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200 mg Isinokosterone
Information about Syntrabol from Derek Cornelius, President of Syntrax Innovations:
Isoinokosterone, also known as 20-Hydroxyecdysterone, is a polyhydroxylated sterolic invertebrate growth hormone. The action of this hormone is quite potent on insects and is actually necessary for their ongoing survival. Because there is much cross-reactivity and homology in invertebrate and vertebrate hormones, Doctor Burdette in 1960 began a pioneering work on the effects of ecdysteroids in vertebrates. As early as 1963, Burdette found that Isoinokosterone enhanced the rate of protein synthesis in mammalian tissue. This discovery brought many scientists to the table to study the effects of this interesting hormone. Over the next 36 years, scientists discovered that Isoinokosterone improves nearly every bodily function. I will gradually introduce you to this amazing dietary supplement by first reviewing the relevant research and then describing the real-world results.
In the early 60's, Burdette discovered that Isoinokosterone stimulated protein synthesis but the extent of its stimulatory actions was quite unknown. In the late 60's, some forward thinking Japanese scientists by the name of Okui and Otaki studied the effects of Isoinokosterone on protein synthesis in male and female mouse liver. In these experiments, the results were compared against the protein stimulating actions of 4-chlorotestosterone, a potent anabolic steroid. Amazingly, the time-course of change induced by Isoinokosterone and 4-chlorotestosterone was similar, with a maximum effect of 200% of controls observed after 5 hours and a return to initial levels after 12 hours. Many similar studies were performed which verified these results including ones which showed that the protein stimulation occurred in both the microsomal and polysomal fractions. Other studies in '69 and '84 showed that Isoinokosterone even stimulates protein synthesis in nervous tissue and increases nerve function. Obviously, the implications of this research are far-reaching. Could it be possible that Isoinokosterone promotes nerve tissue healing or even regrowth? Could it be possible that Isoinokosterone restores and supercharges nervous tissue to work at a maximum level in conjunction with the other parts of the body?
As positive results were obtained with Isoinokosterone, an increasing amount of research was performed looking for whole body anabolic effects. In 1969, another Japanese researcher named Hikino administered Isoinokosterone orally to mice for a period of 60 days. He found increased growth of the treated mice and enhanced protein synthesis in the liver and kidney. These results provided more evidence that Isoinokoste one might produce anabolic effects in vertebrates including humans. In the 1970's the former Soviet Union decided to become involved with the compound as a way to enhance their athletes and still beat drug tests. Many papers were published on Isoinokosterone in the subsequent years which convincingly showed its anabolic effects. Most of the experiments used 5mg per kilogram of body mass per day as the dosage. The effects were evaluated by measurements of the increased mass, total protein, and glycogen content of specific muscles (i.e. levator ani and tibialis anterior). As before, the results were compared against the effects of true vertebrate anabolic steroids. For instance, a researcher named Chermnykh compared the effects of Isoinokosterone and Methandrostenolone (a very potent anabolic steroid) in mice and found some astounding results. These compounds were given to two parallel experimental sets of mice for seven days-one untrained and the other subjected to training in the form of repeated swimming. Chermnykh found that both compounds caused anabolic increases of body mass only under the conditions of temporary training. Although Isoinokosterone generally stimulated physical capability for labour, Methandrostenolone could do the same only in association with temporary training. Methandrostenolone stimulated biosynthesis of the myofibrilar proteins in the musculus soleus but not in the musculus extensor digitorum longus, while Isoinokosterone increased the myofibrilar proteins in both muscles. Similar results have been confirmed in other vertebrate species consuming Isoinokosterone such as various birds, cattle, pigs, and even humans!
Besides the clear anabolic effects of Isoinokosterone, let us now look at the myriad of other positive benefits of this incredible compound. Because of the anabolic similarities between anabolic steroids and Isoinokosterone a researcher named Yoshida decided to see if there were any other similarities. In 1971 he studied whether Isoinokosterone would educe the hyperglycemic response to exogenous glucagons. As expected, Isoinokosterone had a suppressive effect on hyperglycemia. Interestingly, it did not affect those animals that had normal blood sugar levels. Furthermore, even though the blood sugar levels were unaffected in normal animals, it did stimulate the incorporation of glycogen into proteinaceous tissue such as liver and muscle. The scenario couldn't be more ideal! Here we have a compound that will powerfully stabilize your blood sugar levels and at the same time 'feed' your muscles and organs with energy-giving glycogen. Isoinokosterone is the perfect glycemic regulator. It will not only prevent you from having high blood sugar levels but also high insulin levels. High insulin levels stimulate lipogenesis-a process which basically makes you gain fat mass. With steady and even insulin levels, these fat-producing processes are halted in their tracks. Even blood sugar levels also are integral in the feeling of well being for a person as it ensures constant energy levels. Finally, Isoinokosterone actually pushes nutrients into muscle and organ tissue allowing for accelerated growth.
