draw on the cell's own metabolism to magnify its protective effects and that of other antioxidants.
According to Dr. Burt Berkson, the doctor appointed by the FDA as the principle investigator for intravenous use of ALA, and author of The Alpha Lipoic Acid Breakthrough:
"Several factors make ALA the ultimate antioxidant.[viii] One very basic reason is that ALA is both a hydrophilic and lipophilic molecule. Because it is hydrophilic, it is soluble in blood and other watery body fluids. Because it is lipophilic, it is also soluble in fats. In contrast, vitamin C is only hydrophilic and vitamin E is only lipophilic. These qualities make ALA an ideal antioxidant that works double duty. It prevents free radical damage in every setting regardless of whether it is the brain fluids, the blood, stored fat, the heart, the pancreas, the kidneys, bone, cartilage, the liver, and for that matter every cell in every organ. ALA can perform the same functions in the watery fluids of the cell and in the blood and other aqueous fluids that come in contact with the body's tissues, just like vitamin C. Because of these remarkable characteristics, ALA can also easily pass through the blood-brain barrier and increase brain energy availability."
Inflammation, ALA and Magnesium
According to Dr. Berkson "ALA may be effectively used to prevent and treat many of the medical conditions associated with the oxidative stress that occurs when the body is overwhelmed by toxic chemicals. This list includes diabetes, toxic states, hyperlipidemia, heart disease, stroke, cataracts, organ damage, cancer, neurological disease, and radiation damage." All antioxidants are anti-inflammatory agents, but lipoic acid is regarded as an especially effective anti-inflammatory.
Alpha-Lipoic has a chiral center, which means it can be found in 2 mirror image
forms (S- and R-a-lipoic acid) that cannot be superimposed on each other.
Dr. June Paul Ridker, a Harvard cardiologist said, "We have to think of heart disease as an inflammatory disease, just as we think of rheumatoid arthritis as an inflammatory disease." He asserted that it's inflammation that leads to pieces of arterial plaque breaking off and causing heart attacks, even in people with normal or low cholesterol. The growing understanding of the major role that oxidative stress and inflammation play in the development and progression of various pathologies will play a major role in bending the river of medicine towards treatments that actually work and help people instead of hurt them.
ALA inhibits the "hydroxyl radical."[ix] The hydroxyl
radical is considered to be the most damaging of
the free radicals due to its ability to initiate heart disease.
Recognizing the role of inflammation in arteriosclerosis represents a huge paradigm shift for cardiologists. Until recently the American College of Cardiology, The American College of Physician's and The American Heart Association tended to largely ignore the involvement of inflammation in heart attacks and strokes. Inflammation is a prominent component of many diseases, including primary retinal degenerations, insulin resistance, and diabetes.
Once we understand the critical importance of
inflammation and glutathione depletion in brain diseases,
we can take steps to prevent or even reverse the damage.
Dr. David Perlmutter
Inflammation and systemic stress are central attributes of many pathological conditions. Thus if we find a way to directly and safely reduce inflammation and systemic stress we have found a potent medical approach that would be effective across a wide range of pathologies.
Inflammation is the missing link to explain the role
of magnesium in many pathological conditions.
Dr. A. Mazur et al[x] have shown, in experimentally induced magnesium deficiency in rats, which after only a few days of deprivation a clinical inflammatory syndrome develops that is characterized by leukocyte (white blood cell) and macrophage activation, release of inflammatory cytokines and excessive production of free radicals. "Magnesium deficiency induces a systemic stress response by activation of neuro endocrinological pathways," writes Dr. Mazur. "Magnesium deficiency contributes to an exaggerated response to immune stress and oxidative stress is the consequence of the inflammatory response," he continued.
Increases in extracellular magnesium concentration cause a decrease in the inflammatory response while reduction in the extracellular magnesium results in cell activation. Inflammation causes endothelial dysfunction and activated endothelium facilitates adhesion and migration of cancer cells.[xi]
Please note that although magnesium chloride is probably the most powerful safe nutritional drug on earth, with a largely unexplored clinical potential to resolve many medical conditions, it is not appropriate to consider drugs or nutritional agents in isolation.[xii] It is generally a mistake to try to isolate drugs the way the pharmaceutical companies do and pin the hopes of millions on a single medication. We need safe protocols that involve careful study and planning. A focus on combination therapy enables us to encompass and manage multiple risk factors. Multidimensional etiologies call for multiple therapeutic interventions. Whether or not to use combination therapy is no longer the question; rather physicians are now asking which combinations to use for which risk factors. Though this chapter is specifically about ALA, one cannot talk about using it alone to treat diabetes and heart disease or any other disorder. What we are trying to do here is lay the groundwork for rational drug designs and forms of treatment that reach escape velocity from the obsession to lay all the focus on one drug or nutritional substance at a time. This combination or protocol approach is theoretically impossible with pharmaceutical drugs because it is impossible to predict how toxic chemicals and poisons (drugs) will mix together. It is also not ethical to try to study such combinations and effects for all such studies involve poisoning the subjects studied with multiple poisons.
The growing understanding of the major role that oxidative stress and inflammation play in the development and progression of various pathologies is especially important in neurological disorders for inflammation is a central key to understanding and treating neurodegenerative diseases. The "brain on fire" or "sparks," as Dr. Rashid Buttar calls it when mercury penetrates the blood brain barrier are actually important images that mirror what is happening in many brains. Dr. Buttar uses this image to accurately describe effect of each molecule and atom of mercury which acts like a spark that sets the brain on fire with inflammation.
