Last month, I promised you I would continue my discussion of joint care products and tell you about a few more really cool compounds. However, I changed my mind; I figure that I have to keep some secrets to myself. You see, I have a tendency to be too forthcoming with information, quite often to my detriment. Sorry, sorry. I know you might be disappointed right now, but I can’t give away everything—  I have to keep some of my aces in the hole.

I will discuss one product— or group of products— which I believe can have remarkable benefit for degenerative joint disorders as well as many other things. I am not talking about something completely novel here, and many of you may be familiar with this stuff. However, no one that I know has ever contemplated these compounds having utility in the treatment and/or prevention of connective tissue problems.

Last month, I promised you I would continue my discussion of joint care products and tell you about a few more really cool compounds. However, I changed my mind; I figure that I have to keep some secrets to myself. You see, I have a tendency to be too forthcoming with information, quite often to my detriment. Sorry, sorry. I know you might be disappointed right now, but I can’t give away everything—  I have to keep some of my aces in the hole.

I will discuss one product— or group of products— which I believe can have remarkable benefit for degenerative joint disorders as well as many other things. I am not talking about something completely novel here, and many of you may be familiar with this stuff. However, no one that I know has ever contemplated these compounds having utility in the treatment and/or prevention of connective tissue problems.

What Are 7-oxygenated DHEA Metabolites?

The compounds I am talking about are the 7-oxygenated DHEA metabolites. You may have heard of 7-keto DHEA. That, along with androst-5-ene-3b,7b,17b-triol (beta-androstenetriol, or beta-AET), constitutes the two major compounds of interest. Also included are androst-5-ene-3b,7a,17b-triol, androst-5-ene-3b,7b-diol-17-one and androst-5-ene-3b,7a-diol-17-one.

The granddaddy of all the aforementioned steroid hormones is DHEA. As you probably know, DHEA is produced in the adrenal gland and secreted into the bloodstream. It is the largest circulating steroid hormone in the body and it serves several known (and perhaps some as yet unknown) functions. It acts as a precursor to androgens and estrogens and also imparts non-genomic influences upon certain neurological systems in the brain (such as antagonizing GABA-a receptors). But perhaps its most important— and most interesting— function is as the parent prohormone to the amazing class of steroids known as the 7-oxygenated DHEA metabolites.

7-oxygenated DHEA metabolites are renowned for their unique immunostimulatory, anti-obesity, anti-diabetic, anti-inflammatory, and anti-catabolic properties. Many of these benefits are related to the fact that these metabolites antagonize the actions of glucocorticoids (aka cortisol) on many systems in the body. However, there are also modes of action beyond that, such as the stimulation of thermogenic enzymes in the liver.

These properties have only recently been observed and described by scientists, and for decades these compounds were thought merely to be inactive androgenic metabolites. Recently, however, the potential for these metabolites in the treatment of conditions such as radiation sickness, Metabolic Syndrome (also known ‘as syndrome X’), autoimmune disorders (such as lupus and rheumatoid arthritis), and cancer have resulted in many of these compounds— as well as some synthetic analogs— being developed as actual pharmaceuticals.

Of course, this magazine is about bodybuilding and not general medicine per se, so we should examine more closely how the special powers of 7-oxygenated DHEA metabolites can be harnessed and exploited for our own selfish, narcissistic benefit. Seriously though, what is so great about these compounds is that they can do wonderful things for your physique and your performance, while at the same time providing a myriad of additional health benefits.

Benefits of 7-oxygenated DHEA Metabolites

The number one most valuable property of this stuff is its ability to help you get lean. How that works, no one is exactly 100 percent sure. At least two things contribute to this— the ability to stimulate thermogenesis in the liver, and the ability to suppress the activity of cortisol.

The hepatic (liver) thermogenesis activity is due to stimulation in the activity of the liver malic enzyme and glycerol-3-phosphatase. Stimulation of these enzymes leads to a disruption in the cycling of energy in liver cell mitochondria. This metabolic inefficiency results in excess energy being thrown off as heat, and the resulting increased energy demand is fueled by fatty acids. This is pretty much the way thyroid hormone works in the liver. But unlike thyroid hormone, these metabolites do not have the potential for cardiac toxicity, skeletal muscle catabolism, or thyroid gland suppression.

The anti-glucocorticoid role of 7-oxygenated DHEA metabolites as it pertains to fat loss is much more difficult to pinpoint. One aspect involves suppression of the 11beta-hydroxysteroid dehydrogenase type I enzyme responsible for the conversion of circulating cortisone into active cortisol at target tissues. Another aspect probably involves a modulation of the immune response to cortisol in various sites in the body— especially the visceral area and the liver. The etiology of the Metabolic Syndrome is now known to be intimately related to immunoregulatory dysfunction.  Elevated cortisol likely plays a key role in this dysfunction and 7-oxygenated DHEA metabolites may prevent and/or reverse this phenomenon.

Corticosteroid shots are often used when connective tissue injuries produce chronic and debilitating inflammation and discomfort. While often quite effective, they do nothing to help healing and in fact can lead to further degeneration. Corticosteroids work in large part by suppressing the production of pro-inflammatory eicosanoids and cytokines. These substances are secreted by injured cells as well as immune system cells called leukocytes, which are often present at the site of injury. The problem with corticosteroids is that they pretty much shut down all the eicosanoids and cytokines produced by these immune system cells, including the ones necessary for growth and recovery.

7-oxygenated DHEA metabolites, on the other hand, suppress inflammation in a much more finely-tuned and desirable way. While overactive immune system activity at the site of injury is often a culprit behind chronic injury that won’t go away, you don’t have to— nor do you want to— shut down this activity completely to achieve relief and recovery. The way 7-oxygenated DHEA metabolites achieve their goal is thought to be by increasing the activity of a certain group of leukocytes called T-regulatory cells. T-regulatory cells act to keep other immune system cells in check, so that they behave normally and don’t become overactive and destructive. By doing so, the proper balance between destructive immune overactivity and undesirable immune underactivity is struck, and inflammation is controlled while keeping recovery at a healthy pace.

Practical Application

There are many other benefits of 7-oxygenated DHEA metabolites. The increase in immune system competence, for example, can help prevent you from catching a cold or flu. I am not going to delve into these other areas, because they are not directly related to the realm of this magazine, which is bodybuilding.

As far as practical usage of 7-oxygenated DHEA metabolites go, the two compounds currently available on the supplement market are 7-keto DHEA and beta-AET. The former converts into the latter, and vice versa. Both are potent compounds, but beta-AET seems to be the more active of the two. 7-keto DHEA is sold as the 3-acetate, and this form is much more soluble than the free alcohol— and therefore, probably more absorbable. Beta-AET, on the other hand, is sold as the free alcohol. My experience has shown that the 3-acetate is vastly superior in solubility.

Both of these can be taken orally, but their bioavailabilities are very low that way. Of course, injection of these compounds would provide 100 percent bioavailability, but obviously that method is impractical. One method that I have found works to provide good bioavailability is the transdermal route. I formulated a topical liquid that contains 50 percent 7-keto DHEA 3-acetate and 50 percent beta-AET 3-acetate, and the results have been very impressive. The effects I have observed are greater fat loss, improved energy, resistance to illness, and reduction of inflammation. I believe there are a few transdermal 7-keto DHEA formulas currently on the market, but none that I know of also contain beta-AET or beta-AET 3-acetate. I wouldn’t be surprised that after this issue of MD comes out, someone starts to sell one.

That’s it for this month. See you next month.