Some of you might be saying, 'WOW!' right now, but it gets even better. For instance, Isoinokosterone has a potent cholesterol lowering effect that is brought on by increasing cholesterol secretion in the bile as well as inhibiting de novo synthesis of cholesterol. While studying this effect, researches found that Isoinokosterone produced profound increases in the specific activity of phosphatidyl-ethanolamine and phosphyatidyl-serine. These phospholipids are integral to nearly every bodily process and are linked to enormous health benefits when they are stimulated. A final benefit of Isoinokosterone that was discovered while studying the cholesterol lowering effect was a potent hepatoprotective action. This is good news in light of the many potentially harmful compounds we ingest everyday in our highly processed environment.
The good news hasn't stopped yet! Isoinokosterone also has beneficial effects on the cardiovascular system. Because of its cell membrane stabilizing properties, Isoinokosterone has distinct anti-arrhythmia effects on the heart as well as a restorative action atherosclerosis. In fact, researchers have witnessed overall improvements in the hemodynamic conditions of the heart as well as heart contractility. Continuing along, Isoinokosterone has been also demonstrated to have analgesic properties as well as potent antioxidative properties. An important effect of Isoinokosterone for sports enhancement is its powerful anti-inflammatory properties. Almost too good to be true, Isoinokosterone has been shown to be as potent as cortisone acetate on specific inflammatory responses. We thus see Isoinokosterone as an agent that works against high cortisol levels. How so? Well, glucocorticoids like cortisol are released in response to stressors such as inflammation. By actively reducing or eliminating many of these stressors, Isoinokosterone prevents cortisol from being released from the adrenals. Since glucocorticoids are catabolic to proteinaceous tissue, it is highly beneficial to do whatever you can to restrict their release.
A final effect that is hinted at in the literature but not fully elucidated is Isoinokosterone's effect on the skin. Some research shows a positive effect on keratinization and differentiation but beyond that-nothing! I have seen, first hand, its positive effects on acne and believe me it is quite amazing. Even better is the fact that positive results can be seen within a few days. Combined with a high quality guggul extract, incredible improvements can be seen towards blemish-free skin. My guess would be that Isoinokosterone would also be an effective agent against psoriasis although I have no specific knowledge of it working therapeutically for this purpose.
One of the greatest things about Isoinokosterone is its utmost safety profile. Lately, some scoundrels in the industry are gung-ho on calling everything poisonous and dangerous that they do not distribute (you got it-they are supplement manufacturers). Unfortunately, they do a ton of damage to this industry by spreading their false information. Isoinokosterone though is beyond reproach. You would be hard pressed to find even one small detail that was negative about Isoinokosterone. In fact, it is so safe that the LD50 in mice is 9grams per kilogram. At this level, an adult male would have to consume nearly one kilogram of Isoinokosterone to have a good chance of killing you! Since, Isoinokosterone is recommended at a dosage of 500mg per day, there is basically zero chance of any problems.
'All of this research is great', you say, 'but what about real world results?' Some of you might remember that many years ago several companies were distributing a Suma extract that had Isoinokosterone in it. A whole handful of pills would only profit you less than 50mg of Isoinokosterone. Not only was the Isoinokosterone not very bioavailable but the dosage was way too low for noticeable results. The dilemma with this dietary supplement has always been obtaining a high potency, pure or semi-pure product that was priced reasonably. For years, there were only two choices: the ineffective Suma extract and pure Isoinokosterone from Russia that cost $20,000 per kilogram. Although effective, it would cost you about $50.00 per day retail to use it in sufficient quantity. Several years ago, I became very interested in this compound and began looking into all the possibilities of obtaining a high-potency, economical product. About a year ago, I started working with an Israeli company on a new process that would produce Isoinokosterone from an in vitro cell culture system. This process is extremely high-tech and yields a large amount product at a very cheap price. Finally, in the 20th century we are able to reap the benefits of this awesome compound.
At this point, real world results are restricted to the trials that the Russians did on this compound as well as the 20,000 people who have bought the new, pure version that is now available in the U.S. I communicated with several Russian researchers who extensively studied this compound on world-class athletes. Combined, they experimented on about 65 athletes. My staff and I have also communicated with at least 300 individuals. None of the reports that we received indicated any negative side effects. Furthermore, nearly every person, including the Russian scientists, indicated that they noticed significant increases in lean body mass, endurance, strength and feelings of well-being. Several experienced bodybuilders that I talked with indicated that they did better on Isoinokosterone than anything else except high dosages of anabolic steroids. One runner that I talked to shaved two minutes off his best time! Finally, a female fitness competitor gained 3 pounds of lean body mass while becoming significantly leaner.
