H.E.A.T. STACK for Fat Loss, Full Write up

Posted: December 13, 2010 in Misc., Nutrition, Training
Tags: , , , , , , ,

Awesome new product from the good people at Genomyx, they even had the foresight to hire me to do their write-up.

Genomyx is proud to introduce its newest revolutionary product, a scientifically sound, truly advanced fat loss formula.

The recent trend in fat burner/thermogenic supplements has been to add numerous high dose central nervous system stimulants leading users to believe the product isn’t working unless they’re tweaked to the point of being uncomfortable.

Genomyx prefers a more scientific approach to fat loss by including more progressive ingredients designed at achieving the optimal ratio of norepinephrine (NE) to epinephrine while providing a significant dopamine boost and suppression of appetite. This dopamine boost not only affects mood (as dopamine levels decrease during dieting), but it also antagonizes the negative central effects of too much NE.

By combining years of metabolic research with volumes of user feedback, H.E.A.T. STACK blows the doors off all the other products in its class.

Not only will H.E.A.T. STACK strip fat off at an alarming rate, it also offers a variety of general health benefits. Boasting antioxidant, anti-inflammatory and blood pressure regulating effects, H.E.A.T. STACK is the real deal and should be regarded as a staple in any fat loss program from this day forward.

Here’s an in-depth look at the individual ingredients

Bergenin

A coupound isolated from the Bergenia crassifolia plant (pictured), Bergenin seems to strongly oppose the fat storage action of insulin while effectively enhancing the fat burning effects of NE (working synergistically with other H.E.A.T. STACK ingredients that elevate NE levels) (1). Basically it makes your body do exactly what you want when you’re trying to lean out.

In addition to the potent body composition benefits bergenin provides, it also appears to offer other profound health benefits. Research demonstrates its ability to act as an antioxidant and liver protectant, as well as potentially being supportive to anti-cancer and anti-HIV protocols (2),(3),(4). A 1997 study also showed bergenin to display gastroprotective effects, which may be beneficial for people with ulcers or other digestive disorders (5).

Bergenin also appears to support healthy blood pressure, and may alleviate the blood pressure elevation side effects seen in some users of fat loss compounds (6).

Alpha Yohimbine

Extracted from yohimbe bark, yohimbine has been a popular fat loss staple with bodybuilders for years due to its antagonism of alpha-2 adrenoreceptors (7),(8),(9),(10). It induces lipid mobilization through NE activity without an elevating effect on epinephrine, which makes it a great stackable fat loss candidate (9),(11). Although it can potentiate post-prandial insulin response (yet no insulinogenic effect is seen without food), yohimbine also has the ability to downregulate lipoprotein lipase activity in adipose tissue, which counteracts any anti-lypolytic activity of insulin (11),(12).

Some people have found the side effects of mixed isomer yohimbine make effective dosing tough to tolerate. The most common complaints involve elevated blood pressure and a “tweaked” feeling, especially when combined with other stimulants. This is where Alpha Yohimbine, a.k.a. rauwolscine comes in. Standard yohimbine is a mixture of alpha and beta isomers, whereas rauwolscine is only the alpha, which eliminates the undesired side effects while actually increasing fat loss activity due to better receptor binding affinity and increased central dopaminergic activity.

It also has a fairly pronounced aphrodisiac effect in most users, which, in males, couples nicely with its ability to cause vasodilation, aka increased blood flow to the “extremities”, in part through 5-HT2b antagonism. And if that weren’t enough, it has also been shown to increase ejaculatory volume, which you’ll appreciate after you lose enough body fat for someone else to finally find you attractive (13). Interestingly, a-Yohimbine binds to human alpha-2 adrenoreceptors with a higher affinity than it does in rodents, which make the slew of rodent studies even more impressive (14).

Rounding off the alpha-Y benefits, it also offers some pretty potent mental stimulation and mood elevating effects by modulating dopamine and serotonin, all while suppressing appetite, making pissed off and hungry dieting a thing of the past (15)(16)(17).

