PCr Animated

Animation of the interconversion of creatine and phosphocreatine.

Creatine Synthesis

Illustration showing how creatine is synthesized from 3 amino acids: Arginine, Glycine and Methionine.

Creatine Transport Mechanisms

Illustration showing how Creatine is transported into muscle cells from the blood stream.

(bringing it all together)

Legend: Creatine harnesses the potential energy of sodium (Na) wanting to enter the muscle cell. Therefore, any agent that increases the extrusion of sodium, should likewise increase the transport of creatine into the muscle cell. Physiological agensts that are well known to increase sodium efflux include insulin and adrenalin (epinephrine). Review Chapter 4 of my creatine guide for a more detailed discussion about the implications of this process to the athlete.

Two sodiums need to accompany each creatine molecule being transported inward. Therefore, doubling the driving force for sodium inwardly will effectively increase creatine transport by 50%.

Creatine transporter expression is also greatest on type II muscle fibers. Recall that these are the muscle fibers with the greatest requirement for creatine.

Finally, due to its electrical charge creatine becomes trapped within the muscle cell once transported within. PCr is even more highly charged and likewise is trapped once produced. Creatinine, on the other hand, lacks electrical charges at physiological pH and hence is able to escape across the muscle cell membrane. This is shown in greater detail here and establishes our daily creatine requirement.

Legend: Reaction 1 (catalyzed by AGAT) is the rate limiting step in creatine biosynthesis. AGAT expression is also reduced by the presence of creatine. This raised concerns that prolonged creatine supplementation might inhibit endogenous creatine synthesis for an indefinite period of time. See Chapter 16 of my creatine guide for greater discussion of the implications of this effect.

Finally, notice that Glycine is completely incorporated into the creatine backbone, whereas Arginine and Methionine only contribute side groups.

Legend: ATP (Adenosine TriPhosphate) is the energy storage molecule of all cells. After donating its energy allotment to the contractile apparatus of muscle, ATP becomes ADP (Adenosine DiPhosphate). During intense physical exertion ATP is rapidly recreated from ADP by the donation of a phosphate group from Phosphocreatine (PCr).

Creatine kinase is the enzyme responsible for swapping the phosphate groups (shown in red) between PCr and ATP. The upward reaction predominates during strenuous exercise when energy (ATP) is needed to fuel explosive movements. The downward reactions primarily takes place during moments of rest and recreates our PCr reserves. The larger our PCr reserves, the longer we can sustain intense muscular activity. This is the basic premise behind creatine supplementation.

Take a closer look at the reaction.

Creatine and PCr later spontaneously degrade into creatinine, which is able to escape from the cell.

The production of ATP from PCr has the added advantage that it also neutralizes muscle acidity (H+). This effect should heighten our fatigue threshold during moments of intense physical exertion.

Spontaneous one-way conversion of PCr and Creatine
into Creatinine

Legend: The presence of charged groups on creatine and PCr prevent them from transversing the muscle membrane. Creatinine, by contrast, has no charge and is thus able to freely slip through the muscle membrane escaping to the outside. This leakage pathway sets our requirement for new creatine (~2 grams per day, also see Chapter 4 of my creatine guide for greater explanation).

Also note that most of the muscle creatine is in the form of PCr, which also degrades at twice the rate of creatine. Hence, degradation rates should be quite appreciable under resting conditions.

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The most common health disorder inflicting older men is not hypertension, or arthritis, but Erectile Dysfunction; ED, for short. In the United States alone between 10-20 million males are affected with some form of severe erectile dysfunction. When including less severe degrees of erectile dysfunction this number swells to nearly 30 million!

Erectile dysfunction typically appears in males in their fifth decade of life. Estimates are that over half of all males between the ages of 50 and 70 exhibit some degree of erectile dysfunction. Surprisingly, the incidence of erectile dysfunction in males in their 40s is only around 5%, nearly ten-times less, demonstrating an alarmingly steep increase during middle age (45-65 years of age). Furthermore, environmental factors such as drug abuse, stress, anabolic steroids, poor diet and bad health, can accelerate the development of erectile dysfunction causing it to manifest at an earlier age. Sadly, despite the high incidence of erectile dysfunction in otherwise generally healthy males,less than 5% ever seek treatment.

