Hormones - Testosterone

Testosterone
Testosterone is a sex hormone produced under the influence of Adrenocorticotropic Hormone (ACTH). Testosterone is linked to high levels of curiosity and aggression. Sex hormones are manufactured from cholesterol which is converted to Pregnenolone by the ACTH. High levels of ACTH therefore stimulate greater manufacture of testosterone from cholesterol. Testosterone is indeed produced in large quantities in the testes, and androgens (the parent hormones that give rise to testosterone) are actually produced by two small glands next to the kidneys, the adrenals, in both men and women.

Testosterone is an anabolic hormone that will increase protein synthesis in both men and women however adult males produce significantly more than females. The adult male body manufactures 2.5 - 11 mg per day while females only produce 0.25 mg.

Stimulating testosterone production in order to promote muscle growth is not an easy task as a series of chemical changes are undergone within the body beginning with the conversion of cholesterol into pregnenolone under the influence of ACTH.

CHOLESTEROL

ACTH INFLUENCE

PREGNENOLONE - In common with DHEA, estrogen and testosterone, pregnenolone is synthesised from cholesterol. Seen as the 'mother' hormone, this important steroid is prescribed for many illness or symptom for which cortisone is prescribed. These include asthma, arthritis, depression, fatigue, SLE (Lupus) and many others. Although not so speedy in its effect or so powerful as cortisone, it does not produce the side effects that are characteristic of cortisone therapy. These can include high blood pressure, fluid retention, weight increase, immune breakdown and blood vessel brittleness, loss of bone mass and a tendancy to diabetes. Pregnenolone was initially researched in the 1940s as a treatment for arthritis. However, as a natural substance ot could not be patented, and cortisone (prednisolone) soon replaced it as the treatment of choice.

PROGESTERONE CORTICOSTEROIDS

Progesterone and estrogen are mainly produced in ovaries. Small amounts are also released from the adrenal glands. The role of the two hormones is key to understandings of a womans menstrual cycle. Estrogen dominates the intial two weeks and progesterone is the dominant hormone for the final two weeks of the month. Low progesterone in women is often misdiagnosed as a thyroid deficiancy. And it is progesterone that is responsible for the female sex drive, not estrogen.

The thyroid hormones and progesterone compliment each other. Conversly a thyroid deficiency can stimulate a large estrogen production. Large estrogen dominance further lowers available progesterone. Significantly the body can convert progesterone into estrogen. So for women estrogen supplementation is now very much questioned. Especially since such good natural and safe phytoestrogens are available through the environment and food. These phytoestrogens are chiefly found in soya products. This is a very good reason for the male to avoid soya products completely.

LH INFLUENCE

ANDROSTENEDINE TESTOSTERONE

ESTRONE ESTRADIL

Progesterone molecules undergo hydroxylation by which side chains are cleaved leaving behind essential hormones called corticosteroids. Corticosteroids are responsible for the catabolism (the breakdown as apposed the build up) of body proteins and fats. Under the influence of luteinizing hormone corticosteroids yield testosterone, an androgen, responsible for protein synthesis and muscle growth.

A number of factors influence the levels of testosterone produced by the body. Boron is an essential mineral for testosterone production but it is not a causal factor, alone it would have little effect, it is simply one of many links in a synergystic chain. Vitamin C is a vital stimulus to testosterone production. When levels of ascorbic acid are high the adrenal gland's response to ACTH is inhibited and consequently greater amounts of pregnenolone are available for conversion to testosterone.

Free testosterone molecules in the bloodstream binds with skeletal muscle cells at specific hormone receptor sites forming what is known as a 'receptor complex'. The complex (made up of the hormone molecule and the receptor site) travels into the cells nucleus and attaches to specific sections of the cells DNA strand. Once attached, the complex activates the transcription of specific genes and the process of protein synthesis begins. The testosterone molecule simply carries the code to activate protein synthesis in the cell's nucleus, once it has delivered this code it is released back into the cell's cytosol where it can interact with other cells in the same way.

