Physiological Properties and Effects:
L-carnitine is a derivative of the amino acid lysine and, as certain conditions outpace the body’s ability to produce it, l-carnitine is considered a conditionally essential amino acid. While endogenous biosynthesis of l-carnitine from the amino acids lysine and methionine is sufficient for essential processes – along with dietary sources of carnitine from protein-rich red meat, for example – dietary supplementation of carnitine may pose benefits in certain physiological conditions.
Unfortunately, due to excess metabolism of l-carnitine by microorganisms in the small intestine, exogenous supplementation with oral l-carnitine has proved ineffective. ALCAR, an acetylated version of l-carnitine, has considerably higher oral bioavailability, due likely to only partial hydrolytic metabolism. Once in the bloodstream, ALCAR plays a fundamental role in the production of energy, acting as the catalyst for the beta-oxidation of long chain fatty acids by the mitochondria; regulating the CoA to Acyl-CoA ratio (necessary for the production of ATP); and the metabolism of carbohydrates. ALCAR also is an excitatory agent for neurons, increases neuronal transmission, and increases the production of neurotransmitters and neurohormones such as dopamine and serotonin.
Green Tea Extract (Camilla sinensis) (leaf) (50% EGCG):
Along with caffeine from the coffee plant, EGCG (Epigallocatechin gallate) from various sub-species of Camilla sinesis (green tea) is perhaps the most widely known and reputable anti-lipogenic and lipolytic agent in the world. Both compounds have well established anti-obesity effects, detailed in a deep body of literature featuring in vitro cell culture, as well as in vivo animal and human trials.
In animal and human studies, green tea generally and EGCG more specifically has been demonstrated to reduce the absorption of dietary lipids and modulate their subsequent metabolism, increase glucose utilization in resting states, as well as initiate de novo lipogenesis in both maximal and submaximal exercise states.
A two month dietary intervention, for example, showed that the daily consumption of a catechin-rich tea – EGCG is the most well-known of the catechins – by healthy humans led to a reduction of bodyweight of up to 20%, the consequence of increased lipolysis (as measured by FFA urinary clearance). A separate double-blind, placebo controlled trial using EGCG consumption both with, and without caffeine, demonstrated the increased oxidation of fatty acids within two hours of a meal – at level increases of 49% and 35%, respectively.
These studies suggest that EGCG not only exerts an inhibitory effect on the accumulation of lipids, but that it perhaps actively leads to the hydrolyzation of triglycerides for use as energy in the form of FFAs. In particular, this effect seems to be potentiated in the presence of caffeine ingestion, suggesting a synergistic effect between EGCG and caffeine on the hydrolyzation and subsequent oxidation of triglyceride stores.
Green Coffee Extract (Coffee arabica) (bean) (50% chlorogenic acid):
Chlorogenic acids (CGAs) are phenolic compounds created during the metabolism of various isoquinic acids found in the leaves of both coffee and tea. In addition to the well-established sympathomimetic effects of coffee and tea’s constituents, recent research has demonstrated a range of other potential benefits for compounds such as chlorogenic acids.
Recent literature suggests that the consumption of both green coffee, as well as standardized extracts of CGAs, relax the vasculature and improve vasoreactivity, impose an inhibitory effect on lipid accumulation and body weight in both mice and humans, and modulate glucose metabolism via the glucose-6-phosphate pathway.
Trials in both humans and mice using 1% extracts of green coffee bean revealed significant bodyweight reductions over periods of two and eight weeks. Researchers hypothesized that the bodyweight reductions associated with oral CGA administration was associated with the products numerous mechanisms of action, rather than a single, isolated cause.
Olive Extract (Olea europaeai) (leaf) (20% oleuropein):
Olea europaea, more commonly known as the olive, is a species of a small tree in the family Oleaceae, native to the coastal areas of southeastern Europe, western Asia and northern Africa, as well as northern Iran at the south end of the Caspian Sea.
As the fruits, oils, and extracts of Olea europaea L. are a dietary component for a significant portion of the world’s population, the plant has become associated with a wide-range of physiologic and metabolic benefits. These properties are largely attributed to the phenolic compounds of olive leaves, including: caffeic acid, verbascoside, oleuropein, luteolin 7-O-glucoside, rutin, apigenin 7-Oglucoside, and luteolin 4′-O-glucoside. Collectively, these olive polyphenols are responsible for a wide-range of postulated health benefits.