Erectile dysfunction IS NOT an inevitable consequence of aging! Viable treatments do exist that will allow one to continue healthy sexual relations well into later life.

Penile Anatomy and Physiology

Images courtesy of Markis Rix Labs.

In essence, an erection results from blood flowing into two chambers on either side of the penis, the Corpora Cavernosa (see figure on right). This process is greatly facilitated by the fact the corpora cavernosi act as a single functioning unit due to the existence of an extensive system of interconnected blood vessels. This vascular arrangement is the reason why most treatments for erectile dysfunction are targeted at promoting penile blood flow.

Blood flow into each cavernosal chamber is regulated by a criss-crossing matrix of smooth muscle cells and cartilage filaments. When the smooth muscle cells contract (shorten), the corporal chambers collapse and blood flow into the penis is impeded; the penis becomes flaccid. On the other hand, when the smooth muscle cells relax, the cavernosal chambers open and the penis engorges with blood. Furthermore, as these chambers swell with blood (and intra-cavernosal pressure increases) they press against, the small veins that drain the penis, effectively closing them; hence, penile blood flow increases as drainage is impeded when the cavernosal smooth muscle matrix is relaxed. The net result of these events is penile rigidity, i.e. an ERECTION.

Therefore, contrary to popular myth, an erection results from muscle relaxation, not contraction!

Nervous System Control of Erection

Unfortunately, obtaining an erection is not an entirely voluntary act. It might not happen when you want it to and, conversely, may happen when you least expect it. It thus makes sense that the Involuntary, or Autonomic Nervous System, controls penile erection. The Autonomic Nervous System has two principal branches, the Parasympathetic and Sympathetic branches.

Parasympathetic Nervous System: Smooth muscle relaxation is achieved with an agent known as cyclic Guanosine MonoPhosphate, or cGMP, for short. cGMP is degraded by an enzyme known as cGMP Type V Phosphodiesterase, or PDE. This fact will become important a little later.

Activation of the Parasympathetic Nervous System innervating the penis produces cGMP and thus gives rise to an erection.

Sympathetic Nervous System: Sympathetic activation produces smooth muscle contraction which results in flaccidity (detumescence). Sympathetic Nervous System stimulation also causes ejaculation.

Factors that Contribute to Erectile Dysfunction

Erectile deficiency can arise from physiological, psychological or environmental factors. Although initially they can be divided into either psychogenic (of the mind) or organic (of the body) causes, they are not mutually exclusive. Below we outline the most relevant.

Psychogenic

Psychogenic: Erectile dysfunction of psychogenic origin is thought to make up 10-50% of all cases. Daily stress, divorce, death of spouse, loss of job can all contribute to the incidence of psychogenic erectile dysfunction. Often guilt, or anxiety, contribute to the development of psychogenic erectile dysfunction.

• Performance Anxiety: After an initial episode of erectile failure, further attempts at sexual contact may produce anxiety, which could further contribute to lack of response. This is referred to as Performance Anxiety.
• Widower’s Syndrome: Widower’s Syndrome refers to a male who experiences erectile dysfunction after the death of a spouse.

Organic

• Endocrinologic: Hormone levels strongly influence our sexual performance. A reduction in serum testosterone lowers our libido and makes it more difficult to maintain an erection. Interestingly, an elevation in serum prolactin also reduces serum testosterone and can have the same effect.
• Neurogenic: Damage to the Autonomic Nervous System may result in erectile dysfunction. Common causes are lower spinal cord injury and multiple sclerosis. Erectile dysfunction has been determined in 50-70% of men with multiple sclerosis.


• Vascular: Atherosclerosis and venous leaks of the penile blood vessels are the two most common forms of vascular erectile dysfunction. Vascular disease is estimated to cause 10-20% of all cases of erectile dysfunction. Importantly, elevated serum homocysteine levels is a leading cause of vascular disease in later life and has been recently been shown to be involved in the manifestation of certain forms of erectile dysfunction.
  Click here for more information about homocysteine and coronary heart and vascular disease.

  Importantly, the incidence of vascular erectile dysfunction increases to nearly 50% in men over 50 years of age.