Raspberry Ketones

Structurally similar to capsaicin and synephrine, Raspberry Ketones (RK’s) display a lipolytic effect through the activation of the transient receptor potential vanilloid type 1 (TRPV1) protein located throughout the central and peripheral nervous system in the body.

TRPV1 modulation has been a hot area of research lately, implicated with regards to numerous health and body composition benefits. Researchers from Current Pharmaceutical Design reported that activation of TRPV1 receptors in the brain can potentially alleviate symptoms of pain and anxiety (18). A team out of Brown University found that TRPV1 activation may be an effective angle at treating depression through interneuron formulation, stating “TRPV1 channel activation is necessary and sufficient to trigger long-term synaptic depression (LTD)” (19).

Through modulation of NE and hormone sensitive lipase, RK’s appear to be a powerhouse for encouraging fat loss and prevention of fat gain. When mice were fed a high fat diet, RK’s prevented visceral and liver fat accumulation as well as reversing the gain in previously obese mice (20). Recently liver fat has been implicated in metabolic disturbances to an even greater degree than the previous villain, visceral fat, so this is a benefit of great magnitude for overall health (21).

In another study, after 120 days of a TRPV1 agonist researchers concluded adipogenisis and obesity were prevented by activation of TRPV1 channels (22). And if anybody tries to tell you RK is an anti-androgen, yes, it is a weak anti-androgen in breast cancer cell lines, in vitro, which is a good thing (23). Antiandrogenic activity in muscle tissue has never been demonstrated in the research. Numerous compounds are antiandrogenic in certain tissues (and beneficially so, such as milk thistle and the prostate) yet do not display this activity in skeletal muscle (24), (25).

Piperine

Extracted from black pepper, piperine is the alkaloid responsible for pepper’s spicy, biting flavor. Initially investigated for its ability to inhibit certain liver enzymes responsible for drug metabolism, piperine has recently been the subject of research looking at various fields of health enhancement and positive modulation of multiple physiological systems, as discussed below.

Researchers out of Thailand noted in a recent study, “…piperine at all dosage range used in this study possessed anti-depression like activity and cognitive enhancing effect at all treatment durations. Therefore, piperine may be served as the potential functional food to improve brain function” (26). In a University Study out of China, researchers looked at the MAO inhibition properties of piperine and found an anti-depressant effect due to serotonin modulation (27).

Another related study covered the IC50 values (the concentration of a drug that is required for 50% inhibition in vitro) of piperine’s function as an MAOa and MAOb inhibitor at 20.9 microM and 7.0 microM respectively. Called a “promising pharmacotherapeutic candidate as an antidepressant agent”, the researchers determined this was due at least in part to its MAO inhibition properties (28).

The Institute of Neuroinformatics in Dalian, China, looked at piperine’s action in mice exposed to Chronic Mild Stress (CMS). They found that after two weeks of administration, piperine “reversed the CMS-induced changes in sucrose consumption, plasma corticosterone level and open field activity”, which basically means they stopped guzzling sugar and feeling sorry for themselves and started becoming more active. Piperine was also found to be neuroprotective by reversing the effect on the brain of elevated corticosterone by up-regulation of the progenitor cell proliferation of hippocampus (29).

Previously discussed in the Raspberry Ketone section, piperine is another favorable modulator of the TRPV1 protein. Since researchers started looking at TRPV1, capsaicin has been the predominant compound used for modulation due to its predictable efficacy for desired outcomes (also included in H.E.A.T. STACK). A study published in the British Journal of Pharmacology was the first to implicate piperine as a TRPV1 modulator, stating, “our data suggest that the effects of piperine at human TRPV1 are similar to those of capsaicin except for its propensity to induce greater receptor desensitization and, rather remarkably, exhibit a greater efficacy than capsaicin itself.” (30). Shortly after this study was published, a review of piperine in Trends in Pharmacological Sciences stated, “This finding raises the intriguing possibility that piperine can be used as a chemical template for the design of improved TRPV1 agonists” (31).

