Theobroma Cacao extract for 12% OEA
(oleoylethanolamide) and 3-Thia-Palmitic Acid (Tetradecylthioacetic acid)
are very cool compounds that promote lipolysis (blubber burning) through
some unique pathways.
OEA is produced in the small intestine and belongs
to a group of fats produced in response to nervous system activity and
certain metabolic events.
In an
interesting mammal study published in the Journal of Biological Chemistry,
OEA was shown to reduce feeding and body weight gain by activating the
nuclear receptor PPAR-alpha (peroxisome proliferator-activated receptor
alpha). In the present report, we examined whether OEA can also influence
energy utilization. OEA stimulated glycerol and fatty acid release from
freshly dissociated rat adipocytes. OEA enhanced fatty acid oxidation in
skeletal muscle strips, dissociated hepatocytes, and primary cardiomyocyte
cultures. Administration of OEA in vivo produced lipolysis.
In short, the
OEA study results showed a decrease in food intake and an increase in
calorie expenditure by way of lipolysis and fat oxidation through a unique
pathway. The same study left us with this quote to consider: “The results
suggest that OEA stimulates fat utilization through activation of
PPAR-alpha and that this effect may contribute to its anti-obesity
actions”.
Then Why Add 3-Thia Palmitic Acid Too?
The Department
of Clinical Biochemistry, Haukeland Hospital, University of Bergen, Norway
did a study on 3-Thia fatty acids that resulted in conclusions anyone
wanting to create and maintain a lean body would salivate over…
“The
biological responses to tetradecylthioacetic acid include mitochondrial
proliferation, increased catabolism of fatty acids, antiadiposity,
improvement in insulin sensitivity, antioxidant properties, reduced
proliferation and induction of apoptosis in rapidly proliferating cells,
cell differentiation and antiinflammatory action.”
“These
biological responses indicate that tetradecylthioacetic acid changes the
plasma profile from atherogenic to cardioprotective. As a pan-peroxisome
proliferator-activated receptor ligand, tetradecylthioacetic acid
regulates the adipose tissue mass and the expression of lipid metabolizing
enzymes, particularly those involved incatabolic pathways.”
Translation?
- Fat burning due to more mitochondria
to do so and fat oxidation via our good friend PPAR-alpha.
- Fat storage control.
- Better insulin activity control so
calories are stored as lean tissue instead of waist wrap for
winter.
- Anti-oxidant qualities to protect
cells form the damage normally done by calorie restricted diets and
training.
- A cool hatred for cells that are not
supposed to be mass produced.
- Improved lipid
metabolization.
- So,
Together, OEA and 3-Thia Palmitic Acid make for serious synergistic
lipolytic action!
Cool, Now, How About Blocking Fat
Storage?
Polygonum
Multiflorum Proprietary Extract is one of the new sensations in the fat
burning industry. The really hard part is actually creating the most
effective proprietary extraction procedure to make it work and at a
concentration that makes it possible to put in a capsule.
Polygonum
Multiflorum Proprietary Extract has been used in herbal medicine for
centuries for its reported ability to promote lipid control and aid
cardiovascular health. Oh sure, there is a great deal of evidence that the
extract acts as an anti-oxidant, anti-catabolic and nitric oxide
potentiator in mammals, but more recently, and due to some pretty cool
extraction methods…
It has been
found that Polygonum Multiflorum Proprietary Extract has unique properties
that inhibit anti-lipolytic hormone (the hormone that shuts down fat
burning potential) and fatty acid synthase (the enzyme that is the gate
keeper for fat storage).
- As
many fans of ALR Industries are aware, we love to use this and the next
compound in many of our fat loss lean mass promoting products simply
because they work so well.
Beta AET ECPE
(beta-androstenetriol ECPE)? We have all heard, and in many cases
experienced, the positive effects of DHEA and its even better metabolites.
As example are the patented and effective products 7-OXO-DHEA and of
course 7-Hydroxy-DHEA analogs. They are noted for their unique ability to
avoid conversion into androgenic metabolites or affect androgen receptors
while promoting fat loss, lean mass retention and even maximizing thyroid
gland activity. Of course oral bio-availability is pretty poor with most
of these analogs thus requiring higher dosages. Did I mention that bAET
(b-androstenetriol) is between 100 and 100,000 times more active than its
DHEA precursor metabolites? Okay, how about that bAET ECPE is nearly 100%
orally bioavailable? Yup. It’s why we formulated it.
Glucocorticoids in humans are in two forms:
Inactive cortisone and very active for eating muscle cortisol. There are
two enzymes that are able to make each of these convert into the
other.
11b-HSD-1: Converts inactive cortisone into
cannibalistic cortisol. Studies have implicated this event in fat tissue
as a pathway for increased fat storage. Part of the reason GH has a
positive affect upon body composition is through its ability to inhibit
11b-HDS-1
11b-HSD-2: Converts nasty cortisol into cortisone.