• Drugs: Alcohol and tobacco abuse can also result in milder forms of erectile dysfunction; smoking causes vascular disease and alcohol abuse disturbs nervous conduction and lowers testosterone levels. Marijuana and cocaine use have also been implicated in causing erectile dysfunction.
• Diabetes: The prevalence of erectile dysfunction occurs earlier in diabetics. Erectile dysfunction is observed in ~30% of diabetics at age 30 and increases to nearly 55% at age 60. The cause is often vascular disturbances that are a secondary result of diabetes.

Erectile Dysfunction Treatments

Natural Treatments

• Yohimbe: Yohimbe is made from the inner bark of the Yohimbe tree from West Africa. Yohimbe increases the norepinephrine content of the corpus cavernosum which is essential for erections. Yohimbe stimulates chemical reactions in the body to help impotence. Yohimbe also boosts the adrenaline supply to nerve endings, which can quicken male sexual stimulation. Yohimbe expands the blood vessels in the genitals. Poor circulation can cause impotence. Yohimbe also inhibits serotonin. This is important because increased serotonin levels inhibit sexual performance. Yohimbe can help impotence so that men can experience fuller and longer lasting erections. Yohimbe is also responsible for psychic stimulation, heightening of sexual, emotional sensations and a useful substance for treating male sexual dysfunction.
• Epunedum Sagitum: Also known in China as Yin Yang Huo or in the Western World as Horny Goat Weed. Eastern doctors boosts that Yin Yang Huo enhances libido and improves erectile function. Yin Yang Huo works by liberating testosterone thereby increasing sex drive and endurance. Yin Yang Huo is a proven powerful natural aphrodisiac which will enhance physical and sexual sensations.
• Saw Palmetto: Saw Palmetto (Fructus Serenoae) is known to stimulate male libido and increase sexual energy. Components in saw palmetto are also believed to have aphrodisiac qualities, reduce prostate size, enhances sexual functioning, increase desire, reduce serum cholesterol and fatty acids.
• Catuaba Bark Extract: Catuaba has a long history in herbal medicine as an aphrodisiac. The Tupi Indians in Brazil first discovered the qualities of the plant and over the last centuries, have composed many songs praising it’s wonders. Indigenous people and local people have used Catuaba for generations and it is the most famous of all Brazilian aphrodisiaca plants. In the state of Minas there is a saying which goes, “Until a father reaches 60, the son is his, after that the son is Catuaba’s.” According to Dr. Meira Penna, Catuaba “functions as a stimulant of the nervous system, above all when one deals with functional impotence of the male genital organs… it is an innocent aphrodisiac, used without any ill effects at all.

Natural Ayurveda Treatments

• Ashwagandha (Withania Somnifera): Recommended in the ancient Kama Sutra for heightening sexual experience, Ashwagandha is easily the most potent aphrodisiac in the entire botanical kingdom. It has the ability to restore sexual drive, increase endurance and improve overall vitality while promoting a calm state of mind. Ashwagandha is an “adaptogenic” herb which nourishes nerves and improves nerve function to help your body adapt to stress, one of the common cause of sexual problems. Hormones (such as adrenaline) produced during difficult times cause arteries to constrict, keeping blood from the extremities and negatively impacting sexual performance. Ashwagandha brings the body back to equilibrium by relaxing it when stressed and energizing it when fatigued. It also strengthens the reproductive and respiratory systems while serving as a powerful Medhya Rasayana, which means that it enhances all aspects of mind power. Ashwagandha has been used for thousands of year to treat impotence, premature ejaculation, infertility, and erection disorders.
• Shatavari (Asparagus Racemosus): Shatavari is a rejuvenating herb that soothes the body to relieve stress, nurtures the reproductive system, and strengthens and nourishes tissues. It supports proper liver function and metabolic processes to remove toxins from the blood. This herb is also known to increase Sattwa, or positivity and healing power. It enhances the feelings of spiritual love and opens Ojas (”that through which consciousness enters the physiology”). When combined properly with Ashwagandha, Shatavari takes lovemaking capacity to new levels.
• Gokshura (Tribulus Terrestris): Gokshura is a sex and mood enhancer that stimulates the production of the Luteinizing Hormone (LH). When LH levels are elevated, the natural production of testosterone also increases. LH is a hormone that also increases sex drive and virility. Laboratory studies have found that Gokshura increases sperm count after being taken for 30 days and can result in better than 50% increase in testosterone levels. This herb also has a stimulating effect on the liver by helping to convert cholesterol and fats into hormones and energy. When this action is combined with the increase in testosterone levels which promote protein synthesis, positive nitrogen balance as well as faster recuperation and recovery from muscular stress, Gokshura has a tremendous positive impact on strength and stamina.
• Atmagupta (Mucuna Pruriens, or Velvet Bean): This rare herbal extract from India contains high levels of naturally occurring L-Dopa, the world’s most extensively researched amino acid. L-Dopa is one of the few substances that cross the blood brain barrier to convert into Dopamine. Dopamine is a very powerful neurotransmitter that stimulates the hypothalamus and pituitary glands to release growth hormone, increase testosterone levels, boost libido, and increase sperm count. Besides having a powerful impact on sex drive, Atmagupta enhances mental alertness, improves coordination, elevates energy levels, and promotes lean muscle growth.
• Vidari (Pueraria Tuberosa, or Indian Kudzu):The root of this plant has alterative, aphrodisiac, tonic, stimulant properties which are traditionally used to treat male infertility.

