USP Labs LLC., Product Literature:
Anabolic Pump, PowerFULL, SuperCissusRx, ReCreate, and PRIME.
08/08/08
Anabolic Pump
Ingredient Profile:
750mg (proprietary blend) Phellodendron, Lagerstroemia Speciosa.
Method of Action:
The current literature reflects a dual action of Anabolic Pump: A GU (glucose uptake) effect, displaying a specificity for myocytes, as well as potent anti-lipogenic action, thereby reducing the biosynthesis, differentiation, proliferation, and accumulation of lipids in various forms. The data reflects that each ingredient is achieving these effects by somewhat exclusive pathways; though the exact pathway through which Corosolic Acid and Tannins complete these actions are somewhat unknown. Let us begin with Lagerstroemia, relative to Corosolic Acid and Tannins found within it.
Corosolic Acid:
has demonstrated extremely potent glucose-uptake activity in both human trials [3] as well as rat trials [1, 2, 4, 5, 6]. CA’s MGU (muscle glucose uptake) appears to be regulated by the induction of insulin-reactive cascades, though the exact cascades are currently unclear. It is postulated, that in a manner corollary to Berberine, CA is directly altering response to downstream messengers; thereby altering the catabolic:anabolic response pathway. Further, CA prevents lipid metabolism by directly regulating PPAR-Gamma2 and therefore lipid mRNA expression [1]. PPAR-Gamma2 is part of a nuclear receptor family that has diverse physiological action in the body; however, it is paramount in this respect, as PPAR-y2 directly regulates the distribution of adipose in the humab body – specifically, controlling regulation of adipose storage.
Tannic Acid:
This second compound in Lagerstroemia has shown very potent anti-diabetic activity by way of stimulating glucose uptake in muscle cells and by inhibiting key genes related to fat accumulation [7]. Current data reflects this constituent of LS exerts transcriptional control over PPAR-y2 as well; it achieves this by inhibiting the binding of PPAR-y2 to target enzymes (such as CPT-1). As each product within Anabolic Pump, Tannic Acid directly stimulates GLUT4 translocation itself, without directly inducing Insulin’s release [8]. By which exact mechanism is unknown.
Berberine:
The final compound in question is Phellodendron; or more specifically, Berberine. Berberine is the most interesting of all three compounds, due to its direct regulation of the master regulatory switch of energy transaction within the body: AMPk. AMPk regulates the manner in which the human body synthesizes, and expends energy. It directs the body’s response of extracellular energy mechanisms, in order to meet intracellular demand for energy. AMPk regulates the biosynthesis of plasma triglycerides, FAs, and cholesterol, as well as regulating their proliferation via exerting transcriptional control over PPAR-a and PPAR-y [9. 10] in adipose and striated muscle. It not only inhibits lipid synthesis, and induces lipolysis, thereby decreases triglycerol stores (adipose), but modulates the rate-limiting step to B-Oxidation of FAs: CPT-1. It achieves this by inhibiting malonly-cOa, via malonyl-cOa-decarboxlyase, and ACC, and thereby directly increases levels of CPT-1; the target enzyme of the PPAR-Family, responsible for mitochondrial admission of FAs, and their subsequent oxidation. Further, Berberine mediated AMPk expression induces insulin-independent GLUT4 regulation [9]. The whole body improvement in Insulin Sensitivity derived from Berberine is thought to be a result of mitochondrial respiration inhibition; thereby increasing demand for ATP, subsequent AMPk phosphorylation, and the induction of glycolysis and glycogen replenishment [14]. While Anabolic Pump is often solely conceptualized as a glucose disposal agent, its direct control over lipogenic and energy expenditure mechanisms ensures tissue recomposing via preferential energy use – that is, it genetically alters the manner in which your body diverts energy to adipose and striated muscle; decreasing the former, while increasing the latter.
It should also be noted that clinical, long-term trials [11, 12] using the aforementioned ingredients have not noted any adverse biological effects. Microbiological assays [13] have also revealed no damaging effects to mammalian cell function. Further, it should be noted that the vast majority of the clinical research presented in this report converges on a major, health-related note: Both LS and Berberine possess potent anit-lipogenic activity, and thereby mitigate LDL cholesterol, and plasma triglyceride formation and function – key contributors to coronary disease. It should also be noted that both ingredients mitigate abnormal blood pressure levels.
Literature:
[1]Banaba Leaf Research Update Effects of dietary mulberry, Korean red ginseng, and banaba on glucose homeostasis in relation to PPAR-alpha, PPAR-gamma, and LPL mRNA expressions. Life Sci. 2005 Nov 12;77(26):3344-54. Department of Food and Nutrition, College of Human Ecology, Sookmyung Women's University, Seoul, Korea.