The Eternal War
Free Radicals Vs Antioxidants
Lipoic acid is beneficial in reducing ischemic-reperfusion
injury by direct action as well as by glutathione
protection and xanthine oxidase inhibition.[xiii]
There's a great struggle going on in our bodies, some call it a war that we and especially our children, who are more vulnerable, are losing as a broad range of chemical exposures increase through time. Every day, countless trillions of battles are occurring on a cellular level. When we lose too many battles inside of a cell it dies or goes dysfunctional. When we continue to lose we become diseased. According to Dr. Richard Passwater, in his book Lipoic Acid, The Metabolic Antioxidant, losing this struggle that pits free radicals[xiv] against antioxidants can result in approximately 80 different age-related diseases, including cancer, heart attack, stroke, rheumatoid arthritis, cataracts, and Alzheimer's disease.
The actual chemistry of the compound occurs at the dithiol (referring to the two sulfur atoms). During the step in the krebs cycle where pyruvate is converted to acetyl CoA, lipoic acid performs oxidation/reduction chemistry by acting first as a hydrogen acceptor to form dihyrolipoic acid (its reduced metabolite) and then later as a hydrogen donor (whereby it re-forms lipoic acid).
ALA has the ability to salvage and recycle other
antioxidants such as vitamin C, vitamin E, and glutathione.[xv]-[xvi]
Since it is soluble in both water and fat, ALA can move into all parts of the cell to neutralize free radicals. Vitamin C, on the other hand, is limited to the watery parts of cells because it is soluble only in water; while vitamin E is soluble only in fat and sticks to the fatty parts of cells. ALA interferes with the biochemical and physical damage caused by free radicals because it recycles and generates additional glutathione as well as vitamin C and E thus preventing deficiencies.
Vitamins E and C also inhibit the oxidation of LDL cholesterol that,
when found in excess, is laid down within the arterial wall. Alpha
lipoic acid recycles vitamin E and vitamin C and thus prevents
the oxidation of LDL by making these substances useful again.
Dr. Burt Berkson
Studies have shown that levels of the major intracellular antioxidant "Glutathione" is typically about
50% lower in children with autism Impairment in glutathione metabolism has been proven in diabetes
with the rate of outward transport of glutathione disulfide in diabetics decreased to approximately 70%
of that of normal controls.[xvii] Glutathione, which is produced by every cell in the body, is responsible
for a number of functions including removing or neutralizing dangerous substances that we are exposed to
on a daily basis, including toxic metals. Toxins, pollution, disease, stress, and poor diet can all contribute
to loss of glutathione. When glutathione levels reach a critically low level, we are much more
vulnerable to toxins and immune dysfunction.
There is evidence that glutathione depletion can lead to neurological damage; low levels of glutathione have been found in
Parkinson's disease and cerebral ischemia-reperfusion injury.
Some children with autism are poor detoxifiers relative to normally developing children, and in particular, have trouble excreting toxic metals, thus are much more defenseless to the toxic chemicals injected into them via the childhood immunization program. Toxic metals that are injected but not eliminated will build up in the brain and other body tissues causing all kinds of problems. Parkinson's patients also show low levels of glutathione not only in the brain but also in the liver thus they also tend to be poor detoxifiers.
ALA has the ability to continuously provide cysteine,
the rate-limiting amino acid for glutathione production.[xviii]
Dr. David Perlmutter, a neurologist and director of the Perlmutter Health Center in Naples, Florida, and the author of the book BrainRecovery.com - Powerful Therapy for Challenging Brain Disorders, has been injecting patients with glutathione to treat Parkinson's symptoms with profound results. Within less than an hour of intravenous injection, Parkinson's patients experienced an almost complete restoration of the ability to walk, turn around and move their arms. Perlmutter calls this "the glutathione miracle." I have seen similar results over a period of two weeks with only a minimal application of transdermal magnesium chloride therapy.
ALA and Chelation of Heavy Metals
ALA restores the body's natural antioxidant defense
mechanisms, thus preventing a great amount of oxidative stress.
According to Jones and Cherian, an ideal heavy metal chelator should be able to enter the cell easily, chelate the heavy metal from its complex with metallothionein or other proteins, and increase the excretion of the metal without its redistribution to other organs or tissues.[xix] According to Dr. Lyn Patrick "ALA satisfies at least two of the above criteria; i.e., absorption into the intracellular environment and complexing metals previously bound to other sulfhydryl proteins. ALA when found unbound in the circulation, is able to trap circulating heavy metals, thus preventing cellular damage caused by metal toxicity. The fact that free ALA crosses the blood brain barrier is significant because the brain readily accumulates lead and mercury, where these metals are stored intracellularly in glial tissue."
ALA is able to significantly alter the
oxidative stress induced by lead toxicity.[xx]
The ability of ALA to bind inorganic mercury has been compared to glutathione and to DMPS, DMSA and EDTA. It was shown in one study related to kidney toxicity that DMPS removed 86 percent of mercury, DMSA 65 percent, glutathione 50 percent, ALA 35 percent and EDTA only 20 percent.[xxi] The classic chelators (DMPS, DMSA and EDTA) are limited by high cost, difficulty of use and inefficient removal of CNS toxic metal deposits, not to mention significant side effects especially for DMSA and DMPS.
Microorganisms tend to set up their housekeeping in those body
compartments that have the highest pollution with toxic metals.
Redox-active metal ions, such as free iron and copper, can induce oxidative damage by catalyzing reactions that generate highly reactive free radicals. Compounds that chelate (bind) free metal ions in a way that prevents them from generating free radicals offer promise in the treatment of neurodegenerative and other chronic diseases, in which metal-induced oxidative damage plays a key role.