11betaHSD2 debunks intracellular cortisol by 90%. (Let the 11b-HSD-2 rule
the house)
Hmmm, more 11b-HSD-1 means more cortisol which
eats more muscle. And less means…Duh!
Beta-AET ECPE
inhibits the 11b-HSD-1 enzyme both locally and systemically. This means
that there is less conversion of cortisone to cortisol in muscle as a
result of training and everywhere else due to stress like dieting. Based
upon the studies, it appears that in mediating this pathway, bAET ECPE
increases immune function and recovery of cells as well. Add this to its
stimulatory affect upon the thyroid gland to support natural thyroid
hormone production? Yup, less cortisol, higher metabolic rate, inhibition
of that nasty negative thyroid hormone production feed-back loop…less fat,
more lean muscle and positive support to health. Not bad!
Clary Sage
Extract has a really cool effect due to its cAMP stimulating value. There
is a significant similarity between compounds in this interesting herb and
Thyroid Stimulating Hormone (TSH). As most are aware, increased TSH means
more fat burning anabolism promoting T-3 production (yes, it acts
synergistically with the last goodie in this regard…but through different
pathways).
The connection
here is that the TSH-like effect triggers an enzyme called adenylate
cyclase in the thyroid that results in an increase in cAMP activity and
subsequently lots of extra T-3 production…naturally. Since there is an
increase in cAMP, there is an accompanying increase in nitrogen
retention.
What Else?
We added
Salvia Tanshinones to aid lipolysis via improved liver lipid metabolism,
gallic acid to inhibit fat cell uptake of glucose, Oleanolic Acid to block
fat absorption, Bergenin to enhance norepinephrine triggered lipolysis and
Rhodiola to support mood and immune function.
What about Insulin Insensitivity and
Fat?
One reason we
accumulate fat is due to insulin. Insulin is likely one of the most
anabolic to muscle substances on the planet, but it has an evil side in
that it is anabolic to fat cells too. The reason is partitioning meaning
that insulin can store calories in fat or muscle.
As we gain
fat, muscle cells tend to become less sensitive to insulin (Insulin
Insensitivity) and fat cells tend to become ever so accommodating. So the
result is that fat get the lion’s share of calories coming in. When you
diet or cut calorie intake the muscle start to shrink and the fat cells
have the upper hand in the fight for calories which is why most lose more
muscle than fat when dieting.
The goal is to stimulate
muscle cell insulin sensitivity and decrease fat cell feeding frenzies…
Repartitioning!
Peroxisome
proliferator-activated receptor (PPAR)-gamma activators are widely used in
the treatment of type 2 diabetes because they improve the sensitivity of
insulin receptors. Punica granatum flower (PGF) has been used as an
anti-diabetic medicine in Unani medicinal literature. In several studies
the reported active compound in this friendly herb that causes this cool
event is gallic acid. You are already aware of the research that shows
gallic acid inhibits fat cell feeding on glucose, but the right extraction
has been shown in mammal studies to induce muscle cell insulin
sensitivity. When fat is starved and muscle is fed…well, you do the
math.
So fat lipolysis with fat
storage inhibition on multiple levels and repartitioning to support lean
tissue...now you get the “Special Tactics” part?
Zero-Stim™
is the ultimate stimulant free stand alone or stackable synergistic
supplement for any serious fat loss system!
Research, Good Reading and References:
1) Oleoylethanolamide stimulates lipolysis by
activating the nuclear receptor peroxisome proliferator-activated receptor
alpha (PPAR-alpha). J Biol Chem. 2004 Jul 2;279(27):27849-54. Epub 2004
Apr 26.
2) Mechanisms of oleoylethanolamide-induced changes in feeding
behavior and motor activity. Am J Physiol Regul Integr Comp Physiol. 2005
Sep;289(3):R729-37. Epub 2005 May 5.
3) Effects of 3-thia fatty acids
on beta-oxidation and carnitine palmitoylatransferase I activity in
cultured rat hepatocytes. Adv Exp Med Biol. 1999;466:53-7.
4) Metabolic
effects of thia fatty acids. Curr Opin Lipidol. 2002 Jun;13(3):295-304.
Review.
5) Effect of guzhen recipe on glucocorticoid receptor in senile
rate thymocyte] Zhongguo Zhong Xi Yi Jie He Za Zhi. 1995 Feb;15(2):92-4.
Chinese.
6) Effect of the root of Polygonum multiflorum Thunb. and its
processed products on fat accumulation in the liver of mice] Zhongguo
Zhong Yao Za Zhi. 1992 Oct;17(10):595-6, 639. Chinese.