As you can see, Isoinokosterone is truly a revolutionary supplement. Not only does it vastly increase athletic performance but it improves nearly every bodily process. This is very unusual in a compound that does all of this. Usually, like anabolic steroids, the many positive aspects will be somewhat offset by the few negative ones. Isoinokosterone, however, powerfully assists you in your goals while simultaneously improving every aspect of your health. It might not be magic, but Isoinokosterone is the best 'bug juice' I have every seen!
XXX (formerly Triax II)
XXX contains coleolin, from Coleus Forskohlii leaves, a highly unique and potent Ayurvedic nutritional supplement which activates the enzyme adenylate cyclase. This enzyme is linked to the core of metabolic and fat loss biological processes. Activating adenylate cyclase is a crucial component in optimizing your goals to lose unwanted fat stores and gain lean body mass.
The Unique Pharmacology of Coleus Forskohlii
Botanical Research Bulletin Vol.1, No. 6
A plant used since antiquity in Hindu and Ayurvedic traditional medicine is the source of an amazing compound of unique biological importance. The plant, Coleus forskohlii, is the source of the compound forskolin. A large-scale screening of medicinal plants by the Indian Central Drug Research Institiute in 1974 revealed the presence of a hypotensive and spasmolytic component of C. forskohlii which was maned coleanol. Additional investigation determined the exact chemical structure of this labdane diterpene and the name was changed to forskolin. Between 1981 and 1994 forskolin has been used in well over 5,000 in vitro research studies designed to better understand cellular processes governed by cAMP. While most of these studies have used this isolated constituent, there is evidence that other components within the potant extract enhance the absorption and biological activity of forskolin. The pharmacological activity of forskolin is, however, substantiating the traditional uses of C. forskohlii which includes such things as cardiovascular disease, abdominal colic, repiratory disorders, painful urination, insomnia, and convulsions.
Mechanisms of action
The basic mechanism of action of forskolin is the activation of an enzyme, adenylate cyclase, which increases cyclic adenosine monophosphate (cAMP) in cells. Cyclic AMP is perhaps the most important cell regulating compound. Once formed it activates many other enzymes involved in diverse cellular functions. Under normal situations cAMP is formed when a stimulatory hormone (e.g., epinephrine) binds to a receptor site on the cell membrane and stimulates the activation of adenylate cyclase. This enzyme is incorporated into all cellular membranes and only the specificity of the receptor determines which hormone will activate it in a particular cell. Forskolin appears to bypass this need for direct hormonal activation of adenylate cyclase via transmembrane activation. As a result of this activation of adenylate cyclase intracellular cAMP levels rise. The physiological and biochemical effects of a raised intracellular cAMP level include: inhibition of platelet activation and degranulation; inhibition of mast cell degranulation and histamine release; increased force of contraction of heart muscle; relaxation of the arteries and other smooth muscles; increased insulin secretion; increased thyroid function; and increased lipolysis. Recent studies have found forskolin to possess additional mechanisms of action independent of its ability to directly stimulate adenylate cyclase and cAMP dependent physiological responses. Specifically forskolin has been shown to inhibit a number of membrane transport proteins and channel proteins through a mechanism that does not involve the production of cAMP. The result is again a transmembrane signaling that results in activation of other cellular enzymes. Research is underway in the attempt to determine the exact receptors to which the forskolin is binding. Another action of forskolin is on antagonizing the action of platelet-activating factor (PAF) by interfering with PAF binding to receptor sites. PAF plays a central role in many inflammatory and allergic processes including neutrophil activation, increasing vascular permeability, smooth muscles contraction including bronchoconstriction, and reduction in coronary blood flow. After treatment of platelets with forskolin prior to PAF binding, a 30% to 40% decrease in PAF binding was observed. The decrease in PAF binding caused by forskolin was concomitant with a decrease in the physiological responses of platelets induced by PAF. However, this forskolin-induced decrease in PAF binding was not a consequence of cAMP formation as the addition of a cAMP analog could not mimic the action of forskolin. Additionally, the inactive analog of forskolin, dideoxyforskolin, which does not activate adenylyl cyclase, also reduced PAF binding was due to a direct effect of this molecule and its analog on the PAF receptor itself or to components of the post receptor signalling for PAF. The therapeutic ramifications of c. forskohlii based on the pharmacology of forskolin are immense. there are many conditions where a decreased intracellular cAMP level is thought to be a major factor in the development of the disease process. At present C. forskohlii appears to be extremely well indicated in these types of conditions which include: eczema (atopic dermatitis), asthma, psoriasis, angina, and hypertension. this review shall focus primarily on these relevant clinical applications.
