BODYBUILDING PHARMACOLOGY

Kelp: Anti-Estrogen Help?

Jerry Brainum

Page 1

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


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