7) Traditional
Chinese Medicine improves dysfunction of peroxisome proliferator-activated
receptor alpha and microsomal triglyceride transfer protein on
abnormalities in lipid metabolism in ethanol-fed rats. Biofactors.
2005;23(3):163-76.
8) Myricetin, quercetin and catechin-gallate inhibit
glucose uptake in isolated rat adipocytes. Biochem J. 2005 Mar 15;386(Pt
3):471-8.
9) Carnosic acid, a new class of lipid absorption inhibitor
from sage. Bioorg Med Chem Lett. 2004 Apr 19;14(8):1943-6.
10)
Norepinephrine-augmenting lipolytic effectors from Astilbe thunbergii
rhizomes. J Nat Prod. 1998 Aug;61(8):1006-11.
11) Huang TH, Peng G,
Kota BP, Li GQ, Yamahara J, Roufogalis BD, Li Y Anti-diabetic action of
Punica granatum flower extract: Activation of PPAR-gamma and
identification ofan active component. Toxicol Appl Pharmacol 2005 Sep
1;207(2):160-9.
12) Arch Pharm Res. 2003 Jan;26(1):24-7 Further
isolation of antioxidative (+)-1-hydroxypinoresinol-1-O-beta-D-glucoside
from the rhizome of Salvia miltiorrhiza that acts on peroxynitrite, total
ROS and 1,1-diphenyl-2-picrylhydrazyl radical. Kang HS, Chung HY, Byun DS,
Choi JS.
13) Am J Chin Med. 2002;30(1):87-93. Anti-hypertensive effect
of water extract of danshen on renovascular hypertension through
inhibition of the renin angiotensin system.Kang DG, Yun YG, Ryoo JH, Lee
HS.
14) Phytother Res. 2003 Sep;17(8):917-20. Inhibition of angiotensin
converting enzyme by lithospermic acid B isolated from Radix
Salviaemiltiorrhiza Bunge.Kang DG, Oh H, Chung HT, Lee HS.
15)J
Ethnopharmacol. 2003 Oct;88(2-3):249-52. Anti-relapse properties of IDN
5082, a standardized extract of Salvia miltiorrhiza, in alcohol-preferring
rats. Serra S, Vacca G, Tumatis S, Carrucciu A, Morazzoni P, Bombardelli
E, Colombo G, Gessa GL, Carai MA.
16) J Huazhong Univ Sci Technolog Med
Sci. 2002;22(4):302-4. Effect of Salvia Miltiorrhiza on left ventricular
hypertrophy and cardiac aldosterone in spontaneously hypertensive rats.
Han S, Zheng Z,17) Zhongguo Zhong Xi Yi Jie He Za Zhi. 2002
Aug;22(8):607-9. Effect of Salvia miltiorrhiza on neuropeptide Y1-36 and
calcitonin gene-related peptide in neonatal rats with hypoxia-ischemic
brain injury. Hong XR, Wu AQ, You ZD.
18) Antiviral Res. 2002
Jul;55(1):91-106. Isolation of two highly potent and non-toxic inhibitors
of human immunodeficiency virus type 1 (HIV-1)integrase from Salvia
miltiorrhiza. Abd-Elazem IS, Chen HS, Bates RB, Huang RC.
19) Arch
Pharm Res. 2002 Aug;25(4):446-8. Inhibitory activity of diacylglycerol
acyltransferase by tanshinones from the root of Salvia miltiorrhiza. Ko
JS, Ryu SY, Kim YS, Chung MY, Kang JS, Rho MC, Lee HS, Kim YK.
20) J
Bioenerg Biomembr. 1999 Dec;31(6):559-67. Stimulation of mitochondrial
gene expression and proliferation of mitochondria following impairment of
cellular energy transfer by inhibition of the phosphocreatine circuit in
rat hearts.Wiesner RJ, Hornung TV, Garman JD, Clayton DA, O'Gorman E,
Wallimann T.
21) Acta Physiol Scand. 1998 Jul;163(3):251-9. Effect of
chronic electrical stimulation and beta-GPA diet on GLUT4 protein
concentration in rat skeletal muscle. Yaspelkis BB 3rd, Castle AL, Farrar
RP, Ivy JL.
WARNING: NOT FOR USE BY INDIVIDUALS UNDER THE AGE OF 21
YEARS. DO NOT USE IF PREGNANT OR NURSING. KEEP OUT OF REACH OF CHILDREN.
Do NOT consume this product if you have a medical condition and/or taking
any prescription medication. Do not exceed recommended serving.
Discontinue use and call a physician or licensed qualified health care
professional immediately if you experience rapid heartbeat, dizziness,
severe headache, or other similar symptoms.
These statements have not been
evaluated by the FDA. This product is not intended to diagnose, treat, or
prevent any disease.