People with more magnesium and less copper in their
blood could reduce their risk of death from cancer
by as much as 50 per cent, says a new study from France.[xxii]
A very recent study of children living in the area affected by the Chernobyl disaster showed that ALA prevents radiation damage.[xxiii] This is more important than most think especially since the United States has used its depleted uranium weapons on several battlefields. It is also very important because the rising tide of mercury and other toxic chemicals is threatening the environment and everything in it. Though the government has used epidemiologic studies to dismiss the relationship between mercury and autism many scientists see it very differently. The need for a safe chelator of mercury and a range of other toxic metals and chemicals cannot be understated. It is simply imperative in the age of toxicity.
Scientists show, for instance, that serious blood vessel disease can develop when copper levels are too high in diabetics. Some researchers believe that excess levels of copper may be another contributing factor to atherosclerotic vessel disease. Alpha Lipoic Acid has been demonstrated to be an excellent chelator of copper. ALA binds (chelates) with excess copper, rendering it harmless and eliminating it from the body as it does with mercury and arsenic. Other toxic metals that ALA can chelate include cadmium, zinc, calcium and lead.
ALA has also been shown to protect against cisplatin-induced renal
damage in rats by binding to platinum that is responsible for renal toxicity.
Dr. Lyn Patrick wrote, "Glutathione, as both a carrier of mercury and an antioxidant, has three specific roles in protecting the body from mercury toxicity.[xxiv] First, glutathione, specifically binding with methylmercury, forms a complex that prevents mercury from binding to cellular proteins and causing damage to both enzymes and tissue. Glutathione-mercury complexes also reduce intracellular damage by preventing mercury froth entering tissue cells and becoming an intracellular toxin. Glutathione-mercury complexes have been found in the liver, kidney, and brain, and appear to be the primary form in which mercury is transported and eliminated from the body. The transport mechanism is unclear, but complexes of glutathione and mercury are the predominant form of mercury in both the bile and the urine."
Because ALA is the only antioxidant that can easily get into the
brain it is being used as a chelator of mercury in autistic children.
ALA and Diabetes
Hyperglycaemia-induced mitochondrial overproduction
of reactive oxygen species (ROS) is central to the
pathogenesis of endothelial damage in diabetes.
Recent evidence indicates increased oxidative damage in Type 1 and Type 2 diabetes mellitus as well as deficits in antioxidant defense enzymes and vitamins. Mechanisms have been considered whereby hyperglycemia can increase oxidative stress, and change the redox potential of glutathione. It seems that reactive oxygen species can cause hyperglycemia. It is argued that oxygen, antioxidant defenses, and cellular redox status should now be regarded as central players in diabetes and the metabolic syndrome.[xxv]
Oxidative stress is increased in the retina in diabetes, and it is considered to play an important role in the development of retinopathy. Alpha-Lipoic acid, has been shown to have beneficial effects on polyneuropathy and on the parameters of oxidative stress in various tissues, including nerve, kidney, and retina. Long-term administration of alpha-lipoic acid has beneficial effects on the development of diabetic retinopathy via inhibition of accumulation of oxidatively modified DNA and nitrotyrosine in the retina.[xxvi] R-(+)-alpha-lipoic acid has been shown to prevent microvascular damage through normalised pathways downstream of mitochondrial overproduction of ROS, and preserves pericyte coverage of retinal capillaries, which may provide additional endothelial protection.[xxvii]
Reduced insulin action leads to neurodegeneration.
A Toronto-led team of researchers has recently discovered a trigger for Type 1 diabetes, a breakthrough that has long evaded scientists and could lead the way to preventing the disease. The team found that abnormal nerve endings in the insulin-producing cells of the pancreas initiated a chain of events that caused Type 1 diabetes in mice. When they removed the nerve cells, the mice did not develop the disorder. That means diabetes may be a disease of the nervous system, not just an autoimmune disease, said Dr. Hans Michael Dosch, a senior scientist at the Hospital for Sick Children and the study's main investigator.
ALA prevents free radical damage, a major cause of
diabetic neuropathies. And ALA directly neutralizes
and destroys free radicals in the nervous tissue.
Dr. Dosch identified a control circuit between islet cells and their related sensory nerves. Disrupting this circuit led to inflammation around the islets and eventually to their destruction. Without these nerve cells, the mice could not make insulin. "This control circuit is the real cause of diabetes," Dosch said. We see jeer inflammation that can be treated effectively with magnesium and ALA.
"We now have 4-month-old mice that are non-diabetic that used to be diabetic" - a period equivalent to six to eight years in humans.
Dr. Hans Michael Dosch
Thirty percent of patients taking Zyprexa gain 22 pounds or more after a year on the drug, and some patients have reported gaining 100 pounds or more. Critics, including the American Diabetes Association, have argued that Zyprexa, introduced in 1996, is more likely to cause diabetes than other widely used schizophrenia drugs. Obesity claims more lives and drains more of the healthcare budget than smoking. Obesity is linked to diabetes, arthritis, heart disease, stroke and certain cancers. It inflates healthcare costs by 36 percent and medication costs by 77 percent. After reading the chapter on diabetes and chemical and "drug" poisoning one begins to get a different sense about how factors other than sugar are playing principle roles in the dramatic rise of diabetes in the general population.
The development of insulin-dependent diabetes mellitus
is thought to be dependent on the interaction of
environmental agents with the pancreatic beta cells.[xxviii]
University of Calgary
There are two mammoth factors linked to the horrendous rise in diabetes in adults and children that the western medical establishment is not paying attention to. The first is deficiency in magnesium, and the other is chemical poisoning. Another large contributing factor that no one is thinking of that contributes to the onset of diabetes is dehydration. Certainly our cells are more vulnerable to chemical poisoning when in a dehydrated state. This important subject will be covered in depth in both The Waters of Life and New Paradigms in Diabetic Care.
