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Artificially Speaking, How Sweet It Isn’t

7302-eat9Many people are concerned about the widespread use of artificial sweeteners, including aspartame and sucralose, and the possibility that they may cause serious health problems, ranging from brain tumors to various neurological issues, like chronic headaches. Even so, the majority of studies that have carefully examined the alleged side effects of commercial sweeteners have not confirmed the anecdotal reports of health problems. Yet many people remain convinced that artificial sweeteners pose a risk to long-term health.

If you look at what some of the most popular sweeteners are made of, it’s difficult to understand how they could be toxic, unless they were used in massive amounts. In animal studies any toxicity symptoms appeared only after the animals were given quantities of sweeteners that far exceeded what any rational person would be able to use.

Aspartame is composed of two amino acids, aspartic acid and phenylalanine, both of which occur in every protein food and drink available. Critics argue that the problem is a third ingredient, methanol, commonly known as “wood alcohol.” Methanol is indeed toxic but not in the quantities found in aspartame. There is considerably more methanol naturally occurring in a glass of fruit juice than in the recommended maximum dose of aspartame.

Despite evidence to the contrary, many bodybuilders refuse to use any type of artificial sweetener. That seems ironic when you consider how many of them wouldn’t think twice about using anabolic drugs that do pose definite health threats but balk at putting aspartame in their coffee. Because of the ludicrous articles published on the Internet that “document” the dangers of aspartame and other artificial sweeteners, more-natural sweeteners are now in vogue.

Perhaps the most popular natural-alternative sweetener is stevia, a member of the sunflower family. More than 240 species of Stevia are known to exist. The type used for sweetening purposes is Stevia rebaudiana. In high doses it produces an aftertaste that some describe as being similar to licorice, which may be significant.

Stevia is 300 times sweeter than sugar and has been used in Japan since 1970. Its sweetening power is derived from two glycosides, meaning that they contains glucose. Several health attributes have been associated with stevia, including lower blood pressure and a rejuvenating effect on the beta cells of the pancreas, which produce insulin. That suggests that stevia, unlike sugar, may provide an antidiabetic effect.

Studies have shown that stevia does not promote cancer. After years of use in various countries around the world, it has an excellent safety record, which of course makes it attractive to those who want to avoid artificial sweeteners.

According to a newly published case study, however, stevia may have a previously unrecognized property that may make it even worse than the reviled artificial sweeteners.1 The case involved a 32-year-old woman who had suffered from symptoms of generalized edema for more than six months, including a swelling of her feet, hands and face. She also displayed early signs of high blood pressure, along with low blood potassium. Lab tests revealed low levels of aldosterone, an adrenal steroid hormone linked to sodium retention, and renin, a kidney hormone that adjusts blood pressure. She did show an increase in the ratio of cortisol to its inactive metabolite, cortisone.

It turns out that the woman had been liberally using stevia for nine months before she turned up at the hospital. She did not have any risk factors that would account for her elevated cortisol—for example, she didn’t eat licorice, which is known to produce an aldosterone-like effect, causing high blood pressure and low blood potassium—nor did she use chewing tobacco, which also contains compounds that can boost cortisol. The examining doctors suspected that her intake of stevia might be the root of the problem, so they asked her to stop using it.

Within two weeks her edema symptoms completely subsided. To prove that it was indeed the stevia that caused her symptoms, the doctors requested that she take another dose of stevia, an action that the woman vehemently refused. So the question is, What is it about stevia that would cause the woman’s symptoms, which appeared to be linked to her elevated cortisol?

It has to do with an enzyme called 11 beta-hydroxysteroid dehydrogenase type-2, or 11B2. It’s found in tissues that express mineralocorticoid receptors, such as the kidneys, colon and salivary glands, and it works by converting cortisol into the inactive cortisone. The other form of the enzyme, type 1, works in reverse; it converts inactive cortisone into active cortisol. Anything that interferes with the actions of 11B2 can lead to elevated cortisol in the body, along with various related symptoms, such as edema, loss of potassium and high blood pressure. Licorice can inhibit 11B2, which explains the side effects that can occur when someone eats excessive amounts of black licorice.

When the woman in the study used those generous amounts of stevia, it blocked the 112B, leading to her symptoms. What’s curious is that most studies have found that stevia appears to lower blood pressure, which wouldn’t happen if the enzyme was blocked. So why did it happen to this woman?

It could be that she had a genetic predisposition to problems with the enzyme that were activated by her stevia intake. It could also relate to the large amounts that she used. Smaller amounts might not have been sufficient to produce symptoms or affect the enzyme. It could  have been the length of time over which she used the stevia in large quantities, more than nine months. She might have been drinking a lot of water and taking in a lot of sodium in her diet, which would have made her symptoms apparent. Similar to what happens with other substances, it seems that only the dose determines the poison. Since this particular side effect of stevia hasn’t shown up previously, despite more than four decades of use worldwide, I suspect that she did have a genetic susceptibility.

