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Idebenone the ultimate anti-aging
drug?
by James South MA
Idebenone is a synthetic analog
(variant) of one of life's most essential biochemicals, coenzyme Q10 (CoQ10).
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, which are
the "power plants" of the cell. Most of the oxygen we breathe is used
inside the Electron Transport Chain
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, and Idebenone is a "better CoQ10"
that has been extensively researched the past 15 years.
CoQ10s pro-oxidant action
to
order
When blood flow is seriously
reduced to any part of the body, as in a heart attack, stroke, trauma, shock, or
chronic poor blood circulation- cellular/ mitochondrial oxygen levels
quickly drop in the affected region. Yet because oxygen is seven to eight times more
soluble in the lipid zones of cell membrane, compared to the watery compartments
of the cell, there is still su fficient oxygen remaining in the membranes of cells
and organelles, as well as in the Electron Transport Chain, 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 Electron Transport Chain.
Brain and spinal cord cells are
especially prone to such damage, and may be irreparably damaged or even
destroyed within minutes.
Why Idebenone is superior to
CoQ10
Enter Idebenone 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, Idebenone
prevents the free radical dam-age and maintains relatively normal cell ATP
levels. In short, while Idebenone can effectively substitute for CoQ10's
positive and life essential functions, it doesn't have CoQ10's free radical
producing and energy crashing "dark side" which occurs under hypoxic
(low oxygen) conditions.
Idebenone's potential benefits
fall into five categories; antiaging, energy enhancement, cognition enhancement,
organ protector and protector against excitatory amino acid neurotoxicity.
Idebenone The 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 Idebenone). Mitochondrial DNA (mtDNA) allows
mitochondria to reproduce them-selves.
While the DNA in a cell nucleus
comes from both our parents, mtDNA comes exclusively from our mother's mtDNA.
There are typically two or three
copies of mtDNA in each mitochondrion, with 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 Electron Transport Chain, 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. Idebenone thus offers a prime anti-aging
effect here in several ways. Unlike CoQ10, even under the low oxygen conditions that
may occur periodically over a lifetime, Idebenone will serve as a powerful
mitochondrial free radical quencher, lessening the ever-increasing mtDNA damage
that occurs with age. Idebenone will work even better than CoQ10 within the
Electron Transport Chain 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 episodes that occur due to poor tissue oxygenation.
Idebenone Energy enhancement
Iron is a "dual edged
sword." It is absolutely essential for life, it plays a central role in ATP
generation in the Electron Transport Chain. Yet iron can also be a powerful initiator of free radical
production and cell structural damage, especially under low oxygen conditions.
This occurs, for example, during
stroke, and during the gradual onset of Parkinson's disease. Studies have shown
that Idebenone can tightly couple oxidation to energy production. This prevents
iron ions from wastefully and toxically, diverting oxygen to producing free radicals
inside the mitochondria, instead of energy.
Studies have shown that Idebenone
can almost completely eliminate this, diverting 10% of cellular oxygen 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 Cognition
enhancement
A variety of studies using brain
cells, (animal and humans) have shown Idebenone's ability to enhance brain
structure and function.
Human and animal studies have
demonstrated that Idebenone 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.
Idebenone has enhanced
cholinergic nerve function and consequent learning ability even under hypoxic
conditions, or when an anti-cholinergic drug (Scopolamine) was administered.
Idebenone has increased cellular
catecholamine (dopamine, adrenalin and noradrenanlin) production by enhancing
cellular uptake of the precursor amino-acid tyrosine.
Idebenone enhances long term
potentiation in hippocampal nerve cells, a key part of memory formation and
consolidation. Idebenone has restored glucose (brain fuel) utilization and ATP
production in ischemic (poor blood flow) rat-brain.
Idebenone has been shown to
enhance general cerebral metabolism, lessen the damage from strokes, and has
been used to treat Alzheimer's and other dementias.
And like the original nootropic
drug; piracetam, Idebenone has been shown to promote information transfer across
the corpus callosum, the membrane separating the right and left brain
hemispheres.
This is 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 oxygen 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 a critical
threshold is reached when too many cells within an organ are dysfunctional, and
they can no longer sustain the organ's life and function.
Then the organ- heart,
brain, liver etc. fails.
Idebenone protects organs in many
ways, it cushions them against hypoxic (low oxygen) and/ or ischemic (poor blood
flow) damage.
Idebenone 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.
Idebenone The free radical
quencher
Idebenone is a powerful
antioxidant, more so than CoQ10, and in some studies is 30 to 100 times more
effective, than vitamin E or vinpocetine as a free radical quencher within the
brain cells.
Idebenone 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 Idebenone.