Diabetes is one of the deadliest diseases in the world today and is spreading like wildfire. According to the medical establishment it has no cure. But paying attention to the true causes suggests safe and effective treatments. So effective that it seems in certain cases appropriate treatments will offer a cure. Diabetes and most chronic diseases today demand multi-dimensional thinking and diagnosis. Multiple causes/etiologies should be the watchwords of medicine in the 21st century. (Certainly there are other contributing factors not mentioned in this chapter.)
Among the most pernicious substances ever created is a group of chemicals known as POPs or Persistent Organic Pollutants. Among them: DDT, dioxins, PCBs and Chlordane. And even though twelve POPs -- the so-called "dirty dozen" were restricted or banned by international convention in 2003, they continue to pose a threat to people and wildlife because POPs accumulate in the food we eat. Virtually every person on the planet has POPs in their body and the chemicals have been linked to cancers, birth defects and disabilities. Now a group of researchers in Korea have found strong evidence linking POPs and diabetes.
Dr. David Carpenter, Professor of Environmental Health and Toxicology at the State University of New York at Albany, reviewed the Korean study and said, "Well, one considers individual pollutants the magnitude was between three and five fold increased risk but the most striking observation was when they considered the sum of all six pollutants that they monitored and they selected pollutants that we all have in our bodies so that very few individuals had levels below the level of detection. Under those circumstances they were getting increased risk of the order of thirty-eight fold which is absolutely enormous."
The amount of persistent organic pollutants in each person's body
is a reflection of their diet, where they live, what the concentration
of these substances is in the air they breathe, and probably
related to how rapidly they metabolize these compounds.
Dr. David Carpenter
Dr. Carpenter continued saying, "The most interesting observation in this paper is that there was no relationship between being obese and developing diabetes in those persons that did not have high levels of these organic pollutants in their bodies. It may well be that people that are obese eat much more animal fat than people that are not obese and these persistent organic pollutants are all found in animal fats. So the question really is whether it is the obesity that leads to the diabetes or rather the presence of these persistent organic pollutants. It may well be that it's the pollutants that cause the diabetes, not the obesity."
In the human body these compounds last about
ten years before you get rid of half of them.
In the environment they're even more persistent.
Dr. David Carpenter
Food is not considered junk just because of high fat or sugar content, there is a long list of poisonous chemicals used by the food industry that are striking people down. And there are many serious nutritional deficiencies in today's food that diminish the bodies capacity to deal safely with these chemicals and heavy metals - with magnesium and selenium deficiencies at the top of the list. Magnesium deficiency is a predictor of diabetes; diabetics both need more magnesium and lose more magnesium than most people. In two new studies, in both men and women, those who consumed the most magnesium in their diet were least likely to develop type 2 diabetes, according to a report in the January 2006 issue of the journal Diabetes Care.
Alpha-lipoic acid attenuates hyperglycemia and prevents
glomerular mesangial matrix expansion in diabetic rats.
The combined antioxidant and hypoglycemic actions
of LA contribute to its utility in preventing renal
injury and other complications of diabetes.[xxix]
Researchers have found that administration of ALA (intravenously or orally) is effective in alleviating many of the problems accompanying diabetes.[xxx]-[xxxi]-[xxxii] And no wonder, people with diabetes mellitus have characteristically low levels of glutathione in their blood and ALA is a key dietary/drug substance that brings glutathione levels back up. The accumulation of high levels of free radicals, a common development in diabetics, results in depletion of glutathione, the destruction of cell membranes, and nucleic acid damage.
Alpha Lipoic acid prevents hypertension, hyperglycemia,
and the increase in heart mitochondrial superoxide production.[xxxiii]
What is especially interesting about ALA is that it also has an insulin like effect. It does not take the place of insulin, but it does mimic part of its function. ALA has been shown to increase glucose uptake by mimicking insulin and shuttling it to Glut-4 receptors, which is one of the 5 GLUT-transporters necessary for glucose uptake. Because ALA has increased the number of Glut-4 receptors on the outside of muscles, more glucose can be absorbed. Unlike the other transporters, GLUT-4 is regulated by insulin. Lipoic acid supplementation in micromolar concentrations increases insulin stimulated glucose transport by increasing the activity of the insulin signaling pathway and the expression of GLUT-4 transporters at the genomic level.
In plain English this basically says that ALA allows our cells to more efficiently take up nutrients (both food nutrients and dietary supplements), which would obviously enhance their effectiveness. It is lipoic acid's direct involvement in the insulin signaling pathway that makes it unique among current anti-hyperglycemic treatments.[xxxiv]
Animal experiments have already shown that ALA can also prevent the development of Type I (insulin-dependent) diabetes and enhances glucose uptake in Type II (non- insulin-dependent) diabetes.[xxxv]-[xxxvi] In studies on obese rats, ALA was shown to reduce body weight, decrease food intake and increase energy expenditure. It exerts its effects by suppressing hypothalamic AMP-activated protein kinase. Additional testing on obese rats showed that glycosuria occurred at 40 weeks of age and was completely prevented by the administration of ALA. Beta cell destruction was completely prevented. In these same studies on obese rats Alpha lipoic acid also reduced triglyceride accumulation in skeletal muscle and pancreatic islets. These results indicate that alpha lipoic acid may also prevent diabetes mellitus in obese diabetes-prone rats by reducing lipid accumulation in non-adipose tissue as well as in adipose tissue.
