Arachidonic Acid (eicosa-5,8,11,14-enoic acid) anabolic agent (non-steroid) profile

akn

Musclechemistry Member
Description:
Arachidonic acid is an omega-6 essential fatty acid that
serves as the principle building block for the synthesis of
dienolic prostaglandins (such as PGE2 and PGF2a). These
prostaglandins are integral to protein turnover and muscle
accumulation, and have such important activities as
increasing blood flow to the muscles (pumps), increasing
local IGF-1 and insulin sensitivity (corresponding receptor
levels), supporting satellite cell activation, proliferation, and
differentiation, and increasing the overall rate of protein
synthesis and muscle growth. Arachidonic acid release
serves as the main thermostat for prostaglandin turnover in
skeletal muscle tissue, and is responsible for initiating many
of the immediate biochemical changes during resistance
exercise that will ultimately produce muscle hypertrophy. As
such, it is a highly anabolic nutrient. Among the large variety
of nutrients available to athletes and bodybuilders for
supplementation, next to protein, arachidonic acid is the most
integral to muscle growth, as it sits at the very center of the
anabolic response.
Clinical Studies:
In 2005, the Exercise & Sport Nutrition Laboratory at Baylor
University conducted a double-blind placebo-controlled
study to determine if 50 days of resistance training and
arachidonic acid (X-Factor™) supplementation would affect
training adaptations in 31 experienced (>1 year) resistancetrained
males. The results were presented at the International
Society of Sports Nutrition conference on June 15, 2006. All
subjects ingested a total of four capsules each day (one 250
mg capsule of AA or placebo every four hours). Subjects
taking X-Factor added an average of 25lbs to their bench
press maximum weight in 50 days, which was an increase of
nearly 45% greater than the placebo group. The X-Factor
group outperformed the placebo group on Average Power
(225% > placebo), Peak Anaerobic Power (600% >
placebo), and Total Work Capacity (250% > placebo). No
side effects were reported during the investigation
Pharmacology:
Arachidonic acid begins to display its anabolic activity early
during exercise. This nutrient is released from your muscle
fibers as they are damaged during intense training, triggering
a localized inflammatory and anabolic response. This is part
of the same biological process that causes you to be sore a
day or two following a good workout, and reminds us that the
old adage “no pain, no gain” is a fundamentally true one.
Arachidonic acid liberation from damaged muscle fibers is,
similarly, the very first anabolic trigger in a long cascade
that will control the rebuilding and strengthening of muscle
tissue after exercise.628 629 630 Among other things, by
increasing local IGF-1 and insulin receptor density,
arachidonic acid supports the anabolic actions of these
hormones, making the repair process both faster and more
intense. As a crude explanation, arachidonic acid helps
direct the body to where it needs muscle tissue repair by
facilitating the localized actions of anabolic hormones.
The availability of arachidonic acid, and our ability to
liberate it during exercise, is important to the anabolic
productivity of our workouts. We also need to be aware of
the fact that regular exercise significantly lowers the content
of arachidonic acid in skeletal muscle tissue.631 632 633 Since
dienolic prostaglandin synthesis is tied to the amount of
available arachidonic acid, lower levels result in less
arachidonic acid being released during exercise, and a less
intense anabolic response. The depletion of arachidonic acid
in skeletal muscle tissue is also one of the key reasons we
find it harder to get sore the more regularly we exercise.
With lower levels of arachidonic acid, you need to work
more vigorously to receive the same level of release and
anabolic stimulation. On the same note, when you change up
your routine and hit your muscles from new angles,
arachidonic acid is the reason you may find yourself more
sore than usual. You have called upon new muscle fibers,
which have higher stores of arachidonic acid to work with.
Dan Duchaine once said,“ The best exercise is the one you
are not doing.” This may have a lot to do with what he was
talking about.
History:
The arachidonic acid supplementation protocols, and the
concept of using this nutrient to improve muscle mass,
strength, and performance, were first developed by William
Llewellyn, author of this book series. Llewellyn filed patent
on the technology on November 27, 2002, and released an
arachidonic acid supplement under the X-Factor trademark
(Molecular Nutrition) shortly after. Although the product was