A 2009 study out of Seoul, Korea looked at the effect of piperine on various markers of pain and biochemical inflammation in arthritic models, with exciting results. They demonstrated that piperine “significantly reduced the inflammatory area in the ankle joints”, and concluded that “piperine has anti-inflammatory, antinociceptive, and antiarthritic effects in an arthritis animal model.” (32). For those unfamiliar with the term, antinociceptive basically refers to a pain reduction effect.

Previously, researchers from the Molecular Immunogenetics Laboratory in India set out to find how piperine exhibits its anti-inflammatory effects, finding that it blocks TNF-alpha induced expression of certain cell adhesion molecules (33). TNF-alpha regulation is a crucial factor in whole body inflammation and overall health, when levels get out of range (high or low), numerous problems arise.

Research published in the Journal of Cardiovascular Pharmacology found that piperine exhibits a blood pressure lowering effect possibly through blockage of calcium channels with effects similar to the prescription hypertension drug verapamil (34).

In a recent study out of India, researchers looked at the chemoprotective ability of piperine (combined with curcumin) in oral cancers. They developed oral cancer in hamsters through a known carcinogen, then gave another group the piperine/curcumin combination and noted a complete prevention of oral carcinoma (35). The researchers determined this was probably due to the antilipidperoxidative and antioxidant potential of the piperine/curcumin. The fact that curcumin was included in this study cannot be ignored but piperine was almost certainly a contributing factor to the positive outcome, and therefore the research is worth noting.

Another study out of India looked at the chemoprotective capabilities of piperine alone, along with its antioxidant and immunostimulatory properties. The researchers induced immunocompromisation in murine splenocytes with cadmium, which induces apoptosis (cell suicide, basically) at 6 hours onwards in treated cells. Piperine was able to completely abolish the toxic effect of the cadmium, and the researchers concluded, “The findings strongly indicate the anti-oxidative, anti-apoptotic and chemo-protective ability of piperine in blastogenesis, cytokine release and restoration of splenic cell population and is suggestive of its therapeutic usefulness in immuno-compromised situations” (36).

Last but certainly not least, a brief discussion of the gastrointestinal and liver enzyme modification effects of piperine. A review paper titled “Black pepper and its pungent principle-piperine: a review of diverse physiological effects”, detailed many numerous benefits of the compound including (bullets paraphrased from review) (37):

  • Protection against oxidative damage by inhibiting or quenching free radicals and reactive oxygen species
  • Inhibitory influence on enzymatic drug biotransforming reactions in the liver
  • Strongly inhibits hepatic and intestinal aryl hydrocarbon hydroxylase and UDP-glucuronyl transferase
  • Documented to enhance the bioavailability of a number of therapeutic drugs as well as phytochemicals
  • Bioavailibility enhancing property partly attributed to increased absorption as a result of its effect on the ultrastructure of intestinal brush border
  • Non-genotoxic and has been found to possess anti-mutagenic and anti-tumor influences

Researchers out of Germany were actually the first to clinically demonstrate piperine’s drug metabolism effects in a study titled ”Piperine, a major constituent of black pepper, inhibits human P-glycoprotein and CYP3A4”. Their summary concluded, “…we showed that piperine inhibits both the drug transporter P-glycoprotein and the major drug-metabolizing enzyme CYP3A4. Because both proteins are expressed in enterocytes and hepatocytes and contribute to a major extent to first-pass elimination of many drugs, our data indicate that dietary piperine could affect plasma concentrations of P-glycoprotein and CYP3A4 substrates in humans, in particular if these drugs are administered orally” (38). P-glycoprotein or PGPs, can be thought of as first-pass eliminators, meaning they can block absorption of certain compounds in the gut, acting as goalies for the later actions by enzymes in the liver. Piperine blocks PGPs as well as key liver enzymes, leading to elevated concentrations of active ingested compounds in the bloodstream, i.e., other ingredients in H.E.A.T. STACK.