[2]Effects of malted barley extract and banaba extract on blood glucose levels in genetically diabetic mice. J Med Food. 2004 Winter;7(4):487-90
[3]Antidiabetic activity of a standardized extract (Glucosol) from Lagerstroemia speciosa leaves - banaba - in Type II diabetics. A dose-dependence study. J Ethnopharmacol. 2003 Jul;87(1):115-7. Judy WV, et al.
[4]An extract of Lagerstroemia speciosa L. has insulin-like glucose uptake-stimulatory and adipocyte differentiation-inhibitory activities in 3T3-L1 cells. J Nutr. 2001 Sep;131(9):2242-7
[5]Antiobesity activity of extracts from Lagerstroemia speciosa L. leaves on female KK-Ay mice. J Nutr Sci Vitaminol (Tokyo). 1999 Dec;45(6):791-5.
[6]Hypoglycemic effect of extracts from Lagerstroemia speciosa L. banaba leaves in genetically diabetic KK-AY mice. Biosci Biotechnol Biochem. 1996 Feb;60(2):204-8.
[7]Tannic acid in banaba herb Tannic acid stimulates glucose transport and inhibits adipocyte differentiation in 3T3-L1 cells. J Nutr. 2005 Feb;135(2):165-71. Liu X, Kim et al.
[8]Antidiabetes and Anti-obesity Activity of Lagerstroemia speciosaGuy Klein,1 et al.
[9]Berberine, a natural plant product, activates AMP-activated protein kinase with beneficial metabolic effects in diabetic and insulin-resistant states.Department of Biological Sciences, Seoul National University, San 56-1, Sillim-Dong .
[10]Berberine-stimulated glucose uptake in L6 myotubes involves both AMPK and p38 MAPK Zhe Cheng et.
[11] Effect of a proprietary Magnolia and Phellodendron extract on stress levels in healthy women: a pilot, double-blind, placebo-controlled clinical trial.Nutr J. 2008: (7): 11.Douglas S Kalman et al.
[12] Phellodendron and Citrus extracts benefit cardiovascular health in osteoarthritis patients: a double-blind, placebo-controlled pilot study.Nutr J. 2008: (7):16. Laboratory of Nutrition and Nutritional Biochemsitry, Department of Biochemistry, University of Yaounde, Cameroon. Oben et al.
[13] Genotoxicity Study of Water Extract of Anemarrhena asphodeloides
and Phellodendron amurense in Bacterial and Mammalian Cell Systems.
Young-Shin Chung et al.
[14] Berberine and Its More Biologically Available Derivative, Dihydroberberine, Inhibit Mitochondrial Respiratory Complex I:A Mechanism for the Action of Berberine to Activate AMP-Activated Protein Kinase and Improve Insulin Action. Diabetes and Obesity Research Program, Garvan Institute of Medical Research, Darlinghurst, Australia. Nigel Turner et al.
PowerFULL
Ingredient Profile:
750mg (proprietary blend) Extracted Sapogenins from Chlorophytum Borivillanum, and Dolichos Pruriens L.
Method of Action:
As stated, PowerFULL Is comprised of two major components. PureSAP, an extraction of steroidal sapogenins from the Chlorophytum (Velvet Bean) Plant, and PureDOPA, an extract of Dolichos Pruriens L., engineered for high concentrations of the Dopaminergic precursor, L-DOPA. As such, each adjuvent must be discussed separately in its pertinent effects.
PureDOPA:
Containing said extract of Dolichos Pruriens L., induces an increase in endogenous (natural) L-DOPA production that vastly outperforms synthetic L-DOPA with 110% higher peak concentrations, 165% longer peak concentrations, and an onset time around 50% shorter [1]. LD itself then leads to an increase in natural Growth Hormone production, by way of modulating the Dopaminergic-Pituitary-GH release axis;research has reflected that the Substantia Nigra (part of mid-brain containing Dopamine ions) need not be in a degraded state to illicit to prominent GH induction; the relevant data displays such effects even in healthy, normal patients[3, 4]. Research has also shown that this increase is most likely occurring by way of LD-induced hypothalamtic GHRH (growth hormone releasing hormone) production [2, 4].
It should be readily noted that the increases of plasma GHRH and GH [1,2,3,4] have been noted as a result of synthetic L-DOPA administration. However, Dolichos P.L., not only contains natural sources of L-DOPA, with demonstrated efficacy at raising L-DOPA (with its subsequent effect on GHRH and GH) of twice to three times that of synthetic L-DOPA [1, 6, 7], but also most likely contains independent L-DOPA enhancing adjuvents, or possibly inherent decarboxylase inhibitors [6. 7. 8]. The latter scenario is likely as Dopamine and its metabolites have not been found in the nigrostriatal tract after Mucuna administration [8], as well as a lack of dyskensia in Parkinson’s patients [1] and lack of side-effects in normal patients [3]. This data is indicative of a lack of Dopaminergic transmission in peripheral tissues.