Water Retention and Bodybuilding

One of the common side effects of using large doses of anabolic steroids is a form of edema, more popularly known as “water retention.” It’s often attributed to sodium and water retention in the body caused by the high-dose steroid use. The effect subsides when the user gets off all steroids. Interestingly, anabolic drugs not often linked to water retention, such as growth hormone, may be even more potent in that regard than are steroids because growth hormone triggers the release of aldosterone, which, as noted, causes potassium excretion and sodium retention, along with water retention.

Many of the possible adverse cardiovascular effects of steroids are related to that water retention, including high blood pressure and damage to arteries that could result in atherosclerosis. What is it about steroids that causes the edema?

One of the known effects of steroids is that they compete with cortisol for binding to mineralocorticoid cell receptors. In short, steroids block the effects of cortisol in the body. In fact, that is considered a primary anabolic effect of steroids, since cortisol is the body’s primary catabolic hormone, linked to excessive muscle loss. Some scientists even speculate that the muscle-protein-synthesis effect produced by steroids is short-lived, and that any anabolic effects that occur with extended steroid use are likely due to cortisol inhibition.

On the other hand, you still see those common signs of water retention in high-dose steroid users. How can that be if steroids oppose cortisol actions in cells? For some it could be the result of excess estrogen, produced as a result of aromatization, which is the conversion of androgens into estrogen by way of the enzyme aromatase. Since most steroid users also use other drugs that block excess estrogen activity, the probability of that being the case is low. There are, however, other hormones that can produce estrogenlike side effects, including DHT, a metabolite of testosterone linked to various side effects, including acne and hair loss, and as noted, growth hormone can also produce a significant amount of water retention.

All that said, the most probable cause of edema in bodybuilders on high-dose-steroid regimens is a blocking of the enzyme 11B2. Several steroids are known to do that, including Anadrol (trade name for oxymetholone), Oranabol (oxymesterone) and testosterone, but they all have a rather weak effect on the enzyme, which is the reason that everyone who uses them suffers the bloat effect. A recent report, however, found that one particular steroid, Halotestin (fluoxymesterone), is a potent blocker of 11B2, meaning that it significantly boosts cortisol in the body by preventing the 11B2 from inactivating it.2

Halotestin was briefly popular among pro bodybuilders in the ’70s. It had the reputation of producing a harder-looking physique, and since it wasn’t subject to conversion to estrogen, it avoided the problems related to high estrogen levels. It was, however, subject to conversion to DHT. The drug was not very anabolic but was highly androgenic, likely because of its tendency to be converted into DHT. That produced a lot of aggression, which aided intense training but also triggered adverse personality changes. Still, the main reason that it fell out of favor was that it proved highly toxic to liver function.

Halotestin is structurally similar to cortisol, which may explain its effect in blocking the type 2 enzyme, but if it produces a lot of cortisol in the body, how did it get the reputation of being a “hardening drug”? While it may have blocked cortisol cell receptors in muscle, thereby exerting an anticatabolic action conducive to building muscle, in the kidneys it has a reverse effect of activating mineralocorticoid receptors, producing aldosterone-like effects, such as high blood pressure, potassium excretion and sodium retention. That also increases the risk of cardiovascular disease, since mineralocorticoid receptors are also activated in the heart, opening the door to the development of atherosclerosis.

Small wonder that Halotestin rarely, if ever, shows up in current athletic anabolic drug stacks. While no anabolic steroid is completely safe, some are far worse than others, and Halotestin is at the top of that list. Interestingly, President John F. Kennedy used Halotestin as part of his daily drug regimen. He used it to offset the cortisol drugs that he had to take because of his Addison’s disease, in which the body doesn’t produce enough cortisol.

Editor’s note: Jerry Brainum has been an exercise and nutrition researcher and journalist for more than 25 years. He’s worked with pro bodybuilders as well as many Olympic and professional athletes. To get his new e-book, Natural Anabolics—Nutrients, Compounds and Supplements That Can Accelerate Muscle Growth Without Drugs, visit   IM


1 Esmail, S., et al. (2012). Edema, enigma: 11-B-hydroxysteroid dehydrogenase type-2 inhibition by sweetener “stevia.” Open J Endocrine Metab Dis. 2:49-52.

2 Furstenberger, C., et al. (2012). The anabolic-androgenic steroid fluoxymesterone inhibits 11-B-hydroxysteroid dehydrogenase-2 dependent glucocorticoid inactivation. Toxicol Sci. 126:353-61.

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