Capsaicin

Capsaicin is part of the vanilloid family, and is the phytochemical in chili peppers that causes them to be hot. Current research and user feedback both strongly support capsaicin for fat loss, working through increased channel expression of TRPV1 (like piperine and raspberry ketones), AMPK activation, and NE elevation (39), (40), (39).

A 2008 study published in the journal Life Sciences showed that when rats were fed capsaicin in their diet (the same percentage of energy intake that average rural Thai folk consume daily, at 0.014%), they showed a 29% reduction in visceral fat with no change in caloric intake (41).

Capsaicin is a novel compound in that it not only promotes fat loss, but it also helps to prevent fat cells from forming in the first place (from a process known as preadipocyte differentiation and proliferation). It has also been shown to inhibit the expression of PPARgamma (which regulates fatty acid storage) and upregulate adiponectin, an adipokine of which higher levels are associated with leanness (41). In concert with the previous study on preventing fat gain, a 2007 study out of China showed that giving mice capsaicin for 120 days on a high fat diet prevented fat gain, compared to the same capsaicin protocol with a high fat diet given to TRPV1 knockout mice. “Knockout” is a science nerd term for genetically altering a subject to eliminate or emphasize a variable, in this case by removing the TRPV1 receptor, which just gives us more evidence that capsaicin works (at least in part) through TRPV1 regulation (42). Another recent study along these lines from the Journal of Clinical Nutrition demonstrated that capsaicin (in conjunction with green tea) reduced energy intake during a positive energy balance, while subjects in a negative energy balance noticed less hunger and more satiety (40).

The Journal of Nutrition and Metabolism recently published a study showing multiple benefits in humans from oral capsaicin administration, including an increase in VO2, increase in plasma NE, decrease in serum FFA’s (meaning they were oxidized), blunted accumulation of blood lactate and a shift in substrate utilization towards fat at rest (40).

Capsaicin may also be a great tool to help prevent fat re-gain after getting down to goal body fat levels. In a 2003 study published in the British Journal of Nutrition, subjects were given capsaicin after a four week very low calorie diet to see if it prevented fat re-gain after losing 5-10% of bodyweight. The researchers determined that “capsaicin treatment caused sustained fat oxidation during weight maintenance compared with placebo” (43).

Green Coffee Bean extract

Before coffee beans are roasted to the dark brown color we’re used to seeing, they’re typically a green or brownish green. In this state, they offer an unadulterated source of chlorogenic and caffeic acid, which may be quite beneficial in the quest to lose body fat.

Shimoda, et al. found green coffee bean extract (GCBE) to reduce body weight and visceral fat in mice, and concluded that “GCBE is possibly effective against weight gain and fat accumulation by inhibition of fat absorption and activation of fat metabolism in the liver” (44). The same study found that GCBE was capable of reducing hepatic triglycerides, which when elevated can contribute to significant metabolic damage.

Chlorogenic acid contains ferulic acid, which has been shown to act on nitric oxide from the vascular endothelium. In a 2004 study conducted in Japan, the researchers put subjects with a reduced vasodilation response on either a GCBE or a placebo drink for 4 months and measured changes. After one month, measures of vasoreactivity increased, and continued to improve over the course of the whole four months of testing. The GCBE subjects also had a significant decrease in plasma homocysteine compared with pre-ingestion levels (45).

Chlorogenic and caffeic acids have been shown to have a significant and favorable impact on adipokine modulation. A 2010 study published in the American Journal of Clinical Nutrition showed that the two acids decreased interleukin-18 and isoprostane while elevating adiponectin. For those of you not quite up to speed on your adipokines, here’s a quick description-

Interleukin-18

A pro-inflammatory cytokine with the ability to induce severe inflammatory reactions in the body. Like most cytokines it has important functions (in this case, combating intracellular bacteria), but being pro-inflammatory, it’s something we definitely don’t want getting too high (46). The above study showed a decrease in interleukin-18 by 8%.

