Competitive bodybuilders’especially male bodybuilders’consider excess estrogen a problem. Among its effects in men is gynecomastia, which is the development of excessive glandular tissue in breasts’make that pecs. It may be responsible for water retention and increased fat deposits under the skin, which obscure muscular definition, especially in the lower body, according to some bodybuilders.
Hardcore female bodybuilding competitors also consider estrogen a problem. Women have a harder time producing extreme muscular definition in their legs for two reasons. One is that female fat cells in the lower body are marked by a preponderance of alpha-adrenergic receptors. Unlike beta-adrenergic receptors, alpha receptors resist the signals that call for fat mobilization. Some speculate that it has to do with human evolution, since successful pregnancy requires a certain number of calories, and nature locks them into a woman’s lower body.
The second reason women experience problems in reducing lower-body fat and producing a highly defined appearance is their naturally higher estrogen levels. Estrogen works with the alpha-adrenergic receptors to make fat cells slow to release fat. It promotes processes that result in increased fat deposits in the female body, particularly the thighs, hips and buttocks.
Elevated estrogen levels aren’t natural in male bodybuilders; however, estrogen could rise naturally through the activity of aromatase, a ubiquitous enzyme that converts androgens, such as testosterone, into estrogen. One-third of women’s entire estrogen production stems from the action of aromatase on adrenal and ovarian androgens. Aromatase is particularly active in peripheral fat stores, such as the ones in the legs. So a man carrying excess fat in his legs would likely produce higher levels of estrogen than a leaner man.
But estrogen levels don’t usually get high enough to cause distinct estrogen-related problems, such as gyno. For that to occur, they have to be comparable to or higher than what an average woman generates. In reality, that happens either under pathological conditions or through the use of anabolic steroid drugs, such as testosterone injections, that aromatize. Other drugs can also cause gyno, including growth hormone when used by older men.
While excess estrogen used to be a significant problem for drug-using athletes, the advent of anti-estrogen drugs has considerably blunted the problem. Since gynecomastia is still evident on some bodybuilders, they either aren’t taking pharmacological steps to inhibit estrogen production or are using drugs such as human chorionic gonadotropin, a.k.a. HCG, which increases both testosterone and estrogen production.
Some drugs, such as Nolvadex, keep estrogen from binding to its cellular receptors. While effective, Nolvadex brings problems of its own. Structurally similar to estrogen, which likely explains why it can bind to estrogen receptors, it can induce paradoxical estrogenic effects if taken too long or in too high a dose. In addition, Nolvadex inhibits two enzymes that the testes require for the synthesis of testosterone.
The current drugs of choice take a more direct approach by stopping the source of excess estrogen itself’the aromatase enzyme. They’re sold under various trade names, such as Arimidex, Aromasin and Farestan. They all short-circuit the activity of aromatase, and they’re all expensive. They were designed to treat breast cancer in older women whose cancers don’t respond to the older drugs, such as Nolvadex.
Some natural anti-estrogens exist. Soy, like Nolvadex, is molecularly similar to estrogen and can interfere with its actions. High intakes of soy are thought to explain the lower incidence of estrogen-related cancers that occur in Asian than in Western women. Soy, however, presents problems for men; above a certain level it acts like an estrogen in them.
Other natural substances inhibit aromatase. An example is green tea, but the activity is weak, not comparable to the anti-aromatase drugs by any standard. Brown kelp, however, is another matter.1 ALL Kelp was a popular supplement among bodybuilders around the time Arnold was king of the posing platform. The idea was that it helped increase muscular definition by stimulating the thyroid gland. Kelp, or seaweed, is rich in the trace mineral iodine, which makes up two-thirds of thyroid hormone. What bodybuilders at the time didn’t realize was that kelp was also loaded with sodium, a mineral known for its water-retaining property.
As for thyroid stimulation, a deficiency of iodine can impair thyroid activity, but too much can do the same thing. Since kelp was thought to be a natural, innocuous substance, it wasn’t unusual for bodybuilders to pop as many as 30 to 50 tablets a day, which may have had the paradoxical effect of inhibiting thyroid hormone synthesis.
Where estrogen is concerned, kelp has promise. In fact, some scientists now think that it wasn’t the soy that prevented all those cancers in Asian women; it may have been their high kelp intake.
