Idebenone:

Idebenone The Ultimate Anti-Aging Supplement?
James South, MA

Idebenone (IDB) is a natural analog (variant) of one of lifes most essential biochemicals, coenzyme Q10 (CoQ10) (Fig. 1). CoQ10 is an important antioxidant component of the lipid (fatty) membranes that surround all cells, as well as the lipid membranes surrounding the various organelles (little organs), such as mitochondria and microsomes, inside cells.

CoQ10 is also an important member of the Electron Transport Chain (ETC) within mitochondria, the power plants contained in every cell (Fig. 2). Most of the oxygen we breathe is used inside the ETC to produce much of the ATP bioenergy that powers virtually every activity of our cells and bodies.

Without CoQ10, or a good substitute, human life quickly ends. Idebenone (IDB) may be a better CoQ10 that has been extensively researched for over 15 years.

CoQ10s Pro-Oxidant Action
When blood flow is seriously reduced to any part of the body -- due to heart attack, stroke, trauma, shock, or chronic poor blood circulation -- cellular and mitochondrial oxygen (O2) levels quickly drop in the affected region. Yet because O2 is seven-to-eight times more soluble in the lipid zones of cell membranes, compared to the watery compartments of the cell, there is still sufficient O2 remaining in the membranes of cells and organelles, as well as in the ETC, to auto-oxidize CoQ10. As the CoQ10 auto-oxidizes, hydrogen peroxide, superoxide and hydroxl free radicals are rapidly formed in massive numbers. These free radicals quickly damage cell/ organelle structure and function, as well as rapidly halt ATP energy generation by the ETC.

Brain and spinal cord cells are especially prone to such damage, and may be irreparably damaged or even destroyed within minutes.

Idebenone Superior to CoQ10
Enter IDB to the rescue! Studies have shown that under the same cellular low oxygen conditions that cause CoQ10 to act as a pro-oxidant producer of damaging free radicals, IDB prevents the free radical damage and maintains relatively normal cell ATP levels. In short, while IDB can effectively substitute for CoQ10s positive and life- essential functions, it doesnt have CoQ10s free radical-producing and energy-crashing dark side which can occur under hypoxic (low O2) conditions.

IDBs potential benefits fall into five categories: (1) antiaging, (2) energy enhancement, (3) cognition enhancement, (4) organ protector, and (5) protector against excitatory amino acid neurotoxicity.

Anti-Aging Benefits
The mitochondrial power plants produce over 90% of all cellular ATP bioenergy. They are also generally the richest sites in CoQ10 (or IDB). Mitochondrial DNA (mtDNA) allows mitochondria to reproduce themselves.

While the DNA in a cell nucleus comes from both our parents, mtDNA comes exclusively from our mothers mtDNA.

There are typically two or three copies of mtDNA in each mitochondrion, with an average 1000 mitochondria per cell. Because mtDNA exists in the heart of the fiery furnace where electron sparks are constantly leaking as ATP is produced in the ETC, mtDNA is far more prone to free radical electron damage than is the DNA in our cell nuclei that contains the blueprint for our entire organism.

At the same time, the repair capacity of mtDNA is much less than that of our cell nucleus DNA. As a consequence, over the course of a lifetime our mtDNA becomes ever more damaged, and the mitochondria produced therefrom become ever more ineffective at energy generation. Studies comparing heart tissue from young people with that from elderly people have shown almost no significant mitochondrial dysfunction in young hearts, with significant, often severe mitochondrial dysfunction in elderly hearts.

The cells that are most susceptible to mitochondrial energy depletion with advancing age are the brain, skeletal muscle and heart muscle cells. IDB thus offers a prime anti-aging effect here in several ways. Unlike CoQ10, even under the low O2 conditions that may occur periodically over a lifetime, IDB will serve as a powerful mitochondrial free radical quencher, lessening the ever-increasing mtDNA damage that occurs with age.