Isoprostane

A prostaglandin like compound produced as a byproduct when free-radicals cause peroxidation of essential fatty acids (47). This is marker of bad things happening in the body, so when it decreases that means you’ve effectively reduced EFA peroxidation, which is a good thing. The above study showed a decrease in isoprostane levels by 16%.

Adiponectin

As the outlier of adipokines, levels of adiponectin are inversely related to body fat levels in adults. It’s anti-inflammatory, anti-atherogenic, it helps repair glucose metabolism and insulin signaling, and does a whole host of other beneficial things in the body, some that aren’t even fully understood yet (48). The above study showed an increase in adiponectin by 6%.

Aside from that, these coffee compounds also improved the LDL:HDL cholesterol ratio and caused a decrease in overall inflammation, which was further replicated in a 2006 study demonstrating a pain reduction effect in animal testing due to the anti-inflammatory effect (49).

Hordenine

Hordenine (also known as N,N-dimethyltyramine) is a phenylethylamine alkaloid found in the sprouted seeds of barley. While hordenine doesn’t have a lot of published data, we have enough to understand what it does and how it can be beneficial for fat loss.

A study done on horses showed a significant increase in NE related physiological effects (which works harmoniously with bergenin to accelerate fat burning), which has also been demonstrated in dogs and rats (50), (51).

Hordenine also targets the ever-important dopamine pathway of successful fat loss programming, due to it being a highly selective substrate for the monoamine oxidase-b (MAO-B) enzyme (52). So you can expect a boost in energy and mood as well as significantly accelerated fat loss.

Tyramine

Tyramine is monoamine and trace amine compound derived from the amino acid Tyrosine, found naturally in the body as well as in wine and some cheese. Tyramine works more magic through NE, in that it is competitively and preferentially taken up at the NE transporter, leaving more NE in the body to do work. In addition, it also competes with NE for breakdown by the MAO-a enzyme, so that less NE is broken down.

Aside from the potentiating effects on NE, Tyramine also gives dopamine a run for it’s money in a multi-faceted manner by again competing for MAO breakdown, as well as directly elevating dopamine levels by conversion through the CYP-2D6 enzyme, and finally by inhibiting dopamine uptake thereby leaving it active for a longer time to do it’s thing (53), (54). Tyramine should also aid in nutrient partitioning due to its vasodilation effect, making it a good choice for pre-workout usage, whereas independently jacking up NE levels without this tyramine driven dopamine boost would cause unwanted vasoconstriction (54).

It appears that Tyramine also activates the trace amine associated receptor 1 (TAAR1) which elevates adenyl cyclase, a lipid mobilizing 2nd messenger which should not only accelerate fat loss but also help to elevate mood and energy, as this is the same receptor activated by amphetamines, MDMA, LSD, and other psychoactive compounds (albeit to a much lesser extent, so don’t plan on getting twisted Hunter S. Thompson style on tyramine) (55), (56), (57).

Evodiamine

Found in the Evodia fruit, this alkaloid is somewhat similar to capsaicin in it’s biological effects, and that it is a TRPV1 modulator (58). This compound has about 10 years of steady research behind its fat loss benefits, and it just keeps getting better.

A study out of Japan showed that when rats fed a high fat diet were given Evodiamine, they lost body fat and decreased serum free fatty acids and hepatic lipid measurements. This same study also showed Evodiamine to offer a pretty cool heat regulating effect, as it increases heat production and heat loss at the same time, dissipating food energy (59).

Evodiamine has been shown to delay gastric emptying and cause a large release of cholecystokinin, which will cause an automatic reduction in food intake due to appetite reduction/satiation, making it easier to stick to your diet (60). It has also been shown to directly decrease food intake and weight gain through hypothalamic modulation of neuropeptide Y and mRNA expression (61).