The final point of concern relative to L-DOPA, and therefore Dolichos P.L., is long-term safety and tolerability concerns associated with synthetic L-DOPA administration. Synthetic L-DOPA has been noted to have many adverse side-effects including hypertension, dyskenisia (uncontrollable movement), dizziness, nausea, and so on. However, Dolichos has not shown these same side-effects in Parkinson’s patients [1], and L-DOPA administration has not displayed these same side-effects in healthy, normal subjects [2, 3].
Along with the above side-effects, synthetic L-DOPA has been shown to have damaging effects to dopamine ions in the region of the brain most responsible for dopamine transmission (the substantia nigra). This can lead to an aggregate decrease in endogenous dopamine production; however, DLP has displayed neuro-restorative effects in the relevant data, increasing levels of serotonin, dopamine, levadopa, and norepinephrine [9]. This is most likely due to a more efficient transmission of dopamine, and Mucuna containing NADH and COQ-10, both powerfull neurorestorative compounds [9. 10].
Literature:
[1] Mucuna pruriens in Parkinson's disease: a double blind clinical and pharmacological study. Katzenschlager R, et al.
[2] L-dopa stimulates release of hypothalamic growth hormone-releasing hormone in humans. K Chihara, et al.
[3]Intravenous levodopa administration in humans based on a two-compartment kinetic model. Mollie Gordon, et al.
[4] Effect of oral administration of L-dopa on the plasma levels of growth hormone-releasing hormone (GHRH) in normal subjects and patients with various endocrine and metabolic diseases. Mitsuhashi S, et al.
[5] Bioavailability of L-DOPA from HP-200-a Formulation of Seed Powder of Mucuna pruriens (Bak): a Pharmacokinetic and Pharmacodynamic Study. S.Mahajani et al.,
[6] Mucuna pruriens proves more effective than L-DOPA in Parkinson's disease animal model. Ghazala Hussian, Bala V. Manyam
[7] Beans (Mucuna Pruriens) For Parkinsons Disease:An Herbal Alternative. Bala V. Manyam, M.D.,
[8] Effect of antiparkinson drug HP-200 (Mucuna pruriens) on the central monoaminergic neurotransmitters. Bala V. Manyam et al.,
[9] Neuroprotective effects of the antiparkinson drug Mucuna pruriens. Manywam et al.,
[10] Protecting Axonal Degeneration by Increasing Nicotinamide Adenine Dinucleotide Levels in Experimental Autoimmune Encephalomyelitis Models.Shinjiro Kaneko, et al.
PureSAP:
Containing the powerful plant sterols Stigmasterol, Hecogenin,Desoxydiosgenin, Tigogenin, Neotigogenin vis-à-vis extraction from the Velvet Bean Plant, is thought to have a dual effect on hormonal homeostasis; a) by directly raising endogenous levels of Testerone via AR (androgen receptor) binding [1,3]; and, b) by serving as non-hormonal intermediates in the biosynthesis of cholesterol derivatives [1,2,3]. While research is not abundant, the current data hypothesizes that the triterpene sapogenins – primarily Stigmasterol – contained in Chlorophytum Borivillanum, undergo enzymatic conversion of the Testes in order to produce Testoserone [1, 3]. It is thought this action is possible via the incredibly similar structure of Stigmasterol to Testerone. Further, the other sapogenins found in C.B., have been found to bind directly to AR [1] without exerting intrinsic action at the receptor site – that is, while the compounds bind and therefore increases steroidal mRNA expression, and thereby increase protein synthesis and muscle mass, they do not modulate negative feeback loops. The limited clinical data reflects only increases, and not decreases, to endogenous Testosterone production from C.B., [3].
Literature:
[1] Salvi VS, Mukhurjee D, Engel CR (1986). Steroids and related products LIV. The synthesis of 11-oxa steroids VI. The Synthesis of11-oxatestosterone. Steroids 48(1-2):47-53.
[2] Johns W (1970) The 12a,13b-Etiojervance Analog of Testosterone. J. Org. Chem. 36(5): 711-19.
[3] Kaushik, N (2005) Saponins of Chlorophytum Species. Phytochemistry Reviews. 4(2-3): 191-196.
SuperCissusRx
Ingredient Profile:
750mg Cissus Quadrangularis.