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Synthetic Treatments

• Sildenafil: Popularly known as Viagra. Sildenafil blocks the breakdown of cGMP by inhibiting the actions of PDE. Inhibition of PDE allows relaxation of the smooth muscle of the Corporal Cavernosa. This, in turn, increases blood flow into the cavernosal spaces, leading to erection. Viagra has been used with great success in the treatment for erectile dysfunction.
• Trazodone: Trazodone’s mechanism of action isn’t well understood. Trazodone might cause smooth muscle relaxation by interfering with the sympathetic control of penile flaccidity, or detumescence.
• Pentoxifylline: Pentoxifylline decreases red blood cell membrane rigidity making them more flexible, and allowing them to pass more readily through partially obstructed arteries. Use of pentoxifylline in erectile dysfunction is limited to patients with penile vascular disease.
• L-Arginine: L-Arginine is an amino acid precursor to nitric oxide with limited evidence to support its use in treating erectile dysfunction.

This attitude could have disastrous consequences!

There’s a smarter alternative….

Treating and Preventing Sports Injuries & Secondary Arthritis

Joint injuries are an unavoidable fact of life for most of us involved in sports. It doesn’t matter if you are a professional or recreational athlete, your joints are at risk all the time. The pounding and twisting our joints have to endure during normal everyday sporting activities can be absolutely devastating to the surrounding joint tissues.

When discussing “sport injuries” most of us think about the common broken bone or sprained ankle. There is, however, a more insidious kind of sport injury that can remain hidden for years before finally revealing the full extent of its damage. This kind of injury arises from the daily strain that exercise places on the joint and can lead to a lifetime of debilitating pain through the development degenerative joint disease, or arthritis.

When arthritis develops as a result of injuries, it is generally referred to as “secondary” osteoarthritis. This simply means that the deterioration of the cartilage was initially caused by a traumatic injury to the joint.

Each one of our 147 joints has cartilage protecting the bones from coming into contact with one another. It is this cartilage that takes the brunt of the pounding during heavy training. It is also the degradation of this cartilage that results in the development of arthritis.

So, what does all this have to do with athletes? Athletes have an increased risk of developing secondary osteoarthritis as a consequence of sports injury.

This is what years of heavy exercise does to your joints.
You have two options:
Don’t exercise or… Take care of your joints!

The wrong approach: Treating the Symptoms, but not the Disease!

Most of us continue doing sports or working out and endure the pain rather than taking positive steps to put an end to it. After all, it is very easy to take a quick trip to the drugstore and pick up an over-the-counter painkiller. Quite frankly, this is the wrong approach; a short term “solution” to a long term problem!

Since pain goes hand in hand with being athletic, the most common approach is to take aspirin, Tylenol, Ibuprofen or one of that family of “drugs” (called nonsteroidal anti-imflammatory drugs or NSAIDs, for short) and let it go at that. What we may not realize is that the relief offered by these drugs comes at a very high price. Over time, they all have dangerous and possibly even life threatening consequences.

The smart approach: Preventing Joint Deterioration.

The wisest approach is to attack joint disease at its origin, the way the body would. Glucosamine been shown in recent clinical studies to rebuild damaged joints and diminish pain. In fact, higher quality forms of glucosamine can halt your pain in just a matter of days.