Testosterone produces characteristics in the body, brain and behaviour that we might call 'male typical'. At the purely physical level, these would include a low degree of facial fat,a more pronounced jaw and prominant cheekbones, a deep voice, large hands and greater upper-body strength. At the psychological level we find a heightened curiosity and sex drive, aggression and competitive behaviour.

Alongside its role in protein synthesis, high androgen levels promote the production of Creatine Phosphate (CP), a vital component in the manufacture of Adenosine Triphosphate (ATP) which is the primary source of energy for muscle cells. During the contraction of the muscle tissue ATP molecules are broken down into ADP (Adenosine Diphosphate) which results in the the release of an energy molecule. CP is used to restore ADP to its original state enabling a constant flow of energy. During intense exercise this process is cannot keep up with the rate at which energy is being used; essentially, the ATP molecules cannot be restored fast enough to supply the body with sufficient energy and the muscles will become fatigued. High levels of CP are therefore vital to maintain energy in muscle tissue.

Testosterone Supplementation - A Fine Line?

So we know that testosterone is key in building bigger and stronger muscles. We know we can boost Testosterone levels naturally through nutrition and training, but what about all of the ambiguous supplement, almost drug like compounds, still available to athletes (for the time being at least)?

While adding new muscle mass may require a cocktail of several endogenous hormones, there can be no doubt that when it comes to the acquisition of superhuman strength and enviable virility, then testosterone is the undoubtable king! In fact, you would be hard pushed to find any individual who couldn’t benefit from an extra helping of testosterone, -and that includes female athletes too, when it comes to competitive results. This is not to endorse the use of illegal testosterone manipulation of course.

In the U.S., the FDA have now staked their claim on your right to enhance your anabolic count. From March of this year, they have launched a crackdown on any company that manufactures, markets or distributes products containing androstenedione, taking the view that the first and most infamous of prohormones is in fact a performance-enhancing drug. No longer is Andro a sports dietary supplement as it has been for some time, but it is now a categorised and legitimate drug. Many companies may be breathing a huge sigh of relief that it was this antiquated forerunner that was targeted (as androstenedione has been far outdated with better testosterone boosters these days), but their joy may indeed, be short lived.

It is unfortunate that the FDA have taken the line that, as a new dietary ingredient, androstenedione should have had pre-market safety notification, -something that has never been submitted. Applying this rule, it would seem that the writing must surely be on the wall for the whole continually evolving array of second generation esterified “super-prohormones”, e.g. 4-AD-EC. Does this mean that the end is nigh for testosterone manipulation through sports supplements?

Some feel that such a crackdown isn’t such a bad thing. The prohormones have brought nothing but adverse publicity to sports nutrition; the Mark McGwire story and a host of nandrolone positives have fuelled draconian legislation that will limit the rights of the world’s supplement consumers for ever more. The ethics surrounding the use of prohormones as a supplement is a whole issue in itself; even the term “prohormone” may be a misnomer. Whatever the view, with many companies having literally built their empires on prohormones over the last few years, the race to find a natural testosterone booster that actually delivers has never been more frantic. The Green Solution: Phytochemistry. Phytochemistry is essentially the science of chemistry involving natural plant extracts, as apposed to chemical man made synthetics. Most supplement foundations are natural because of this fact, that they are founded on natural substances, not chemical synthetics. This is the difference between, say, Tribullus Terrestris and Clomiphene Citrate. One is a natural Testosterone booster, one is chemcial.

Almost every culture has its own traditional product for this objective (natural testosterone elevation); from ayurvedic to Chinese medicine, from rainforest shaman to African witch doctor, they all have a special elixir guaranteed to bring about higher levels of the anabolic hormone that seems to fuel the sex drive. But the aphrodisiac property of an indigenous herb (muira puama, catuaba, etc) may have nothing to do with testosterone, this could well be accounted for by an influence on serotonin or dopamine. It’s also quite possible that these herbs could contain constituents that actually have a negative impact on testosterone or fertility; many herbs are known to have this effect. Conversely, some herbs that have known fertility enhancing properties have no impact on testosterone; Maca is an example here. So, although we know testosterone itself can positively impact libido, it does not follow suit that certain natural libido enhancing herbs also enhance testosterone, although you can see where the logical conclusions first came from.