A study out of Japan demonstrated a strong favorable influence of Evodiamine on pain signaling by desensitizing sensory nerves (62). This is the fifth ingredient boasting a pain reducing effect (in addition to raspberry ketones, piperine, capsaicin and green coffee bean extract), so H.E.A.T. STACK is not only a superior fat loss agent, but also potentially a potent pain reducer. Along these lines, Evodiamine is also a known anti-inflammatory by inhibiting COX-2 and NF-kappaB, and is used in Traditional Chinese Medicine for this purpose (63)(64). It also reduces TNFa and IL-4, causing an antiallergic action in IgE induced problems such as atopic dermatitis and rhinitis (65). Since inflammation is the root of almost every problem in the body, including excess fat storage, controlling whole body inflammation will put the body in a more optimal fat burning state.

Another notch on the belt for increasing general health, Evodiamine has been shown in numerous studies to cause apoptosis in a variety of tumor cells (including cervical and prostate) while inhibiting proliferation, invasion and metastasis (66)(67)(68). It has also been recently shown to inhibit angiogenisis in human endothelial cells, which means it will halt the growth of new vessels that cause the spread of diseased tissue (69). Take that, cancer.

Ok, being healthy is cool…but what about some more direct activity on fat loss? In addition to being an activator of uncoupling protein-1 (UCP1) thermogenesis, Evodiamine reduces expression of PPARgamma, inhibits adipocyte differentiation, reduces phosphorylation of Akt, and favorably modulates the insulin signaling pathway (70)(71)(72).

New research has shown that Evodiamine works it’s fat loss magic in other ways than solely through TRPV1. While this stuff gets pretty complex, the short version is that it also works through protein kinase C (PKC) and something called the epidermal growth factor receptor (EGFR) (73). While understanding the intricacies of those systems is probably not important to most people, the important thing to note here is that Evodiamine is working through multiple mechanisms to inhibit fat storage and encourage fat loss.

Evodiamine will also bolster thermogenesis by causing an increased catecholamine secretion in the adrenal medulla (epinephrine, norepinephrine), and increase sensitivity of those cells to acetylcholine (74).

And finally, a brand new study in the International Journal of Obesity showed a significant reduction in body weight gain and reduced plasma insulin levels in rats fed evodiamine. The researchers confirmed previous research on prevention of adipocyte differentiation, and also demonstrated an overall improvement of insulin resistance (72).

Conclusion

Losing body fat isn’t just about working hard; it’s about working smart. H.E.A.T. STACK delivers the most advanced fat loss ingredients on the planet to ensure you reach new levels of leanness in record time. By optimizing the body’s fat burning machinery while suppressing appetite and enhancing mood, you have no choice but to take your physique to a new level.

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Comments
  1. RJ says:

    Question regarding dosing. I have been on this a week, and don’t really get any feeling from it. Self admittedly I am a bigger guy with a lot of weight to lose. Would it be recommended to play around with the dosing on this? Maybe 4-5 a day or maybe dose 2 – 1 – 1 or maybe even all the way up to 2 – 2 – 2, or is there any reason I should hold off on playing around here? Thanks!

    • Fitport says:

      You could probably go up to 4-6 caps per day, but you may not feel a whole lot from it. Gauge it by fat loss instead of feeling, or add some caffeine if you need more stimulation.

  2. silenthunder says:

    I was wondering if the h.e.a.t. stack has any warnings against taking the product if you have hypertension (because of the yohimbine content), if you are already taking wellbutrin/chantix (similar affect on NE/E and dopamine as this supplement product), and indicating not taking the supplement if currently taking MAOI drugs (because of the inclusion of tyramine). I am also interested if there are any reports of how this product is actually performing in people taking it (I appreciate the amount of science you included in your writeup). I’m a bigger guy with lots of weight to lose – I would consider taking this – but am not interested in unproven supplements.

  3. […] H.E.A.T. STACK for Fat Loss, Full Write up […]

  4. I know this if off topic but I’m looking into starting my own blog and
    was curious what all is required to get setup? I’m assuming
    having a blog like yours would cost a pretty penny?
    I’m not very web smart so I’m not 100% sure. Any recommendations or advice would be greatly appreciated.
    Thanks

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