With the release of scientific studies demonstrating the effectiveness of glucosamine in treating joint disease the market was literally flooded with competing products. So how do you choose the glucosamine formula that is right for you?

As a general rule, the lower the grade of the product the less pain relief it offers. Using medium grade products, it will take 5-6 months for you to experience relief. On the other hand, a high-quality product will usually end your pain in 10-25 days, depending on the extent of your disease. When choosing among glucosamine products a pharmaceutical grade liquid formula will bring the maximum relief and protection. In addition, a high quality liquid glucosamine formula will do wonders for those recovering from orthopedic surgery.

The smart athlete is already taking a glucosamine formula as a preventive measure. Given its low cost and availability without a prescription, it’s a smart move both for the short term and the long one. After all, there is no sense in paying the physical price for doing the things we enjoy doing. Learn about other natural joint remedies .

Sore Joints?
Check out this video describing a natural treatment for sore joints that can spare you years of pain later on in life.

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First, look for a fast acting liquid Glucosamine and Chondroitin formula. Glucosamine and Chondroitin are important building blocks for the cartilage and proteins that protect and lubricate our joints.This is the least one needs to do.

Omega-3 and Omega-6 fatty acids: Also known as Eicosapentaenoic Acid and Docasahexaenoic Acid (DHA), respectively. These fatty acids are essential for reducing the inflammation and pain of injured joints.

Incidentally, omega fatty acids are also good for overall health. Omega-3 fatty acids reduce the risks of heart disease, cancer, autoimmune disorders and depression. Smart athletes should already be supplementing their diets with Omega Fatty Acids.

Vitamins A, C & E: These antioxidant vitamins prevent free radical damage resulting from intense exercise. In addition, Vitamin A (Beta Carotene) is essential for the growth and repair of bone and joint tissues. Vitamin C (Ascorbic Acid) mobilizes your body’s immune system to combat disease. Vitamin E (Tocopheral) is most famous as an antioxidant that protects cell membranes from oxidative damage as result from exercise.

Boswellin: Boswellin has been used for centuries in the Indian Ayurvedic system of medicine to maintain healthy joints. Boswellic acids improve blood supply to the joints and maintain the integrity of blood vessels. Boswellin also serves to reduce swelling and improve mobility where individuals experience stiffness in the joints.

Bromeliane: Bromelaine reduces pain and swelling by inhibiting pro-inflammatory compounds. Unlike aspirin, bromelaine does not inhibit the production of prostaglandins which can have undesirable side effects.

Yucca: Yucca has a lengthy history in the treatment of arthritis and rheumatism. The root is rich in sponins that elevate your body’s ability to produce “natural” cortisone. Yucca also helps to block the release of toxins from the intestines that inhibit the normal function of cartilage. Yucca also has anti-inflammatory properties.

Scientific Reference

Authors: Jean Yves Reginster, Rita Deroisy, Lucio C Rovati, Richard L. Lee, Eric Lejeune, Olivier Bruyere, Giampaolo Giacovelli, Yves Henrotin, Jane E. Dacre, Christiane Gossett

Title: Long-term effects of glucosamine sulphate on osteoarthritis progression: a randomised, placebo-controlled clinical trial.

Journal: Lancet (2001), Volume 357 (9252): pages 251-256.

Interpretation: Glucosamine stops joint deterioration.

Two recent studies examined the ability of Ginkgo biloba (EGb761) to attenuate indicators of stress, namely elevated blood pressure and serum cortisol levels.

Cortisol is the nemesis of any athlete undergoing strenuous training. Cortisol is catabolic, meaning that it literally causes the body to breakdown its own tissues for conversion into immediate energy (ATP) during moments of stress. The so-called fight-or-flight response. Unfortunately, the body mignt interpret excessive exercise as a stressful situation, which will recruit the actions of cortisol and potentially undermine muscle anabolism (tissue building). This hormonal imbalance is the physiological basis of OverTraining Syndrome, or OTS. In essence, training too heavily, eating inadequately, and resting insufficiently, shifts the balance from total body anabolism to catabolism-defeating the purpose of training in the first place.