A recent study examined the effects of kelp in both rats and isolated human cells derived from female ovaries. Giving rats kelp led to an 18 to 33 percent reduction in circulating levels of 17-beta estradiol, the most potent form of estrogen. The amount of kelp they got was comparable to the daily human intake in Asian populations. In the human cells, kelp resulted in a 23 to 35 percent reduction in active estrogen. The experimenters think that kelp may either directly inhibit estrogen production or enhance its rapid metabolic breakdown. Kelp showed no effects on aromatase.
The researchers also found that kelp binds to estrogen cell receptors much in the manner of Nolvadex. The question that remains is what in kelp is responsible for what looks like anti-estrogen activity.
Several constituents of kelp are candidates: bioactive polyphenols, which have potent antioxidant activity; sulfated polysaccharides, a combination of sulfur and sugar; and substances called fucosterols. As a practical matter, depending on kelp to neutralize the effects of drug-related high estrogen levels would be foolish. From a health perspective, however, the effects are worth a look.
The Arginine-Testosterone Connection
Although it’s considered a conditionally essential amino acid, arginine has always been a popular supplement among bodybuilders and other athletes. That’s because it was considered a potent promoter of growth hormone release, a notion based on provocative use of arginine to cause release of GH from the pituitary gland in the brain. The problem was that the effect required average arginine infusions of 30 grams, a level that, taken orally, usually led to nausea and vomiting. Taking too much at one time also activated arginase, a liver enzyme that rapidly degraded it.
Recently, forms of arginine have enjoyed a resurgence as active constituents of nitric oxide food supplements. Nitric oxide is a natural body chemical’a free radical, in fact. It has many functions in the body, its most familiar being to dilate blood vessels. The rapid widening of blood vessels induced by nitric oxide fosters an exorbitant muscle pump, and as the Governator noted in the film ‘Pumping Iron,’ the pump is where it’s at in bodybuilding.
Arginine is the direct precursor of nitric oxide synthesis in the body. No arginine, no nitric oxide. It’s also involved in other important body functions. It’s required for synthesis of growth-promoting compounds called polyamines and is the primary amino acid precursor of creatine synthesis in the body.
Perhaps its least known property is its effect on testosterone. A recent study using rats as subjects focused on the not so apparent metabolic partnership between arginine and testosterone.2 A key finding was that testosterone was required for the production of enzymes that regulate kidney function. When arginine was omitted from the rats’ diets, the anabolic activity of testosterone in their bodies significantly declined. The effect was noted in the animals’ kidneys and muscles.
The authors aren’t sure of the precise connection between arginine and testosterone, but they think it’s related to the protein-binding property of insulinlike growth factor 1. They observed that when arginine is deficient in the body, IGF-1 production is blunted in the kidneys and liver. Previous studies have showed that testosterone and IGF-1 have an anabolic partnership in muscle, and this study’s authors suggest that supplementing with arginine may improve the anabolic results of testosterone. If the rat-based findings hold true for human subjects, it could cast a whole new light on arginine. Another Designer Steroid Emerges
The World Anti-Doping Agency recently announced the seizure of a mysterious-looking vial from a car traveling from Montana across the Canadian border. While the incident occurred in December 2003, the results of an analysis of the vial’s contents were just announced. Ostensibly, WADA held back the information until the drug could be identified and a drug test instituted.
The vial contained a designer steroid, so designated because it had never appeared on the commercial market and was likely conjured by a renegade chemist somewhere. But WADA officials also said that unlike THG, the notorious designer steroid from the Balco drug scandal, the new drug is more sophisticated.
It was called desoxy-methyl-testosterone, or DMT. According to the Canadian lab that identified and developed a test for the drug, it hasn’t yet found its way into professional sports, perhaps because it contains markers that would show up in a normal anabolic drug screen. Which makes you wonder just how sophisticated the drug actually is.
The drug bust was the result of an ‘anonymous tipster,’ according to WADA, as was the discovery of THG. The fact that DMT hasn’t yet reached any market and contains elements that would arouse suspicion during a plain-wrap drug test makes you wonder about the legitimacy of the bust. The entire episode may in fact be a ruse, intended to warn renegade chemists and dastardly purveyors of designer steroids that the intrepid WADA enforcement apparatus is on the job. IM
1 Skibola, C., et al. (2005). Brown kelp modulates endocrine hormones in female Sprague-Dawley rats and in human luteinized granulosa cells. J Nutr. 135:296-300.
2 Cremades, A., et al. (2004). Influence of dietary arginine on the anabolic effects of androgens. J Endocrino. 183:343-351. IM