Method of Action:
Cissus Quadrangularis is an ancient medicinal plant native to the hotter parts of Ceylon and India. It was prescribed in the ancient Ayurvedic texts as a general tonic and analgesic, with specific bone fracture healing properties. Modern research has shed light on Cissus' ability to speed bone healing by showing it acts as a glucocorticoid antagonist [1,2]. Since anabolic/androgenic compounds are well known to act as antagonists to the glucocorticoid receptor as well as promote bone growth and fracture healing, it has been postulated that Cissus possesses anabolic and/or androgenic properties [1,3]. In addition to speeding the remodeling process of the healing bone, Cissus also leads to a much faster increase in bone tensile strength. In clinical trials Cissus has led to a fracture healing time on the order of 55 to 33 percent of that of controls. That Cissus exerts antiglucocorticoid properties is suggested by a number of studies where bones were weakened by treatment with cortisol, and upon administration of Cissus extract the cortisol induced weakening was halted, and the healing process begun.
While the increased rate of bone healing may be of great significance to persons suffering from chronic diseases like osteoporosis [4], the antiglucocorticoid properties of Cissus are likely of much more interest to the average bodybuilder or athlete, since endogenous glucocorticoids, particularly cortisol, are not only catabolic to bone, but catabolize muscle tissue as well. Numerous studies over the years have suggested that glucorticoids, including the body's endogenous hormone cortisol activate pathways that degrade not only bone, but skeletal muscle tissue as well. A recently published report documented exactly how glucocorticoids (including cortisol) induce muscle breakdown: They activate the so-called ubiquitin-proteasome pathway of proteolysis [5]. This pathway of tissue breakdown is important for removing damaged and non-functional proteins. However, when it is overactive during periods of elevated cortisol (e.g disease states, stress, and over-training) excess amounts of normal tissue are broken down as well. By exerting an anabolic, antiglucorticoid effect cissus helps preserve muscle tissue during times of physical and emotional stress. Further, Cissus has also been shown to attenuate oxidative stress, and combat lipid peroxidation and pro-inflammatory cytokine pathways [8]; most importantly, Cissus immediately inhibits levels of TNF-1 Alpha (tumor necrosis factor) a damaging isoform responsible for overzealous tissue destruction.
Besides the above-mentioned properties of Cissus, the plant is also rich in the vitamins/antioxidants vitamin C and beta-carotene. As analyzed, Cissus quadrangularis contained ascorbic acid 479 mg, and carotene 267 units per 100g of freshly prepared paste in addition to calcium oxalate [6].
Cissus also possess analgesic properties on a mg per mg basis comparable to aspirin or anti-inflammatory drugs like ibuprofen. Cissus quadrangularis, which has been proved to be highly effective in relieving pain, reduction of swelling and promoting the process of healing of the simple fractures as well as in curing the allied disorders associated with fractures [7]. The mechanism through which Cissus exerts its analgesic and anti-inflammatory properties has not been well characterized. It may act centrally, but the anti-inflammatory features suggest that it acts by preventing the conversion of arachidonic acid to inflammatory prostaglandins.
[1] Chopra SS, Patel MR, Awadhiya RP. Studies of Cissus quadrangularis in experimental fracture repair : a histopathological study Indian J Med Res. 1976 Sep;64(9):1365-8
[2] Chopra SS, Patel MR, Gupta LP, Datta IC. Studies on Cissus quadrangularis in experimental fracture repair: effect on chemical parameters in blood Indian J Med Res. 1975 Jun;63(6):824-8.
[3] PRASAD GC, UDUPA KN. EFFECT OF CISSUS QUADRANGULARIS ON THE HEALING OF CORTISONE TREATED FRACTURES. Indian J Med Res. 1963 Jul;51:667-76.
[4] Shirwaikar A, Khan S, Malini S. Antiosteoporotic effect of ethanol extract of Cissus quadrangularis Linn. on ovariectomized rat. J Ethnopharmacol. 2003 Dec;89(2-3):245-50.
[5] Combaret L, Taillandier D, Dardevet D, Bechet D, Ralliere C, Claustre A, Grizard J, Attaix D Glucocorticoids regulate mRNA levels for subunits of the 19 S regulatory complex of the 26 S proteasome in fast-twitch skeletal muscles. Biochem J. 2004 Feb 15;378(Pt 1):239-46.
[6] Chidambara Murthy KN, Vanitha A, Mahadeva Swamy M, Ravishankar GA. Antioxidant and antimicrobial activity of Cissus quadrangularis L. J Med Food. 2003 Summer;6(2):99-105.
[7] Panda, J Res Ayurv Siddha, 1990, 11, 7rences.
[8] Jainu et al., Attenuation of Neutrophil Infiltration and Proinflammatory Cytokines by Cissus Quadrangularis A Possible Prevention Against Gastric Ulcerogenesis. Journal of Pharmacotherapy. 2006: (5) 3: 33-42.
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.