IDB will work even better than CoQ10 within the ETC to keep energy production high, even under hypoxic conditions. This is especially critical to brain and heart cells that may be rapidly damaged during low ATP production due to poor tissue oxygenation.

Energy Enhancement
Iron is a dual edged sword. It is absolutely essential for life, and plays a central role in ATP generation in the ETC. Yet iron can also be a powerful initiator of free radical production and cell structural damage, especially under conditions of low O2.

This occurs, for example, during stroke, and during the gradual onset of Parkinsons disease. Studies have shown that IDB can tightly couple oxidation to energy production. This prevents iron ions from wastefully and toxically, diverting O2 to producing free radicals inside the mitochondria, instead of energy.

Studies have shown that IDB can almost completely eliminate this, diverting 10% of cellular O2 away from toxic iron induced free radical generation, to beneficial ATP energy production under hypoxic conditions.

Mild cellular hypoxia can occur even from intense exercise, or even from mild exercise done by out-of-shape couch potatoes.

Idebenone and Cognition Enhancement
A variety of studies using brain cells (animal and humans) have shown IDBs ability to enhance brain structure and function.

Human and animal studies have demonstrated that IDB can enhance serotonin production, even under far less than optimal conditions, as e.g. with a very low tryptophan diet, or in patients with cerebrovascular dementia.

IDB has enhanced cholinergic nerve function and consequent learning ability even under hypoxic conditions, or when an anti-cholinergic drug (Scopolamine) was administered. IDB has increased cellular catecholamine (dopamine, adrenaline and noradrenanlin) production by enhancing cellular uptake of the precursor amino acid tyrosine.

IDB enhances long-term potentiation in hippocampal nerve cells, a key part of memory formation and consolidation. IDB has restored glucose (brain fuel) utilization and ATP production in ischemic (poor blood flow) rat-brain.

IDB has been shown to enhance general cerebral metabolism, lessen the damage from strokes, and has been used to treat Alzheimers and other dementias (Figures 2 and 3).

Like the original nootropic drug, piracetam, IDB has been shown to promote information transfer across the corpus callosum, the membrane separating the right and left brain hemispheres.

This, in turn, may promote the union/ integration of the logical (yang) and intuitive (yin) halves of the brain/ mind.

Idebenone - Organ Protector
As our organs age or are damaged, we age and are damaged. Over a lifetime, blood flow to our organs diminishes due to arteriosclerosis and less efficient heart pumping. This reduces O2 dependent energy production needed for repair, reproduction and normal function of the organ cells. Free radical damage accumulates over time, leaving ever more dead, dying or dysfunctional cells within organs.

At some point when a critical threshold is reached and too many cells within an organ are dysfunctional and can no longer sustain the organs life and function, then the organ--heart, brain, liver etc., fails.

IDB protects organs in many ways. It cushions them against hypoxic (low O2) and/ or ischemic (poor blood flow) damage. IDB enhances both normal and hypoxic ATP energy generation. Each cell in our organs must produce the energy it needs for life and health. Cells cannot borrow energy from each other.

Free Radical Quenching
IDB is a powerful antioxidant. Even more so than CoQ10. In some studies, IDB was 30 to 100 times more effective than vitamin E or vinpocetine as a free radical quencher within brain cells.

IDB lessens the free radical-induced mtDNA damage that accumulates, acceleratingly over a lifetime, slowing organ damage and aging.

A 1995 study in the Journal of Transplantation compared the organ-preserving effects of CoQ10 and IDB. The study measured free radical membrane lipid damage, cell protein damage and cellular energy production under hypoxic conditions.

IDB was dramatically more effective than CoQ10 at preserving liver tissue under conditions identical to that endured by whole livers harvested and stored (briefly) before transplant to another person.

The study recommended using IDB to increase the transplant viability of human livers donated for organ transplant. Why not use IDB to increase your own organ viability, while you still have the use of them?!

Idebenone Protects Against Excitatory Amino Acid (EAA) Neurotoxicity
Glutamic acid and aspartic acid are the two chief EAA neurotransmitters in the human brain. Without them we would be mental vegetables.