initially met with a great deal of skepticism and criticism by
industry peers, it has since been proven effective both in the
marketplace and in clinical trials, and established itself as a
powerful supplement for body recomposition goals. The U.S.
Patent & Trademark Office granted Llewellyn’s patent
application for arachidonic acid on January 11, 2005 (U.S.
Patent # 6,841,573), and the product has since been offered
for license to other companies in the industry. The original
X-Factor product remains widely available in the U.S. and
abroad, and rapid expansion in the arachidonic acid category
is expected as more companies license the technology. Note
that any officially licensed arachidonic acid product sold in
the sports nutrition marketplace will carry the original XFactor
trademark on its packaging.
Structural Characteristics:
Arachidonic acid (eicosa-5,8,11,14-enoic acid) is an
essential polyunsaturated fatty acid found in animal fats.
Supplemental arachidonic acid is commonly produced in two
forms, triglyceride and ethyl ester. As with other fatty acid
supplements such as fish oils, the natural triglyceride form
(as present in X-Factor and licensed products) offers up to
400% greater absorption than the ethyl ester, and is the
preferred form for supplementation.
How Supplied:
Arachidonic acid is sold under the X-Factor trademark by
Molecular Nutrition, and is supplied in 250 mg capsules
Arachidonic acid may also be found in a number of licensed
products; all will display the patent number (#6,841,573) on
the packaging.
Administration (Short-Term Anabolic):
As a short-term anabolic agent, arachidonic acid is
supplemented at a dose of 500 mg to 1,000 mg per day (2-4
250 mg capsules). The full 1,000 mg dose is most commonly
used, regardless of bodyweight. The nutrient is cycled in the
same way steroids commonly are, and is taken for a period
of 7-8 weeks followed by an equal amount of time off. This
level is sufficient to notice measurable increases in lean
muscle mass, strength, and anaerobic power. Depending on
dietary and individual metabolic factors, these gains may be
accompanied by a decrease in body fat. Gains of 1-2lbs of
lean muscle mass per week are fairly consistent, with total
accrued weight gain often measuring approximately 10lbs
during a cycle. There is also no hormonal disruption with
arachidonic acid supplementation, so the retention of gains
after the product is discontinued is generally high. Note that
arachidonic acid also has some effect as a vasodilator, and
may produce increased pumps in response to intense training.
This often occurs within two weeks of initiating
supplementation at anabolic levels.
Administration (Normal Supplementation):
Arachidonic acid may also be an important nutrient to
consider in regular supplemental doses, particularly if you
do not consume animal products (red meat, organ meat, eggs)
on a regular basis. Studies have shown that given somewhat
comparable amounts of protein, those who consume animal
products will make more progress with resistance exercise
than those that do not (vegetarians).634 Arachidonic acid may
be the missing component in such diets, too integral to the
anabolic response for lower dietary levels not to be noticed.
There is also empirical evidence suggesting that an
arachidonic acid deficiency exists in many experienced
bodybuilders, given that training depletes AA stores. On a
number of cases, tissue tests for the content of phospholipids
have revealed unusually low levels of arachidonic acid in
highly trained athletes. For those who find their intake of
animal products inadequate, or feel that they may have
insufficient tissue stores of AA, a single capsule of 250 mg
provides about the equivalent of a day’s supply of
arachidonic acid within a normal western diet with animal
products. Taken every day or two, the capsule should
provide a necessary supply of this essential omega-6 fatty
acid.
Safety:
In clinical studies involving the supplementation of 1,500
1,700 mg of arachidonic acid per day, general markers of
health were also unaffected with 50 days of continuous use.
This includes no notable change in HDL, LDL, or total
cholesterol values, immune system response functioning, or
platelet aggregation values.635 636 637 Furthermore, the
investigation at Baylor University demonstrated safety on all
of the basic markers of health including lipids, blood
pressure, blood cell counts, immune system mediators, and
liver enzymes. The study also produced a strong trend for
reduced IL-6 in the X-Factor supplemented group, which is a
principle inflammatory cytokine and stimulus for the hepatic
production of C-reactive protein. High levels of IL-6 are