Oleuropein, in particular, is purported to have several pharmacological properties including antioxidant, anti-inflammatory, anti-atherogenic, and anti-microbial effects. Recent research in animals has also demonstrated that oleuropein may potentiate the response of 5′-deiodinase, the enzyme responsible for the irreversible conversion of thyroxine (T4) into triiodothyronine (T3), the active thyroid hormone.
Caffeine (1,3,7-trimethylxanthine) and Theomobrine (3,7-dimethyl-1H-purine-2,6-dione):
Caffeine is the most widely consumed, and perhaps one of the most reviewed, psychoactive compounds. Its physiological effects in a range of areas have been well-documented, including exercise performance, information processing, alertness and mood enhancement, attention, and awareness, along with its anti-lipogenic and lipolytic abilities. Caffeine is also the most well-known in the methylxanthine compound class, the constituents of which inter-metabolize into one another in the human body and largely share similar effects.
Various clinical trials have demonstrated that xanthines – including caffeine and theobromine – exert potent lipolytic (the breakdown of triglycerides into fatty acids) and oxidative actions as sympathomimetic amines. In less scientifically-complex parlance, this means caffeine is forcing your body to preferentially use adipose tissue as a fuel source for the oxidative provision of ATP (your body’s energy currency).
Evidence for xanthine’s capacity as lipolytic agents is widely available. In a clinical study featuring four separate trials in both normal and obese subjects, for example, caffeine was found to significantly increase fatty acid metabolism (as measured by serum fatty acid concentration), resting metabolic rate, and total fat oxidation – suggesting the preferential substrate selection spoken about above occurs in both normal and obese individuals. Other trials have demonstrated the effects of methylxanthines on total fat mass (reduction), lean body mass (increases), stamina and endurance, as well as cardiovascular capacity.
Additionally, as selective cAMP potentiators, through the beta-adrenergic pathway, caffeine and theobromine have been hypothesized to exert a synergistic effect on lipolysis when combined with forskolin.
Bacopa monnieri Extract (whole plant) (50% bacosides):
Bacopa monnieri (BM), also known as the water hyssop commonly, or as Brahmi in Ayurvedic texts, is a small creeping herb endemic to sub-tropical India. The herb has been used in traditional Indian medicine for well over one thousand years, with its first recorded usage coming in the 6th century A.D. In this traditional context, BM has been used for a wide-range of purposes, including as a treatment of asthma and epilepsy.
More recently, BM has been the subject of numerous cognition and memory trials, as the plant has a well-established nootropic effect. Likely through modulation of the serotonin reuptake system, clinical trials in healthy human beings have demonstrated that BM possesses a significant effect on the retention of newly-learned information. In several trials utilizing a 300mg daily serving, BM was also shown to decrease the recall delay of newly learned information and reduce short term forgetfulness – suggesting that the herb’s effect on the serotonic and cholinergic systems are increasing the encoding (the literal storing) of memory information.
Beyond cognition and memory encoding, BM has also been demonstrated to function as a potent adaptogen and relaxant – which in the Core BURN formula may help to smooth the effect curve of the product’s stimulants, reducing jitteriness or “crash.”
ForsLean® (Coleus forskohlii) (root) (20% forskolin): Coleus forskohlii is a small perennial endemic to various tropical regions in the world, including South America, sub-Saharan Africa, and India. While the West has recently taken interest in the plant due to the pharmacological properties of its primary bioactive, forskolin, Coleus forskholii preparations and tinctures have been used in both South American and African traditional folk medicinal systems, as well as extensively within Ayurveda.
Due to the ever-increasing interest in the plant’s verifiable pharmacological and physiological effects, however, Coleus forksholii and its extracted constituents have been the subject of numerous animal and human clinical trials in the past decade, primarily in its patented form of ForsLean. These trials have demonstrated the plant to have various effects and applications, including as a lipolytic and anti-lipogenic, and as a powerful antioxidant.
A recent double-blind, randomized, and placebo-controlled human clinical trial featuring obese men found that the daily implementation of ForsLean, for twelve weeks, led to significantly better weight loss outcomes as compared to controls. Overweight men in the ForsLean group experienced not only improved body composition (as measured by total non-lean mass), but also statistically significant increases in lean body mass.
In a separate 8 week trial, in overweight females, ForsLean was found to significantly reduce total bodyweight and significantly increase lean body mass relative to controls. Weight loss was statistically significant after 4 and 8 weeks and the mean amounted to 4.3 and 9.17 lbs respectively.
