Quote:
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USPlabs Recreate
Ingredient Profile:
750mg (proprietary blend) Carralluma Fimbrata, Coffea Arabica L., Olea Europaea, Caffeine, Forslean (extract of Colleus Forskholli), (2-(4-(beta-D-Glucopyranosyloxy)phenyl)-5-hydroxy-6,7-dimethoxy-4H-1-benzopyran-4-one) extracted from Microtea Debilis.
Method of Action:
Forskolin (Forslean):
An adenlyate cyclase activator, which in turn increases intracellular levels of cAMP (cyclic adenosine monophosphate), which eventually works to stimulate lipolysis in adipose cells. Beta 2-adrenergic agonists such as ephedrine and clenbuterol actually work by increasing cAMP as well. Unfortunately, because they work at a receptor, their effectiveness can decrease with continued use as the body down-regulates the number of receptors available. Forskolin bypasses the receptor and directly activates adenylate cyclase, obviating the need for “cycling”, and foregoing potential risks associated with beta-2 Agonists. Another potential benefit is that accumulation of cAMP in skeletal muscle may provide an anti-catabolic/anabolic effect as well [1]. A study which evaluated body composition found that when they gave forskolin to men (without having them change their normal habits), they were able to reduce body fat percentage by 4.14%. In addition, they were able to lose 4.52 kg (9.9 lb) of fat mass and gained 3.71 kg (8.2 lb) of lean body mass (muscle tissue), over a 12 week period [2]. It also slightly increased free testosterone in men, but this would not likely occur in women.
Caffeine:
If there were one potential downfall of forskolin, it would be that the body still has a few mechanisms to reduce cAMP levels, either via modulation of adenylate cyclase activity or degradation of cAMP itself. Caffeine has the potential to work against such mechanisms to increase the effects of forskolin.
Olea europaea:
An extract (performed in a very particular way) of olive leaf, was shown to possess potent thyroid stimulatory properties when it increased T3 levels by nearly 300% as compared to the control group in a study using an animal model [3]. Here is the best part. Unlike many plant extracts which only have an effect in animal models when the dose employed is the equivalent to a human consuming their entire bodyweight of the substance per day, this actually works at a very low dose. Additionally, the thyroid stimulating effects with this plant are dose-dependent.
Coffea Arabica L:
Again, a very precise extract of this substance has been shown to inhibit the enzyme 11-B-hydroxysteroid dehydrogenase type 1, both selectively and very potently [4]. In addition, it was shown to do so in muscle and adipose cells. Why is this good? 11beta-HSD1 is an enzyme responsible for converting the very weak glucocorticoid, cortisone, into the much more powerful, cortisol. We all know that excess cortisol can hamper your progress in the gym, and with the stress of living in our modern world, it’s certain that few people don’t have elevated cortisol levels. Unfortunately, this particular enzyme works against what we all as athletes and bodybuilders would like and works to increase cortisol levels. In addition, another sad bit of news is that activity of this enzyme only seems to increase as we get older [5].
By inhibiting 11beta-HSD1, it is thought that it could be used to treat obesity (reduce body fat) and improve insulin sensitivity. Additionally, a beneficial effect upon muscle mass would be expected [6].
Caralluma fimbriata:
A very specific extract of this plant was shown to reduce waist size by almost one and a quarter inches in only 8 weeks, while decreasing appetite by 20% as compared to placebo [7]. In addition, those taking the active ingredient reduced consumption of sweets, refined sugars, cholesterol and saturated fats by the conclusion of the study as compared to placebo. At the same time, consumption of fruits, vegetables and fish didn’t change. In other words, it nearly “made” them follow a healthy diet and make better food choices, while also causing them to eat less. The group taking the caralluma lost 1.5 kg (3.3 lb) of fat mass as well, over the course of the study. It has been used for centuries by tribal populations that wished to suppress their appetite. It also has a well established safety record and had shown no serious adverse effects. As far as how it works, it is thought that steroidal glycosides present in the plant may increase ATP in the hypothalamus, potentially “tricking” it into thinking that energy or food intake is sufficient so there is no need to increase appetite [7,8].
(2-(4-(beta-D-Glucopyranosyloxy)phenyl)-5-hydroxy-6,7-dimethoxy-4H-1-benzopyran-4-one) extracted from Microtea Debilis) Cactus Alkaloids:
A compound found in a certain cactus plant, has a structural similarity to norepinephrine. It has both alpha and beta-adrenergic activity [9]. Additionally, it directly stimulates postsynaptic receptors while enhancing the physiological effects of norepinephrine via increasing synthesis of it and inhibiting its’ reabsorption. The end result is a stimulant effect similar to ephedrine, without the “all over the place” behavior. In fact, it produces a great deal of focus.
Literature:
[1] Navegantes LC, Resano NM, Migliorini RH, et al. Catecholamines inhibit Ca(2+)-dependent proteolysis in rat skeletal muscle through beta(2)-adrenoceptors and cAMP. Am J Physiol Endocrinol Metab. 2001 Sep;281(3):E449-54
[2] Godard MP, Johnson BA, Richmond SR. Body composition and hormonal adaptations associated with forskolin consumption in overweight and obese men. Obes Res. 2005 Aug;13(8):1335-43.
[3] Al-Qarawi AA, Al-Damegh MA, ElMougy SA. Effect of freeze dried extract of Olea europaea on the pituitary-thyroid axis in rats. Phytother Res. 2002 May;16(3):286-7
[4] Atanasov AG, Dzyakanchuk AA, Schweizer RA, et al. Coffee inhibits the reactivation of glucocorticoids by 11beta-hydroxysteroid dehydrogenase type 1: a glucocorticoid connection in the anti-diabetic action of coffee? FEBS Lett. 2006 Jul 24;580(17):4081-5.
[5] Wiegand S, Richardt A, Remer T, et al. Reduced 11{beta}-hydroxysteroid dehydrogenase type 1 activity in obese boys. Eur J Endocrinol. 2007 Sep;157(3):319-324
[6] Walker BR. Extra-adrenal regeneration of glucocorticoids by 11beta-hydroxysteroid dehydrogenase type 1: physiological regulator and pharmacological target for energy partitioning. Proc Nutr Soc. 2007 Feb;66(1):1-8
[7] Kuriyan R, Raj T, Srinivas SK, et al. Effect of Caralluma fimbriata extract on appetite, food intake and anthropometry in adult Indian men and women. Appetite. 2007 May;48(3):338-44.
[8] MacLean DB, Luo LG. Increased ATP content/production in the hypothalamus may be a signal for energy-sensing of satiety: studies of the anorectic mechanism of a plant steroidal glycoside. Brain Res. 2004 Sep 10;1020(1-2):1-11
[9] Sato PT, Neal JM, Brady LR, et al. Cactus alkaloids. XVI. Isolation and identification of alkaloids in Coryphantha ramillosa. J Pharm Sci. 1973 Mar;62(3):411-4
[10] Girotti C, Ginet M, Demarne FC, et al. Lipolytic activity of cirsimarin extracted from Microtea debilis. Planta Med. 2005 Dec;71(12):1170-2