And according to Dr. Burt Berkson, ALA has also been demonstrated to stop the adhesion of macrophages to the artery wall and thus, theoretically and in proper doses, should be able to stop atherosclerosis (atherosclerotic vascular disease, which is the leading cause of death in the Western World.) in its tracks. Macrophages are a type of immune cell, found in the body's tissues and organs which rid the body of worn-out cells and other debris, secrete powerful antigen-destroying chemicals, and play an important role in activating T cells. Cytokines are soluble molecules produced by cells that serve as mediators of intracellular reactions and biological response modifiers.
I hope it is obvious that what we have done here is outlined a protocol for diabetes that outdistances anything imagined up to this point by either allopathic or alternative medicine. It would be intensive magnesium chloride baths (or body spraying - transdermal magnesium therapy) combined with and ALA based formula like Chelorex that goes the entire nine yards with supportive agents. Mix in spirulina with its GLA as a super food source, the coenzyme Q10 and clay for oral use to clean the intestines, plenty of pure water, organic produce, sensible eating and exercise and you have the best shot of dealing with diabetes and its complications.
If Dr. Burt Berkson can reverse a diabetic patient with ALA alone imagine what can be done with treatments that address magnesium deficiencies, detoxification and chelation all put together. Of course we cannot say we have come up with a cure for diabetes but without stretching our necks too far we can assert that we have found the best treatment approach that will prevent diabetes, cure some of the complications like diabetic neuropathy, in general diminish symptoms and in some cases entirely reverse the progress of the disorder itself.
Dr. Berkson wrote, speaking about one of his elderly diabetic patients, "After three weeks of oral ALA treatment, his health began to change for the better. First he noticed that he was able to read without glasses. At the same time, he noticed that the constant burning in the soles of his feet disappeared. It appeared that the ALA, working at the basic cellular level, improved factors associated with the deterioration of his eyesight and also had a positive effect on his peripheral nerve pains." For another patient on the verge of scheduling extreme surgery for stomach pains he said, "The man was accepted into the program and within three weeks the neuropathies started to disappear. Relieved of his condition, he was prescribed a good diet, nutritional supplements, and exercise. He soon developed increased energy and felt great. His diabetic conditions have not returned."
In my book Transdermal Magnesium Therapy there are several chapters on diabetes and magnesium showing it is not only important in treating and preventing diabetes, it is essential. After reviewing the science on both magnesium and ALA we can only conclude that the two together offer exciting new possibilities in diabetic care. But even then other supporting agents are more than helpful, they too are essential.
Even though magnesium contributes greatly to the body's ability to remove toxic poisons and heavy metals it is not a substitute for other substances that directly chelate metals. I personally use Chelorex (Science Formulas)[xxxvii] developed by Dr. Alan Greenberg for natural chelation because it has a list of substances that work together synergistically to naturally raise glutathione levels and chelate a long list of heavy metals, including uranium. Chelorex has what I call The Golden Triangle of Natural Chelation and at the head of that triangle is ALA.
It is my opinion that we can expect miracles in medicine to occur on such a frequent basis that they will no longer be considered miracles if we follow the path of medical truth. The important point is that a short list of natural and semi-natural substances will serve humanity in a way the pharmaceutical companies and their drug-pushing doctors never will. Reluctance on the part of conventional practitioners to embrace or even consider natural approaches is typically justified by statements indicating a lack of "peer reviewed studies" or "scientific evidence," but when it comes to magnesium and ALA this is not the case. Magnesium as a nutritional drug is backed by more research then any pharmaceutical drug because it has been studied by scientists all over the world for decades.
NAC (N-Acetyl Cysteine- oral)[xxxviii] gives so much value
for the money that the need for glutathione can be met for
days with this oral product. NAC (N-acetyl-Cysteine) is proven
more effective than IV glutathione for acute liver toxicity
Dr. Garry Gordon
When we read statements like this from Dr. Gordon we can begin to understand the tremendous potential of well-coordinated natural treatments and the reason I like Chelorex so much. Chelorex covers a lot of ground with selenium, magnesium, zinc, vitamin C and E, NAC, ALA, chlorella, cilantro, MSM, L-Glutamine and taurine. All the chelators most doctors use cause oxidative stress so you have to give lots of antioxidants. They also dangerously denude the body of vital minerals. Dr. Andy Hall Cutler, one of the leaders in the field of chelation, clearly endorses the use of vitamin C, E, zinc, magnesium and selenium. Dr. Cutler pioneered the use of ALA as a stand alone chelator and has used it extensively with DMSA. Dr. Greenberg's Chelorex is the only formula that combines ALA with cilantro, both natural substances that chelate and pass through the blood brain barrier. DMPS, DMSA and EDTA do not.
Ivy Greenwell, writing for Life Extension Magazine said, "It has been known for almost a decade that lipoic acid effectively inhibits the replication of the AIDS virus in vitro. This is not surprising in view of our knowledge that lipoic acid inhibits the activation of Nuclear Factor kappa B (NFkB), which is believed to play an important role in the activation of the HIV virus. Essentially, the latent virus is activated by certain inflammatory cytokines that result from the activation of NFkB. These cytokines include Tumor Necrosis Factor alpha (TNF alpha)-hence the goal of reducing TNF alpha, and the similarity between alternative treatments against AIDS and hepatitis, Dr. Patrick pointed out. Both protocols emphasize lipoic acid, selenium and a combination of various other antioxidants. In addition, many AIDS patients are co-infected with Hepatitis C. "All AIDS patients need liver support," Patrick said. In addition to 500 mg of lipoic acid/day, she also uses silymarin, shown to be remarkably effective in restoring liver health."