correlated with poor health and mortality, and are deemed
undesirable. The results suggest that while arachidonic acid
may be “proinflammatory” in the sedentary (inactive) state,
when combined with resistance training, a reduction in
systemic inflammation may actually be noticed. It is
speculated that an amplification of some of the healthbeneficial
aspects of resistance exercise, namely the
improved management of insulin, may be responsible for
reducing this inflammatory marker.
On a more general note, the American Heart Association
announced its position on Omega-6 EFA consumption in
early 2010. In reviewing some of the more current data, they
found that diets low in Omega-6 fats were associated with an
increased risk of heart disease compared to diets with higher
intakes. The paper also discusses arachidonic acid, and how
this essential fat is normally not proinflammatory, nor
outwardly unhealthy to consume. The American Heart
Association now recommends that 5-10% of your calories
each day come from Omega-6 fats, including ARA. Diets
rich in Omega-3’s are, of course, also healthy, but not at the
exclusion of Omega-6’s.
Side Effects:
Arachidonic acid (X-Factor) often produces an amplification
of residual post-workout (Delayed Onset) muscle soreness.
Often recovery is slightly prolonged (perhaps an additional
day of rest is required), and the user may need to adjust their
schedule accordingly. This is due to an intensification of the
normal physiological response to training, and represents
increased intensity of the anabolic cascade (and rate of
muscle growth). Those with existing minor muscle,
connective tissue, or joint injuries may notice more pain, due
to the greater prostaglandin signaling caused by
supplementation. While arachidonic acid should not
exacerbate the injury, if greater soreness interferes with
one’s ability to train comfortably, the supplement should be
discontinued until the injury is healed. Arachidonic acid
supplementation may also produce a greater incidence of
headaches in a small percentage of users, which may be due
to its effect as a vasodilator. Increasing daily water
consumption often alleviates this side effect. Additionally,
arachidonic acid seems to produce a very weak androgenic
effect in some users, often producing minor oily skin. This
may be caused by a slight amplification of testosterone’s
effect. It should not be strong enough to concern females
about virilizing side effects.
Contraindications:
Those with an existing medical condition related to
inflammation may find that the added arachidonic acid
exacerbates symptoms of their disorder, and should avoid
supplementation. This supplement should only be used after
the approval of a physician if someone is taking medication,
has an existing medical condition, or has a familial
predisposition for cardiovascular disease, high blood
pressure, or any other disorder that may require the limiting
of dietary arachidonic acid. Also, as a potent growthpromoting
agent, arachidonic acid joins androgens
(testosterone, anabolic steroids), growth hormone, IGF-1,
estrogens,and many other growth factors as potentially
supporting the growth rate of certain cancer cells if you have
the disease. Dietary arachidonic acid intake has been
generally eliminated as a causative factor in cancer,638 639
just as testosterone level has been eliminated as predictive of
prostate cancer risk, however these types of growthpromoting
agents should be avoided in such diseased states
unless approved by a physician. If you have prostate cancer,
for example, the last thing you want to start taking is a growth
promoter like testosterone. The same goes for arachidonic
acid. The bottom line is that if you are in poor health, you
should probably not be taking this supplement. If you are
healthy, you should be able to use it with great safety.

Using the standard Wingate cycle ergometer test to
measure relative peak anaerobic power, subjects taking
X-Factor increased leg power by 1.2 Watts•kg-1.This
represents a net increase of more than 600% over the
placebo group (-.2 Watts•kg-1).


In the standard Wingate cycle ergometer test to measure
anaerobic power and performance, the X-Factor group
outperformed the placebo group on Average Power by an
amazing 21 watts (AA: 37.9W P: 17.0W).That's a net
increase of nearly 225% compared to placebo.


Total Work, as recorded in the standard energy unit
Joules, increased by 1,292J in the group taking X-Factor,
while Total Work increased 510J in the placebo
group.This is more than a 250% increase compared to
placebo.

by William Llewellyn
 
i only read half of the article so far, but good read from what i can surmise!
 
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