Yet under certain conditions, e.g. stroke or traumatic brain injury--excessive amounts of EAAs accumulate in the fluid surrounding brain cells, causing damage and even death to nerve and glial cells through free radical mechanisms.

EAA toxicity is at least partly responsible for the neurotoxicity of the recreational drug Ecstasy or MDMA. Studies over the past 30 years have also shown that excessive dietary intake of EAAs may also damage brain structure/ function, especially in children or EAA sensitive adults.

The two main dietary sources of EAAs are the flavor enhancer MSG (monosodium glutamate) and the artificial sweetener aspartame (Nutrasweet®). Also many processed foods (e.g. canned soups, dry roasted spiced peanuts, beef/ chicken bouillon, canned tuna, spices etc.) contain hydrolyzed vegetable protein, yeast extract, soy protein isolate and similar ingredients that are mostly EAAs.

In studies with various types of nerve cell, as well as oligodendroglial cells (which make up the protective myelin sheaths surrounding many nerves, the so-called white matter of the brain), IDB has shown dramatic protective effects against glutamate toxicity.

Summary
With all these powers, IDB should now rightfully take its place in the first rank of anti-aging/ nootropic/ energizer drugs, along with Hydergine, Piracetam, vinpocetine, acetyl-L-carnitine, deprenyl and GH3/ KH3 (and its one of my personal favorites!) So who can benefit from Idebenone? The answers are:

Healthy people, desiring cognitive enhancement and brain energizer effects (it synergizes well with piracetam, vinpocetine and Hydergine). 2 or 3 tablets (45 mg each) daily.
Stroke victims, wishing to improve memory, emotional or speech disturbances. 3 to 6 tablets (45 mg each) daily.
Alzheimers and cerebrovascular dementia patients. 4 to 6 tablets (45 mg each) daily.
Those preparing for major surgery, especially brain, heart, liver or kidney. Synergizes well with Hydergine. 4 to 6 tablets (45 mg each).
People with heart energetics problems, e.g. cardiomyopathy, ischemic heart disease, congestive heart failure. 3 to 6 tablets (45 mg each) daily.
People with myelination problems, e.g. multiple sclerosis or white matter stroke injury. 3 to 6 tablets (45 mg each) daily.
Those seeking to increase their general energy and vitality levels. 2 to 3 tablets (45 mg each) daily.
People with especially high endurance energy needs, e.g. cross country skiers, long distance runners, cyclists, swimmers etc. 3 to 4 tablets (45 mg each) daily.
Those at risk of EAA brain damage, e.g. people who routinely consume large amounts of aspartame sweetened foods/ drinks, or those who routinely eat MSG or hydrolyzed vegetable protein containing restaurant or prepared foods. 2 or 3 tablets (45 mg each) daily.
People wishing to enhance the brain serotonin benefits of tryptophan or oxitriptan (5-hydroxy-tryptophan) supplements or SSRI drugs, such as Prozac, Paxil, Zoloft or Luvox etc. 2 to 4 tablets (45 mg each) daily.
Those suffering acute or chronic liver damage from poison mushrooms, toxic chemicals, hepatitis etc. 2 to 4 tablets (45 mg each) daily.
People desiring a long haul broad-spectrum anti-aging drug. Synergizes well with deprenyl, Hydergine, GH3/ KH3. 2 or 3 tablets (45 mg each) daily.

Because of its synergy with other life extension drugs, those also taking any or all of Hydergine, Piracetam (and its analogues), vinpocetine, deprenyl, GH3/ KH3 may benefit from even just one 45 mg tablet a day, especially if taken regularly on a long-term basis. Because idebenone is fat-soluble, it is best taken with a fat-rich meal, or with lipid absorption-enhancing agents such as lecithin or phosphatidyl choline.

Numerous studies have shown that idebenone is well distributed throughout the body after absorption, accumulating in cellular and organelle membranes, as well as in the electron transport chain, exactly where it does the most good!

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