The core of my personal health and longevity program is heavy daily doses of natural magnesium chloride applied transdermally, along with spirulina and Chelorex. Even calcium bentonite clay for oral intake is in that program. They make up the core of the protocol I will present later this year in my upcoming book Survival Medicine for the 21st Century. Believe me the day is going to come that we all will wish we had the foresight to stock up on survival medicines, for not only are our economic lives going to change drastically but:
Everything is slowly being in put in place for global laws which will
affect all countries - so called 'harmonization'. The drug companies
are desperate to stem the tide of popularity of natural medicine
and are leaning on governments to create legislation against them.
(A must see video on Codex)
This means there are people out there who have a vested interest in keeping people sick. The sickness, insanity and awful terrorism of the pharmaceutical industry are accepted lamely by the masses yet it was not too long ago that many pushed the American government (and pushed hard) to keep their hands off of peoples' right to choose the supplements they want.
Today, in Europe and America wherever chemicals are likely to become the subject of criticism, the companies move in, balancing, ropagandizing, controlling, mediating protests, funding pseudo-scientific research, buying people off and funding social ventures to enhance their reputation.[xxxix]
Unfortunately for the public that the western medical establishment is against their principle to use safe medicines like ALA[xl] and magnesium chloride. Both are extremely useful in treating disease and protecting the body against the daily assaults that lead to disease and aging. It is also unfortunate to be living in an age where our access to such natural and safe substances cannot be taken for granted. Health This freedom is being threatened by new laws[xli] that once again sustain a most dangerous form of medicine, one that assumes the best and most appropriate way to treat disease is to poison people with toxic drugs.
We are now in a position to witness the unfolding of the
greatest medical tragedy of all time - never before in history
has the medical establishment knowingly created a life threatening
nutrient deficiency in millions of otherwise healthy people.
Dr. Peter H. Langsjoen
Dr. Langsjoen is talking here specifically about statin drugs and the fact that they dinminish CoQ10 levels in the body, which is another important antioxidant. The case is the same for magnesium where we have a medical establishment ignoring the obvious denying the public the knowledge and option of the most necessary of all treatments. There are safe and effective answers that can help us tremendously in our fight against chemical toxicity and the oxidative stress that leads to premature aging and chronic disease.
ALA and magnesium are the safest and most effective dietary drugs that in reality are not drugs at all. Oxygen and water are essential for life and health and God forbid the day when the medical establishment lays claim to these substances demanding we get a prescription for their use. It's the same with magnesium and ALA, both are essential substances needed for life. Yes they can be injected and thus claimed by allopathic doctors as part of their natural domain and both can save lives in the emergency room. But the need for these two substances is universal meaning they need to be taken by the general population in relatively large quantities. They need to remain in the public domain of supplements that do not require a doctor to administer them.
Mark Sircus Ac., OMD
Director International Medical Veritas Association
International Medical Veritas Association
Copyright 2006 All rights reserved.
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[i] 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. Alpha-lipoic acid, also known as thioctic acid, is the newest kid on the antioxidant block. Alpha-lipoic acid (ALA) was first isolated in 1953 and was quickly discovered to be a very important cofactor in the Krebs cycle (citric acid cycle), the body's main process for converting carbohydrates into energy. ALA is a medium length (8 carbon atoms) fatty acid containing two sulfur atoms. It is readily synthesized in the body and is well absorbed from the diet through the stomach and intestines. Liver and yeast are especially good dietary sources of ALA. ALA is the oxidized form of dihydrolipoic acid (DHLA), is water-soluble, and is found in varying concentrations in all muscles and internal organs.In 1959 it was discovered that both ALA and DHLA are powerful antioxidants. ALA scavenges hydroxyl radicals, singlet oxygen and hypochlorous acid, can remove heavy metals by chelation and regenerates other antioxidants like glutathione, vitamin C, ubiquinol (coenzyme Q10) and indirectly, vitamin E. DHLA has similar properties
[ii] Heart attacks and strokes involve a disruption of the oxygen supply to the affected areas. When the oxygen supply is restored a burst of free radicals is produced which can cause additional tissue damage (ischemia-reperfusion injury). Animal experiments have shown that ALA and DHLA are effective in preventing or ameliorating ischemia-reperfusion injury. Cadenas, Enrique and Packer, Lester, eds. Handbook of Antioxidants, NY, Marcel Dekker, Inc., 1996, pp. 545-91
[iii] 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 is 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. 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.
[iv] ALA is approved in Germany for preventing and treating diabetic neuropathy. The effect may result from the antioxidant activity. ALA may also help reduce blood glucose, cataract risk, and damaging glycosylation of proteins. It also increases blood flow to peripheral nerves (Packer L, Antioxidant properties of lipoic acid and its therapeutic effects in prevention of diabetes complications and cataracts. Annals NY Acad Sci 1994;738:257-64; Nagamatsu M, et al, Lipoic acid improves nerve blood flow, reduces oxidative stress, and improves distal nerve conduction in experimental diabetic neuropathy. Diabetes Care 1995;18:1160-67; Jacob S, et al, Enhancement of glucose disposal in patients with Type 2 diabetes by alpha-lipoic acid. Arzneimittel Forschung 1995;45:872-74; Kawabata T and Packer L, Alpha-lipoate can protect against of serum albumin, but not low-density lipoprotein. Biochem Biophys Res Comm 1994;203:99-104) In a four-week, randomized, multi-centered trial, 74 patients with type 2 diabetes received either placebo or ALA at 600 mg once, twice, or three times daily. The results indicated that oral ALA may improve insulin sensitivity in type 2 diabetics (Jacob S, et al, Oral administration of RAC-alpha lipoic acid modulates insulin sensitivity in patients with type 2 diabetes mellitus: a placebo-controlled pilot trial. Free Radic Biol Med 27(3-4):309-314, August 1999).