Cortisol is a steroid hormone secreted by the adrenal glands located on top of the kidneys. The adrenal glands are provoked to release cortisol by another hormone known as adrenocorticotropic hormone (ACTH) that is released from the pituitary gland at the base of the brain. Again, cortisol counteracts the ability of our anabolic hormones, namely growth hormone, testosterone and insulin, to produce muscle growth.

Visit our page concerning the anabolic effects of growth hormone.

Scientific study #1: EGb 761 suppresses cortisol release in response to stressors

The first study (Ref. 1) used a combination of two stressors on which to study the effect of EGb 761, static exercise (handgrip: 3 minutes at 30% of maximum voluntary contraction) and mental load (memory test: memorize the ordering of 25 words in three minutes). Cortisol, blood pressure and heart rate measurements were taken before the administration of EGb 761 to establish a baseline value. Subjects were then given a single dose of EGB 761 and 30 minutes later stressed in the manner described above. Heart rate and blood pressure were taken during the handgrip trial, while salivary cortisol levels were measured one hour later.

A college pharmacology course served as a backdrop for the study from which the participants for the study were selected. The study was placebo controlled and conducted in a double-blind manner, meaning that neither investigator, nor experimental subject, knew who was taking placebo or EGb 761. That is, it was unknown who was taking the ginkgo extract, or who was taking placebo, until after the results of the study were fully analyzed.

The administration of ginkgo biloba had litttle effect over the resting levels of cortisol observed throughout the day, agreeing well with the second study being discussed. Ginkgo did, however, reduce the release of cortisol following stress, but with special considerations (see below).

Diurnal Cortisol Rhythm

Serum cortisol levels obey a circadian rhythm; they are highest in the morning and recede throughout the remainder of the day until almost totally disappearing around midnight.

In males, the stress-evoked release of cortisol was abolished with the administration of a single dose of EGb 761, but only in the afternoon when the ability of stress to increase serum cortisol levels over baseline is most apparent. Due to the large drop in serum cortisol levels in the early morning hours, however, the ability of exercise to increase serum cortisol levels was largely hidden by the declining wave and hence, precluded any apparent effect of EGb 761. That is, baseline and stress measurements were made one hour apart, which was much too slow to discern a change in serum cortisol in response to exercise, or ginkgo, treatment.

Interestingly, women did not exhibit a stress-provoked rise in serum cortisol at any point in the day and accordingly, ginkgo biloba had no effect over serum cortisol levels in women.

Heart rate and blood pressure consistently increased in response to the combined stressors. EGb 761 reduced blood pressure during the handgrip trial in all cases, males and females, at all times of the day, but without altering heart rate.

Therefore, at least in males, Ginkgo biloba appears to reduce the release of cortisol and rise in blood pressure following a combination of physical and mental stresses. These results therefore suggest that ginkgo supplementation might represent a possible way to circumvent the release of cortisol following prolonged exercise and possibly help circumvent the development of Overtraining Syndrome.

Scientific study #2: EGb 761 does not decrease resting cortisol levels

Earlier animal studies have suggested that Ginkgo biloba, or more specifically, one of ginkgo’s components may inhibit the synthesis of the glucocorticoid hormones. This would be good news with reference to cortisol, but may have negative repercusions as far as the steroid sex hormones are concerned, especially testosterone and progesterone.

To paraphrase, the second study (Ref. 2) found that Ginkgo biloba produced a small, yet statistically insignificant, drop in serum cortisol levels after administration of EGb 716 for fourteen days. Other products of steroid hormone synthesis (17a-hydroxyprogesterone, bound testosterone, free testosterone, free androgen index, androstenedione, dihydrotestosterone, sex hormone-binding globulins, etc) were similarly unchanged by ginko administration. With respect to the little change in resting steroid hormone production following ginkgo administration, this study agreed well with the findings of the first study. It thus appears that ginkgo biloba does not alter the resting production of the steroid hormones humans.

Comparison of the two studies

Here is a list of the principal differences between the two studies examining the effects of EGb 761 over serum cortisol levels.