Progress and Standardization

The wealth of scientific expertise now employed within the herbal industry has been highly instrumental in its recent progression, particularly in the application of high technological analytical methodology to the process of standardization. Where once the standard simply meant the ratio of raw material to the finished extract (e.g. a 10:1 extract), today it refers to a percentage of one or more phytochemical “fingerprints” derived from the original raw material. This is a very important distinction. For example, a typical Ephedra Sinica extract may be classed as an 8% extract, meaning that it should contain around 8% ephedrine alkaloids. This is what people really need to know - exactly how much active compound there is in the product.

Breakthroughs in extraction technology, coupled with reliable analytical methodology, now mean that scientists are able to verify the properties of a particular herb, identify the active component responsible and produce a finished extract with a consistent quantity of that component from batch to batch. Standardization is now everything, but only if the correct form of analytical methodology has been used. It is also vital that the plant is standardized for the right component, as many herbs have numerous medicinal uses with different components responsible for each. So people need to do their homework and a little research before blindly following mass advertising hype. Remember, advertising has one goal in mind, to exchange your money for a product. The money being the appropriate portion of the bargain. Marketing is not research or even information, it is pretty pictures and text telling you what you want to hear.

Plant Extracts Boost Testosterone

The take home message here is that if you’re not using a pharmaceutical grade standardized extract, then you’re probably using inactive junk. The exciting fact about these “fingerprint” components, be they saponins, alkaloids, tannins, phenols, flavonoids or whatever, is that their properties are often attributable to the ability to impact various biological systems in the human body. Several of these compounds have an established ability to exert hormone-like effects. For our objective, the system we need to influence is the endocrine system, or to be more specific, the HPT (hypothalamus-pituitary-testicular) axis. There are several ways in which this can be achieved, including:

1. Direct stimulation of the Leydig cells in the testes.
2. Stimulation of the pituitary to produce more LH.
3. Reduction of estradiol levels, either through competitive receptor binding (anti-estrogens) or decreased production of the aromatase enzyme.
4. Competitive binding of sex hormone-binding globulin (SHBG) to produce more biologically active (“free”) testosterone.
5. Increase production of the enzymes responsible for the biosynthesis of testosterone.

Various indirect approaches could involve influencing the production of other hormones capable of impacting Testosterone levels. For example, reducing prolactin can increase testosterone, as can stimulating oxytocin or noradrenaline. The good news is that there are numerous herbs out there for which one or even several of the above properties have been identified. Turning to the relevant scientific research, studies using human subjects are given priority of course (as rats have a very different physiology to us humans making those studies nearly irrelevant), with those using multiple species being next, -there can be large differences in the results between different species. Of course, using a little logical thought, this is obvious. Do you have a long tail, fluffy black hair covering your entire body and stand tall at less than a foot in height. No, then don't expect the same results on your body as in rat trials.

The toxicological aspect also needs to be taken into account, as many companies will run with a particular product after getting only half the story. Mate’ (Ilex paraguariensis) is a good example here, often employed in thermogenic formulas, numerous studies have documented a high incidence of cancer (mainly digestive tract) amongst its regular users.

LH Stimulation Boosting Testosterone

The Contenders for Stimulation of Leydig cell steroidogenesis occurs mainly through a cAMP mediated mechanism, which includes adenylate cyclase activation.