[v] Konrad D. Utilization of the insulin-signaling network in the metabolic actions of alpha-lipoic acid-reduction or oxidation? Antioxid Redox Signal. 2005;7(7-8):1032-1039. (PubMed)
[vi] Good food sources of alpha-lipoic acid include spinach, broccoli, beef, yeast (particularly Brewer's yeast), and certain organ meats (such as the kidney and heart).
[vii] Most of the biochemical activity of ALA occurs in the mitochondria. ALA, thiamine, and niacin are co-factors of the enzyme complex that metabolizes pyruvate (under aerobic conditions) in order to generate ATP via the citric acid (Krebs) cycle and the electron transport cascade (Champe P and Harvey R, Lippincott's Illustrated Reviews: Biochemistry, 2nd ed. Philadelphia: J. B. Lippincott Company, 1994, p107).
[viii] 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.
[ix] The uncontrolled action of hydroxyl radicals the most damaging free radical by far can have devastating effects within the body. The hydroxyl radical is a third generation species of radical which is derived from hydrogen peroxide (HZ02), which, in turn, is derived from the superoxide radical through the action of the enzyme superoxide dismutase. Hydrogen peroxide is reduced to hydroxyl radicals by the enzymes glutathione peroxidase and catalase in the presence of transition metals such as iron or copper. Dr. Russell Reiter of the University of Texas Health Center in San Antonio, involved in anti-aging research explains the dangers thusly: "If the function of radicals is to destroy molecules and tissues, then the hydroxyl radical would be the radical's radical. It reacts at diffusion rates with virtually any molecule found in its path including macromolecules such as DNA, membrane lipids, proteins, and carbohydrates. In terms of DNA, the hydroxyl radical can induce strand breaks as well as chemical changes in the deoxyribose and in the purine and pyrirnidine bases."
[x] Mazur A, Maier JA, Rock E, Gueux E, Nowacki W, Rayssiguier Y. Magnesium and the inflammatory response: Potential physiopathological implications. Arch Biochem Biophys. 2006 Apr 19; PMID: 16712775Equipe Stress Metabolique et Micronutriments, Unite de Nutrition Humaine UMR 1019, Centre de Recherche en Nutrition Humaine d'Auvergne, INRA, Theix, St. Genes Champanelle, France.Arch Biochem Biophys. 2006 Apr 19
[xi] Magnesium and inflammation: lessons from animal models]
Clin Calcium. 2005 Feb;15(2):245-8. Review. Japanese.
PMID: 15692164 [PubMed - indexed for MEDLINE
[xiii] FREE RADICAL BIOLOGY & MEDICINE; Packer, L.; 19(2):227-250 (1995)].
[xiv] Chemicals such as drugs, food additives, and preservatives, as well as cigarette smoke, pollutants, sunlight, radiation, emotional stress, and rancid fats all contribute to the creating an army of free radicals.
[xv]ALA has increased plasma ascorbate, total glutathione, T-helper cells and helper / suppressor ratio in HIV-positive patients (Fuchs J, et al, Studies on lipoate effects on blood redox state in human immunodeficiency virus infected patients. Arzneimittelforschung. 1993 Dec;43(12):1359).
[xvii] A decrease in the levels of the reduced form of glutathione and an increase in the levels of glutathione disulfide were found in erythrocytes of diabetics. The activity of gamma-glutamylcysteine synthetase was significantly lower in diabetics than in normal controls. Data suggests that the impairment of glutathione metabolism weakens the defense mechanism against oxidative stress in erythrocytes of diabetics. Impairment of glutathione metabolism in erythrocytes from patients with diabetes mellitus. Murakami K, Kondo T, Ohtsuka Y, Fujiwara ; Metabolism, 1989 - ncbi.nlm.nih.gov
[xviii] Han D. Handelman G, Marcocci L, et al. Lipoic acid increases de novo synthesis of cellular glutathione by improving cystine utilization. Biofactors 1997;6:321-338.
[xix] Jones MM, Cherian MG. The search for chelate antagonists for chronic cadmium intoxication. Toxicology 1990;62:1-25.
[xx] Gurer H, Ozgunes H, Oztezcan S, Ercal N. Antioxidant role of alpha-lipoic acid in lead toxicity. Free Radic Biol Med 1999;27:75-81.
[xxi] Keith RI., 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.
[xxii] The research, published in the journal Epidemiology (Vol. 17, pp. 308-314), reports from the Paris Prospective Study 2, a cohort of over 4,000 men aged between 30 and 60 at the start of the study.
[xxiii] Korkina, L.G., et al. Antioxidant therapy in children affected by irradiation from the Chernobyl nuclear accident. Biochem. Soc. Trans., Vol. 21, 1993, p. 314S
[xxv] Radicals and oxidative stress in diabetes ;West I.C. Diabetic Medicine, Volume 17, Number 3, March 2000, pp. 171-180(10)
[xxvi] Diabetes. 2004 Dec; 53(12):3233-8. Effect of long-term administration of alpha-lipoic acid on retinal capillary cell death and the development of retinopathy in diabetic rats. Kowluru RA, Odenbach S.