• Dose: 120 milligrams (Ref.1) versus 240 milligrams (Ref. 2) per day; 120 milligrams is the typical dose recommended in the medical literature.
• Duration: Single dose (Ref.1) versus 14 day trial (Ref 2.).
• Sample Size: Seventy subjects (Ref.1; 33 males and 37 females) versus eleven subjects (Ref.2; 6 males and 5 females) participated in the study. The larger sample size was a major advantage of the first study (Ref.1). Too many studies are restricted to small sample sizes, making it more difficult to interpret the statistical significance of the generated data.
• Assay: Salivary sample (Ref.1) versus blood test (Ref.2).
• Product: European manufacturered extract EGb 761 elixir (Ref.1) versus American produced tablets of EGb 761 (Ref.2).
• Study Design: Stress-induced (Ref.1) versus resting cortisol levels (Ref.2).

Both studies utilized relatively young subjects of between 20 and 40 years of age. I would like to see similar studies conducted on older group subjects given that this demographic is where Ginkgo biloba is currently showing the most promise.

What is Ginkgo biloba?

The ginkgo (biloba) is a member of an ancient family of trees, very possibly the oldest living tree species on earth. The first fossil records of ginkgos date back to over 270 million years ago. In evolutionary terms, the ginkgo is more closely related to pine trees (gymnosperms), than to flowering trees (angiosperms), a fact that makes evolutionary sense, given that gymnosperms are phylogenetically much older than angiosperms. The reason that the ginkgo has thus far escaped extinction up to now is its high resistant to disease, pest and environmental insult, a genetic resilience that is also reflected in its potential to live to over 4,000 years.

Also known as the Maidenhair tree, ginkgos were once indigenous to many parts of the world. Today, however, the ginkgo only grows naturally in China. Nevertheless, due to its ability to survive harsh environments, man has once again transplanted the ginkgo to cover many parts of the globe. In fact, the ginkgo is one of the few trees that can survive ‘big city’ environments and hence, is often found lining the streets in some of the world’s busiest metropolitan areas. However, despite the fact that the fruit and the leaves of the Ginkgo have been used in traditional Chinese medicine for over six centuries, its re-appearance in the North American continent only took place a little over two centuries ago.

The ginkgo’s species name, biloba, is derived from the fact that its leaves possess two lobes (see image). Scientific nomenclature is generally straightforward.

Uses of Ginkgo biloba

Extracts of dried ginkgo leaves are among the best selling herbal medications in Europe, especially in France and Germany where it ranks among the top five of all prescriptions written. Achieving nearly a 300 million dollar a year industry at the commencement of the 21st century, ginkgo sales will continue to increase in the upcoming years as research reveals more about its healthful properties. Let there be no doubt, the increasing use of ginkgo for medical purposes stems from its success in the clinical arena.

Ginkgo biloba derivatives are currently being used to remedy asthma, coughs, age-related macular degeneration (reduced vision in the elderly) and bladder inflammation. Ginkgo also improves peripheral and cerebral circulation and, in this capacity, has been shown to be effective in mitigating cases of erectile dysfunction, intermittent claudication (pain caused by inadequate blood flow to the legs) and cerebral insufficiency (reduced blood flow to the brain in the elderly causing symptoms of cognitive decline). In fact, one of the more promising uses of ginkgo is as a neuroprotectant and cognitive enhancer; ginkgo is proving to be an effective anti-Alzheimer’s treatment (see below). Finally, ginkgo also reduces signs of stress, both mentally and physically (see Stress Inhibition).

Components of a standardized extract of Ginkgo biloba: EGb 761

One particularly well-defined extraction, EGb 761 (Extract Ginkgo biloba 761), is recently providing very promising results in scientific studies.

EGb 761 consists of 24% ginkgo-flavonol glycosides and 6% ginkgo terpenoid lactones, which can be further subdivided into the following classes of ingredients:

Ginkgo-flavonol glycosides: A mixture of biflavoness and flavonol glycosides that are found in their highest concentrations in the leaves of the Ginkgo.

Ginkgo terpenoids: Trilactones consisting of a mixture of ginkgolides and bilobalides. Ginkgolides are further separated into several subfractions A, B, C, J and M, with distinct pharmacological activities. These components only constitute about 0.1% of dry Ginkgo biloba leaves and are much more prevalent in the tree itself.

IMPORTANT: When purchasing ginkgo products look for this percentage composition of ginkgo-flavonol glycosides and ginkgo terpenoid lactones.