Asthma and other allergic conditions
Allergic conditions such as asthma and eczema are characterized by a relative decrease in cAMP in the bronchial smooth muscle and skin respectively. As a result of this derangement, mast cells degranulate and smooth muscle cells contract. In addition, these allergic conditions are also characterized by excessive levels of PAF. current drug therapy for allergic conditions like asthma and eczema is largely designed to increase cAMP levels by using substances which either bind to receptors to stimulate adenylate cyclase (e.g., corticosteroids) or inhibit the enzyme phosphodiesterase which break down cAMP once it I formed (e.g., methyxanthines). These actions are different then forskolin's ability to increase the initial production of cAMP via a transmembrane activation of adenylate cyclase. The cAMP elevating action of forskolin supports the use of C. forskohlii extracts used alone or in combination with standard drug therapy in the treatment of virtually all allergic conditions. Coleus forskohlii extracts may be particularly useful in asthma as increasing cellular levels of cAMP results in relaxation of bronchial muscles and relief of symptoms in asthma. Forskolin has been shown to have remarkable effects in relaxing constricted bronchial muscles in asthmatics. The bronchials are composed of what is known as smooth muscle. this type of muscle is also found in the gastrointestinal tract, uterus, bladder, and arteries. Forskolin has been shown to have tremendous antispasmodic action on these various smooth muscles. this antispasmodic action of forskolin supports the long time use of C. forskohlii in the treatment of not only asthma, but also intestinal colic, uterine cramps (menstrual cramps), painful urination, angina, and hypertension. Forskolin's ability to relax smooth muscle in bronchial asthma is most probably due to an increase in cAMP, although forskolin has other anti-allergic activities such as inhibiting the release of histamine and the synthesis of allergic compounds.
One double-blind clinical study sought to determine the antiasthmatic effects of forskolin compared to the drug fenoterol. Sixteen patients with asthma were given single inhalative doses of fenoterol dry powder capsules (0.4 mg), metered doses of fenoterol (0.4 mg) and forskolin dry powder capsules (10.0 mg). All substances caused a significant improvement in respiratory function and bronchodilation. However, while the fenoterol preparations caused tremors and a decrease in blood potassium levels, no such negative effects were seen with forskolin.
In another study, the bronchodilating effect (after five minutes) of forskolin was as good as that produced by fenoterol in 12 healthy volunteers (nonsmokers) as determined by whole body plethysmography. Both substances were administered by metered dose inhalers. At the beginning (after three and five minutes) the protective effect of forskolin against inhaled acetylcholine was as good as that produced by fenoterol while later on (after 15 and 30 minutes) fenoterol resulted in a stronger action. Whether orally administered forskolin in the for of C. forskohlii extract would produce similar bronchodilatory effects has yet to be determined. However, based on the plant's historical use and additional mechanisms of action it is extremely likely.
Psoriasis is an extremely common skin disorder that seems to be caused by a relative decrease in cAMP when compared to another cell regulating compound, cyclic guanine monophosphate (cGMP). The result is a tremendous increase in cell division. In fact, cells divide in psoriasis at a rate 1,000 times greater than the normal rate. Preliminary studies have indicated that forskolin may be of great benefit to individuals with psoriasis via its ability to normalize the balance that exists between cAMP and cyclic GMP.