The study measured various factors, such as free radical membrane lipid damage,
cell protein damage and cellular energy production under hypoxia conditions.
The results showed Idebenone to
be 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
Idebenone to increase the transplant viability of human livers donated for organ
transplant.
Why not use Idebenone to increase your own organ viability, while
you still have the use of them!
Protection against excitatory
amino acid neuro toxicity
Glutamic acid and aspartic acid
are the two chief excitatory
amino acid 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 excitatory
amino acids accumulate in
the fluid surrounding brain cells, causing damage and even death to nerve and
glial cells through free radical mechanisms.
Excitatory
amino acid 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 excitatory
amino acids may also damage brain structure/ function, especially in
children or excitatory
amino acid sensitive adults.
The two main dietary sources of excitatory
amino acids 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 "hydrolized vegetable protein, yeast extract, soy protein
isolate" and similar ingredients that are mostly excitatory
amino acids .
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). Idebenone has shown dramatic protective effects against glutamate
toxicity.
Summary
With all these powers, Idebenone
should now rightfully take its place in the first rank of anti-aging/ nootropic/
energizer drugs, along with Hydergine, Piracetam, vinpocetine, deprenyl and GH3/
KH3 (and it's one of my personal favorites!)
So who can benefit from
Idebenone? The answers are,
1.
Healthy people wishing cognitive enhancement and brain energizer effects (it
synergizes well with piracetam, vinpocetine and Hydergine). 2 or 3 tablets (45mg
each) daily.
2.
Stroke victims wishing to improve memory, emotional or speech disturbances. 3 to
6 tablets (45mg each) daily.
3.
Alzheimer's and cerebrovascular dementia patients. 4 to 6 tablets (45mg each)
daily.
4.
Those preparing for major surgery, especially brain, heart, liver or kidney.
Synergizes well with Hydergine. 4 to 6 tablets (45mg each).
5.
People with heart energetics problems, e.g. cardiomyopathy,
ischemic heart disease, congestive heart failure. 3 to 6 tablets (45mg each)
daily.
6.
People with myelination problems, e.g. multiple sclerosis or "white
matter" stroke injury. 3 to 6 tablets (45mg each) daily.
7.
Those seeking to increase their general energy and vitality levels. 2 to 3
tablets (45mg each) daily.
8.
People with especially high endurance energy needs, e.g. cross country skiers,
long distance runners, cyclists, swimmers etc. 3 to 4 tablets (45mg each) daily.
9.
Those at risk of excitatory
amino acid 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 (45mg each) daily.
10.
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 (45mg each) daily.
11.
Those suffering acute or chronic liver damage from poison mushrooms, toxic
chemicals, hepatitis etc. 2 to 4 tablets (45mg each) daily.
12.
People desiring a "long haul" broad-spectrum anti-aging drug.
Synergizes well with deprenyl, Hydergine, GH3/ KH3. 2 or 3 tablets (45mg 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
45mg 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 through-out 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 .
References
Weyer G, Babeji-Dolle RM, Hadler D, Hofmann S, Herrmann WM,
"A controlled study of 2 doses of idebenone in the treatment of Alzheimer's
disease." Neuropsychobiology 1997; 36(2):73-82
Ranen NG and colleagues, "A controlled trial of
idebenone in Huntington's disease" Mov Disord 1996 Sep;
11(5):549-554
Ikejiri Y, Mori E, Ishii K, Yasuda M, Sasaki M, "Idebenone
improves cerebral mitochondrial oxidative metabolism in a patient with MELAS"
Neurology 1996; Aug 47(2); 583-585.
Pisano P and colleagues, "Plasma concentrations and
pharmacokinetics of idebenone and its metabolites following single and repeated
doses in young patients with mitochondrial encephalomyopathy." Eur J
Pharmacol 1996; 51(2):167-169.
Gillis JC, Benefield P, McTavish D, "Idebenone, a review
of its pharmacodynamic and pharmacokinetic properties, and therapeutic use in
age-related cognitive disorders." Drugs Aging 1994; Aug;5 (2):
133-152.
Bergamasco B, Scarzella L,
"Idebenone, a new drug in the treatment of cognitive impariment in
patients with dementia of the Alzheimer type." Funct Neurol 1994;
May;9(3):161-168.
Nitta A, Hasegawa T, "Oral
administration of idebenone, a stimulator of NGF synthesis recovers reduced NGF
content in aged rat brain." Neuosci Lett 1993 Dec 12;
163(2):219-222.
Suno M, Nagaoka A, "Inhibition of brain
mitochondrial swelling by idebenone." Arch Gerontol Geriatr
1989 May; 8(3):299-305.
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