Unwanted contaminants: Ginkgolic acid should constitute less than 10 ppm (parts per million) to a final extraction, since it might cause skin irritation.

Biological activities of the components of Ginkgo biloba

Extracts of Ginkgo biloba have been found to increase circulation, enhance mood, accentuate cognitive capacity and improve memory. These effects are more often, than not, the result of the combined actions of the individual components of Ginkgo biloba working in concert, the so-called polyvalent effects (see below). Next is a description of the biological activities that each separate fraction of Ginkgo biloba (EGb 761) has at the cellular level.

Ginkgo-flavonol glycosides: Flavonoids (such as quercetin, kaempferol and isorhamnetin) are potent antioxidants. Acting as such, ginkgo’s falvonoids scavenger and neutralize free radicals that might cause the breakdown of integral cell membranes via a deleterious process of lipid peroxidation as well as damage DNA, leading to mutations of the cell’s genetic information. The ginkgo flavonoids thus extend cell survival under conditions (oxidative and free radical stress) that might otherwise lead to cell death or the development of cancer.

In particular, a specific flavonoid fraction of EGb 761 (CP 205) has been recently shown to prevent the death of neurons in an area of the brain known as the hippocampus in response to NO (nitrix oxide) over production (see reference below). As the hippocampus is the part of the brain that consolidates and stores memories, any damage to this part of the brain will severly interfere with normal cognitive capacity.

By acting as free radical scavengers the flavonoids also relax blood vessels by preventing a rise in intracellular calcium concentration that would otherwise cause vascular smooth muscle contraction (vasoconstirction).

Ginkgo terpenoids: Ginkgolides improve blood flow by reducing the stickiness of platelets, supporting cellular energy metabolism and by acting as antioxidants.

• Ginkgolides: These agents are highly selective antagonists of platelet aggregation mediated by platelet-activating factor (PAF) receptor. PAF, synthesized locally, mediate pain perception, blood coagulation, and smooth muscle contraction. When overexpressed, PAF contributes to various inflammatory, cardiovascular, and respiratory disorders.Ginkgolide B is most active of the ginkgolides in this capacity, followed by ginkgolides A, C, M in order of reducing potency.
• Bilobalide: Bilobalide is a sesquiterpene. Recent evidence indicates that bilobalide improves cellular energy metabolism, especially in response to cerebral ischemia, or greatly reduced blood flow. Specifically, bilobalide allows mitochondria to maintain respiratory activity when oxygen levels drop precipitously and by doing so maintains cellular energy (ATP) content from dropping dangerously.Bilobalide derivatives are currently used for treating neuropathy, edema, encephalopathy, spinal cord disease and senile dementia. There is also convincing evidence supporting an antioxidant role for bilobalide.

Bilobalide might also prove useful as an anticonvulsant. Over excitation by neurotransmitters, namely glutamate, can give rise to seizures.

Polyvalent effects: Ginkgo’s broad systemic effects are the consequence of interactions between the individual biological activities (increased circulation, antioxidant effects and metabolic effects) of its separate components (flavonoids, ginkgolides and bilobalide). Such multifaceted actions of ginkgo are most evident in the area of dementia and the decline in mental capacity observed with aging. This needs to be contrasted with synthetic medications that instead target a single cellular pathyway and are more limited in scope. For instance, ginkgo biloba is demonstrating to be effective in retarding the development of Alzheimer’s disease.

Interestingly, a significant proportion of patients suffering from dementia and depression exhibit elevated cortisol levels (see Stress Inhibition). Stress kills brain cells…

Precautions and counterindications of mixing Ginkgo biloba with certain prescribed medications

Ginkgo is widely considered safe and side effects are rare. In a few cases, gastrointestinal upset, headaches, skin reactions, sleeeplessness and dizziness have been reported.

• Because Ginkgo biloba decreases clot formation (platelet aggregation) there is some concern that it may increase the risk of intracranial (brain) hemorrhage. Therefore, until more is known, one should not mix ginkgo with other blood-thinning medications, including aspirin.
• Ginkgo biloba should not be taken within 36 hours of surgery to the possibility of bleeding complications.
• Ginkgo biloba should not be taken in combination with anticonvulsant medication.

This website provides other possible counterindications of Ginkgo biloba use.

Continue reading about Ginkgo Biloba and Stress Inhibition…