[xxvii] Diabetologia. 2006 May;49(5):1089-96. Epub 2006 Mar 7. Effect of R-(+)-alpha-lipoic acid on experimental diabetic retinopathy.Lin J, Bierhaus A, Bugert P, Dietrich N, Feng Y, Vom Hagen F, Nawroth P, Brownlee M, Hammes HP. 5th Medical Clinic, University-Clinic Mannheim, Medical Faculty of the University of Heidelberg, Heidelberg, Germany.
[xxix] Melhem MF, Craven PA, Liachenko J, DeRubertis FR. Department of Pathology, VA Pittsburgh Healthcare System and University of Pittsburgh, J Am Soc Nephrol. 2002 Jan;13(1):108-16
[xxx] Sachse, G. and Willms, B. Efficacy of thioctic acid in the therapy of peripheral diabetic neuropathy. In: Gries, F.A., et al., eds. Aspects of Autonomic Neuropathy in Diabetes. Stuttgart, A. Thieme, 1980, pp. 105-8
[xxxi] Kilic, F., et al. Modeling cortical cataractogensis 17:in vitro effect of alpha-lipoic acid on glucose-induced lens membrane damage, a model of diabetic cataractogenesis. Biochem. Molec. Biol. Int.
[xxxii] Packer, L. The role of anti-oxidative treatment of diabetes mellitus. Diabetologia, Vol. 36, 1993, pp. 1212-13
[xxxiii] Midaoui AE. University of Montreal, Montreal, Canada. Am J Hypertens 2003 Mar;16(3):173-9. The present study was designed to investigate whether the effects of dietary supplementation with alpha-lipoic acid could prevent the increase in mitochondrial superoxide production in the heart as well as the enhanced formation of advanced glycation end-products (AGE) that are associated with the development of hypertension and insulin resistance in chronically glucose-fed rats.Sprague Dawley rats were either given or not given a 10% D-glucose solution to drink during 4 weeks, combined either with a normal chow diet or with alpha-lipoic acid supplemented diet. The oxidative stress was evaluated by measuring the heart mitochondrial superoxide production using the lucigenin chemiluminescence method. The formation of AGE was also assessed in plasma and aorta.Chronic administration of glucose resulted in a 29% increase in blood pressure, 30% increase in glycemia, 286% increase in insulinemia, and 408% increase in insulin resistance index. Chronic glucose feeding also resulted in a 22% greater mitochondrial superoxide anion production in heart and in an increase of 63% in AGE content in aorta. Increases in blood pressure, aorta AGE content and heart mitochondrial superoxide production were prevented in the rats fed glucose supplemented with lipoic acid. The simultaneous treatment with lipoic acid also attenuated the rise in insulin levels as well as in insulin resistance in the glucose fed rats.These findings demonstrate that alpha-lipoic acid supplementation prevents development of hypertension and hyperglycemia, presumably through its antioxidative properties, as reflected by prevention of an increase in heart mitochondrial superoxide anion production and in AGE formation in the aorta of chronically glucose treated rats.
[xxxiv] Am J Physiol Cell Physiol 279: C877-C890, 2000
[xxxv] Alpha-Lipoic acid prevents diabetes mellitus in diabetes-prone obese rats. Biochem Biophys Res Commun. 2005 Jan 7;326(1):197-202. Several lines of evidence have suggested that triglyceride accumulation in skeletal muscle and pancreatic islets is causally related to type 2 diabetes mellitus.
[xxxvi] Expert Opin Investig Drugs. 2004 Dec;13(12):1641-3. Obesity shortens life expectancy and is a risk factor for hypertension and Type 2 diabetes. When added to the standard chow of Sprague-Dawley or Otsuka Long-Evans Tokushima Fatty rats, alpha-lipoic acid (0.5% weight/weight) reduced body weight and food intake. alpha-Lipoic acid also increased whole-body energy expenditure. It exerts its effects by suppressing hypothalamic AMP-activated protein kinase. Long-term studies to determine whether these anti-obesity effects are maintained in animals are required before alpha-lipoic acid is considered for clinical trial in human obesity.
[xxxviii] Although little-known, N-acetylcysteine (NAC) is a powerful antioxidant and a powerful tool in maintaining immunity. It has been used since the 1960s as a mucolytic; that is, a substance that breaks up mucus, especially in lung tissue, and has also been used for years in hospital emergency rooms to counteract acetaminophen poisoning. Acetaminophen is not all that NAC detoxifies. It also detoxifies such heavy metals as mercury, lead, and cadmium (J. Clin. Pharmacol. 13 (1973): 332-6), herbicides such as paraquat (Rev. Respir. Dis. 143, no. 4 part 2 (1991): A731), and some environmental pollutants. Clinical trials in Europe have indicated that NAC may also offer protection against the flu and flu-like symptoms. Research into NAC also indicates that it may enhance the production of human T cells, an important part of the immune system.
[xxxix] Law M R, Morris J K, Weld N J. Environmental tobacco smoke exposure and ischaemic heart disease: an evaluation of the evidence. BMJ 1997; 315:973 Hackshaw A K, Law M R, Wald N J. The accumulated evidence on lung cancer and environmental tobacco smoke. BMJ 1997; 315: 980-8. Davis R M. Passive smoking; history repeats itself. (editorial) BMJ 1997; 315: 961-2.
[xl] No adverse effects have been reported in 30 years of clinical use in diabetes. Dosage up to 600 mg daily is non-problematic. Very low toxicity has been observed in animal studies. Safety in pregnant and nursing women has not been proven. Because ALA lowers glucose in diabetics, blood sugar monitoring is crucial in this condition. Sugar-lowering medicines should be adjusted accordingly to avoid hypoglycemic crises. ALA may reduce the metabolic consumption of other antioxidants (vitamins C and E). ALA works with vitamins B1 and B3
in cellular energy production.