Forskolin, isolated from the plant Coleus forskholii, is a popular ingredient in cutting-edge thermogenic formulas and has a well-established ability to stimulate adenylate cyclase and increase cyclic AMP. These abilities mean that forskolin is commonly used in scientific studies for the purpose of testosterone stimulation. Recently, a compound isolated from sage (Salvia sclarea), known as FSC, has demonstrated a similar activity profile to that of forskolin, but with greater potency. FSC also aids in restoring the level of monoamines for presynaptic availability, giving this compound antidepressant properties. Several plant species are believed to have constituents that may stimulate LH release. One of these is Avena sativa, used for centuries in disability and as a nerve tonic. Japanese scientists have actually identified a substance in this plant that has potent LH-releasing activity, although it is structurally different from LH-RH present in the hypothalamus. Interestingly, garlic has also been shown to increase testosterone by enhancing LH production. The allyl-containing sulfides in garlic are known to stimulate the pituitary gland by increasing the concentration of noradrenaline. The anti-stress properties of garlic, which include reducing stress hormones, may also be partly responsible for this effect.

Plant Extracts As Anti-Estrogens

Unfortunately, most plant constituents indicated to have anti-estrogenic properties have yet to get past the “in vitro” stage, while the few that have show poor oral bioavailability. What this means, is eseentially, that although we have discovered some reasonably good anti-estrogens, they cannot be taken as tablets, pills or powders very effectively as of this time. The main classes of these phytoestrogens are isoflavanoids, phytoalexins and coumestans. One phytoalexin in particular, Resveratrol (3,5,4’-trihydroxystilbene), found in red wine and grapes, has demonstrated a powerful ability to impart the protective effects of estrogen on bone loss and cardiovascular disease in vivo. This means that the estrogen antagonism that it has demonstrated in vitro could possible be replicated after oral administration. Diindolyl methane, a dietary indole isolated from cruciferous vegetables, may be able to promote dramatic and beneficial changes in estrogen metabolism through various mechanisms. Backed by several in vivo studies (rats), it has demonstrated competitive receptor binding and the ability to affect estrogen synthesis and its conversion to weaker metabolites. The real heavyweight contender amongst this section may well be calcium D-glucarate, a compound found in numerous fruits and vegetables. In studies, supplementation with this has been shown to affect estrogen by increasing levels of D-Glucaro-lactone, thereby increasing the metabolism and excretion of estadiol.

Testosterone Boosting Through Decreased Prolactin

As was mentioned earlier, another way to potentially elevate testosterone is by decreasing prolactin. Specialized extracts of the herb Vitex agnus castus have effectively demonstrated this ability in vivo, a group of components called agnusides have been identified as the active principles. Herbs that may also exert a positive effect on Testosterone levels are those with established anti-stress properties. Of these, Rhodiola rosea and Morinda officinalis show real promise, as both of these have demonstrated an ability to support/increase testosterone under stressed conditions. Epimedium, commonly used for the same purpose, has yet to get off the ground, as it hasn’t been shown to have any impact on testosterone and may actually elevate cortisol. Phytoestrogens are no substitute for Clomid (a chemical anti-estrogen, LH stimulating compound, popular amongst drug taking athletes), nor will Avena sativa replace HCG (another chemical used to stimulate the testes into producing more testosterone). But then a few cups of chamomile tea won’t sort you out the morning after a serious alcohol binge either. These products were never intended to be damage control during periods of reckless steroid abuse, but they do have research-backed properties which, though subtle, may pay big dividends if used in combination by drug-free athletes or during steroid/prohormone-free periods.