Perhaps the most useful clinical applications of C. forskohlii extracts will turn out to be cardiovascular diseases such as hypertension, congestive heart failure, and angina. The cardiovascular effects of C. forskohlii and its components have been studied in great detail. Its basic cardiovascular actions involve lowering of blood pressure along with imporoved contractility of the heart. Again this is related to increasing cAMP levels throughout the cardiovascular system which results in relaxation of the arteries and increased force of contraction. The net effect is tremendous improvement in cardiovascular function. Several clinical and animal studies have suggested forskolin may significantly lower blood pressure as well as improve heart function in patients. In one human study involving seven patients with dilated cardiomyopathy, forskolin was shown to improve left ventricular function primarily via reduction of preload and without rising metabolic costs. This study confirmed earlier animal studies which showed that forskolin increases the contractile force of heart muscle. In another human study, the hemodynamic effects of intravenous forskolin given to patients with dilated cardiomyopathy in a concentration of 3 mcg/kg/min was evaluated. Although systemic vascular resistance and diastolic pressure fell, forskolin had no effect on cardiac index, ejection fraction, or myocardial oxygen consumption at this very low dosage. However, when a small dosage of dobutamine was given along with the forskolin, and increase of all four parameters was observed. At a higher dosage (4 mcg/kg/min) forskolin induced an increase in impoved heart function by 19% and produced a 16% rise in heart rate. However, these changes were associated with symptomatic flush syndromes. These results indicate that forskolin may best be used in congestive heart failure in combination with other botanicals such as Crataegus species. Forskolin has also been shown to be a direct cerebral vasodialtor indicating that it may prove to be useful in cerebral bascular insufficiency and post-stroke recovery. An aditional mechanism of action particularly beneficial in a wide range of cardiovascular conditions is inhibition of platelet aggregation. In this case some good evidence indicates the a standaridized C. forskohlii extract is superior to pure forskolin. In an animal model for evaluating in vivo inhibition of platelet aggregation rats were divided into four groups. Group 1 received C. forskohlii extract (480 mg/kg supplying 20 mg/kg of forskolin); Group 2 received forskolin (20 mg/kg), group 3 received dipyridamole; and Group 4 served as the control. All treatments were given orally once daily. ADP-induced platelet aggregation was measured on odd days 1 through 15. All three treatments produced significant inhibition of platelet aggregation. On day 15, the percent inhibition were approximately 42% for Group 1, 37% for Group 2, and 52% for Group 3. Hence, the extract of C. forskohlii produced greater inhibiiton than the pure forskolin.
In clinical studies, forskolin has been shown to greatly reduce intra-ocular pressure (IOP) when it is applied directly to the eyes. This effect indicates that topical forskolin preparations may turn out to be of great benefit in the treatment of glaucoma. Unlike current drug therapy, forskolin actually increases intraocular blood flow, has no side effects, and does not induce miosis.
Other possible clinical applications
C. Forskohlii extracts concentrated and standardized for forskolin content may prove to be useful in a number of other clinical applications including weight-loss programs, hypothyroidism, malabsorption and digestive disorders, depression, prevention of cancer metastases, and immune system enhancement. Here's why.
Lipolysis, the breakdown of stored fat, in regulated by cAMP. Forskolin has been shown to stimulate lipolysis as well as inhibit the synthesis of fat in adipocytes. Forskolin has also been shown to counteract the decreased response of fat cells to lipolytic hormone like epinephrine associated with aging.
Forskolin has been shown to increase thyroid hormone production as well as stimulate thyroid hormone release.
Malabsorption and digestive disorders:
Forskolin stimulates digestive secretions including the release of hydrochloric acid, pepsin, amylase, and pancreatic enzymes. Forskolin has been shown to promote nutient absorption in the small intestine. C. forskohlii extracts may prove to be quite useful in treating dry mouth as forskolin increases salivation.
Forskolin has been shown to exert antidepresant activity in animal studies.
Forskolin has been shown to be a potent inhibitor of cancer metastasis in mice injected with malignant cells. As little as 82 mcg administered to mice inhibited metastases by over 70%.
Immune system enhancement:
Forskolin exhibits potent immune system enhancement (primarily through activation of macrophages and lymphocytes) in several models.
The forskolin content of Coleus root is typically 0.2% to 0.3%, therefore the forskolin content of crude Coleus products may not be sufficient to produce a pharmacological effect. It is best to use standardized extracts which have concentrated the forskolin content. The recommended dosage should be based upon the level of forskolin. Future studies will undoubtedly produce more precise dosage recommendations of a Coleus forskohlii. The current recommendation for Coleus forskohlii extract, standardized to contain 185 forskolin, is 50 mg (9 mg of forskolin) two to three times daily. The animal studies on forskolin indicate an extremely low order of toxicity for forskolin. Based on the pharmacology of forskolin, it may be wide to restrict the use of C. forskohlii preparations in cases of low blood pressure and peptic ulcers. Furthermore, C. forskohlii preparations should be used with caution in patients on presription medications especially anti-asthmatics and anti-hypertensives due to its ability to possibly potentiate the drug's effect.
The ancient medicinal plant Coleus forskohlii is the source of the compound forskolin which possesses unique biological activity. While clinical results are thought to be better obtained using the whole plant versus the isolated constituent forskolin, research on forskolin is upholding the traditional uses of the plant. Due to the unique pharmacology of forskolin, C. forskohlii may prove to be useful in a wide range of clinical conditions. Presently, it appears C. forskohlii is best suited for asthma, eczema, psoriasis, hypertension, congestive heart failure, and angina. It can be used alone, but it may prove to be most useful when combined with other botanicals and/or other measures in the treatment of these disorders.
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