ForsLean – and more specifically, forskolin – achieves this effect by rapidly, potently, and dose-dependently increasing an important metabolic enzyme known as adenylate cyclase. Adenylate cyclase is an enzyme responsible for catalyzing the formation of cyclic adenosine monophosphate (cAMP) from adenosine triphosphate (ATP). This increase in cAMP formation eventually leads to the activation of an enzyme, protein kinase A, which in turn will phosphorylate and hence activate the enzyme, Hormone Sensitive Lipase (HSL) – the rate-limiting enzyme necessary for stored triglycerides within adipocytes to be released as free fatty acids and utilized for energy.
In more basic terms, this means that forskolin quite literally frees up more fatty acids to be used as fuel for exercise – more or less the perfect scenario in a product such as Core BURN!
Yohimbe Extract (Pausinystalia yohimbe) (bark) (8% Yohimbine alkaloids):
Extracts or preparation of Pausinystalia yohimbe, and related sub-species, have been used in traditional and folk medicinal systems such as Ayurveda and Unani for centuries. More recently, the principal bioactive compound in Pausinystalia yohimbe, both as a whole plant, and its extracted components, has been the subject of numerous clinical trials investigating its various physiological pathways.
In particular, recent research has shown that yohimbe bark extracts exert a powerful pre-synaptic inhibiting effect on alpha-adrenergic receptors – making it a potent adrenergic antagonist. This effect seems to be localized and largely specific to adipocytes, attaching to their adrenergic receptor sites and preventing them from receiving the catecholamines (norepinephrine and epinephrine) that would normally initiate growth signals.
While limited, there is some evidence in human, clinical trials to suggest that Yohimbine’s postulated mechanisms of action translate into practical effects. In a placebo-controlled trial involving 20 healthy, lean soccer players, subjects were given 20mg/day in two equal servings, for 21 days. At 21 days, the Yohimbine group reflected small but significant reductions in both total fat mass and bodyfat percentage as compared to controls – at least partially suggesting that Yohimbine may have a plausible role in combination with diet and exercise in weight management.
Advantra-Z® Bitter Orange Extract (Citrus aurantium) (fruit) (50% synephrine):
Synephrine is a naturally-occurring alkaloid with adrenergic agonist activity, structurally related to epinephrine, norepinephrine, ephedrine, and other compounds with a phenethylamine base structure. Despite its chemical similarity to these compounds, synephrine in its various isomers exerts unique effects on adrenergic receptors, in particular, and the human body, in general.
Synephrine exists in three isomer forms: para-, meta- and ortho-synephrine. The molecular changes between the three isoforms are minute, but even this small change results in significant alterations to each isomer’s physiological and pharmacokinetic profile. Two of synephrine’s isomers, both p- and m-synephrine, have been shown to naturally occur in mammals (in low concentrations). As a sympathomimetic, synephrine has been the subject of numerous trials, assessing its effects on weight management, thermogenesis, metabolic rate, and caloric expenditure. In a double-blind, randomized, and placebo-controlled trial involving 10 healthy individuals, the p-synephrine isomer was administered at a 50mg serving, both alone, and in combination with hesperidin and naringin. The authors measured resting metabolic rate (RMR), blood pressure, and heart rate, along with subjective feelings of mood and energy, at baseline, and at 45-mintues and 75-minutes after ingestion. The authors reported a significant increase in RMR in each of the supplement groups, relative to placebo.
In addition to studies on synephrine in its various isomers, Advantra-Z®, the specific form of synephrine utilized in Core BURN, has itself and in combination with other ingredients, been the subject of various clinical trials in humans. In a randomized, double-blind, placebo-controlled trial featuring 70 obese adults, a formulation containing Advantra-Z® was found to significantly reduce fat mass, body weight, and hip and waist girth as compared to controls, while leading to an increase in lean mass. As the authors comment, these results are in-line with a recent systematic review of human clinical studies involving Citrus aurantium, that revealed the ingredient to reliably increase resting metabolic rate up to 7.2%, increase energy expenditure of up to 13.4%, and weight loss of over 2.9 kg, with no serious adverse events in any of the trials.
In addition, the combination of caffeine and synephrine appears to potentiate each ingredient’s effects – with rates of fatty acid liberation, heart rate, metabolic rate, and fatty acid oxidation increased in clinical trials featuring the combination. In the same systematic review mentioned above, the authors note that the combination of synephrine and caffeine led to a small but significant reduction in fat mass of 3lbs, and a reduction in bodyfat of 2.9%.
Combined with not only caffeine, but the other ingredients in Core BURN, Advantra-Z® appears to be a potent weapon in the arsenal for body composition and weight management.