Tribulus Terrestris - The King of Testosterone Boosters

Although Tribulus terrestris has had enjoyed a reputation as a major player in the testosterone stakes for quite some time now, it has never really achieved its full potential. There’s a good reason for this and it’s to do with cutting corners for profit while entirely missing the mark, by some unscrupulous supplement companies looking to cash in quick on a growing trend! As it has been stated earlier the standardization of correct active ingredient/compound and the dosage are very important in the results that you achieve. The original Tribulus product, to which most of the research relates, was claimed to be standardized for 45% protodioscine, -a furastanol saponin indicated to be the active. This of course turned out to be completely wrong, and much time was subsequently wasted by a few conscientious companies trying to match this figure. Several Chinese raw material suppliers even produced material that had been spiked with Dioscorea (yam) extract, -a medicinal plant known to have a higher protodioscine content than Tribulus. Ironically, on analysing the original Bulgarian product, Japanese scientists found the yield of total saponins (not just protodioscine) to be around just 4%! However, when one particular company noted that neither Dioscorea nor any of the other herbs that have a high protodioscine yield exhibit the same pro-testosterone/fertility-enhancing properties of Tribulus, the exact role of protodioscine was brought into question. The big breakthrough came when a large German biochemical company that specialized in phytochemical extraction techniques developed a commercial interest in Tribulus, particularly in the medical application of the anti-tumour activity of protodioscine. They drafted in ChromaDex (Santa Ana, Ca), the market leader in the development of botanical reference standards, to put together standards for all the major components in Tribulus. A custom extract was produced that not only yielded a consistent protodioscine content of around 12%, but also high percentages of other (previously undetermined) saponins, including pseudoprotodioscine, prototribestin (tribulosaponin A) and tribulosaponin B. The co-existence of these saponins would prove to be exclusive to both this pharmaceutical grade extract and the original Bulgarian material. This would tend to indicate that either protodioscine works synergistically with the other saponins or that it may not be the true active ingredient. Further research indicated that the active principle(s) seem to work at the level of the hypothalamus, -strongly stimulating the pituitary to release more LH. Additionally, increases in free testosterone also point to an interaction with SHBG. The bottom line here is that this kind of Tribulus extract will deliver and all other material compares to it in the same way that a weak cup of coffee compares to 200 mgs of ephedrine hydrochloride! For those of you who have experienced this first hand, know exactly what we are saying here. Nothing compares. Its not even the same world, let alone, the same league.

Further Enhancements

Still few of you will have heard of Tongkat Ali, -a traditional Malaysian aphrodisiac prepared from the herb Eurycoma longifolia. It is interesting to note that this obscure Asian plant looks to be the most exciting and effective breakthrough in the quest for optimal testosterone enhancement! The herb is also known as Pasak Bumi in Indonesia; in Vietnam, it’s called Cay Ba Bihn, meaning “plant that cures 101 diseases”. However, although it may have many uses in various Asian cultures, the common denominator amongst them all is the revere shown for this herb as a bestower of superhuman virility. Around three years ago, certain research has been leaked from the East Asian medical world where this herb was being considered as a potential treatment for infertility and impotence. Since then, certain companies have been working with Eurycoma non-stop and can tell you that there’s nothing else out there that even comes close to this herb as a serious Testosterone booster. It’s sturdy and solid reputation is heavily backed up by numerous unrelated, unbiased scientific studies, -both in vitro and in vivo, in multiple animal species and in humans. These studies include: ·

Effects on energy production systems.
Sexual behaviour and mating studies.
Hormone studies.
Studies on anabolic properties.
IVF studies
Sperm characteristic studies
Toxicity studies.

So, what exactly have these studies shown? Many things is the honest answer, take a look at its established impact on the testosterone levels of animals:

Animal % increased
Mice 479%
Rat 380%
Rabbit 320%

As if this isn’t impressive enough, in human testicular tissue the same extract yielded a 440% increase! Taking a look at what this translates to in the real world, human infertility studies have also revealed a suitably impressive testosterone response. So far, its potent pro-testosterone properties have been attributed to three different mechanisms, they are:

1. Increased substrate enzymes for the biosynthesis of testosterone.
2. Increased cAMP.
3. Decreased SHBG.

In another in vivo study, this time using trained subjects, specific anabolic properties were identified. But to fully exploit Eurycoma’s awesome potential, you need to first overcome an inherent problem. Basically, the presence of bitter components, known as quassinoids, have given Eurycoma its other scientifically proven activities (e.g. anti-malarial, anti-tumour and anti-inflammatory), but these are known to be toxic. However, the same big pharmaceutical company from the previously-mentioned Tribulus project, have been called upon to eliminate this problem with the correct extraction process, thereby developing a pharmaceutical grade extract. They have recently labelled and standardized every major component in Eurycoma, as well as confirming its activity; it’s now set to achieve its full potential without any risk attached.