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06.01.2009


New steroid Triolex boosts immune system

The American HollisEden Pharmaceuticals is doing human tests on a new steroid that is distantly related to DHEA. Scientists at the San Diego based research company recently published an article in Autoimmunity Reviews. The researchers think that their new steroid, Triolex, does what DHEA should have done to the immune system: inhibit inflammatory reactions. Triolex may be a medicine that helps rheumatism and MS, and it may also be an effective anti-ageing drug. After all, when it comes down to it, ageing is a cascade of inflammatory reactions.

New steroid Triolex boosts immune system
HollisEden is the company behind Neumune. Neumune is the same as 5-AD, a DHEA metabolite that used to be sold as a prohormone. The American army did tests with 5-AD in the hopes of finding a medicine that would protect Americans in case of a nuclear attack. This was part of the Bioshield project.

When Bush outlawed a number of steroid hormones in designer supplements in 2004, 5-AD was taken off the market. The supplements industry was not to be put off however, and that's why the current designer supplements contain a series of 5-AD analogues with a hydroxyl or carbonyl group on the seventh carbon atom. These are mainly found in products that stimulate fat burning, according to the manufacturers' claims.

One of these steroid compounds is remarkably similar to Triolex: mBAET. But enough about designer supplements; back to the article in Autoimmunity Reviews.

The researchers write that DHEA has a positive effect on the immune system of mice: it inhibits diseases in which the body's own immune cells turn against it. These are diseases like rheumatism, colitis and MS. However, researchers have not been able to demonstrate the same effects convincingly in humans. This is probably because mice, unlike humans, convert DHEA into 5-AD, the active ingredient in Neumune. HollisEden prefers to use the abbreviation AED, from the chemical name 5-androstene-3beta, 17beta-diol.


New steroid Triolex boosts immune system


Of course, you could give humans AED, but you need very heavy doses. So heavy that the conversion of AED into male and female sex hormones becomes a problem. You can avoid this by choosing 5-AD analogues with a hydroxyl or carbonyl group on the seventh carbon atom. As, ehem, the supplements industry already did about eight years ago. These 7-substituted analogues cannot be converted into active androgens or estrogens.

The most effective compound that the researchers found at first was bAET, which is also an ingredient in supplements. The disadvantage, however, was that you needed huge amounts. In animal tests the HollisEden researchers injected doses of 120 mg per kg bodyweight per day.

That didn't get anyone anywhere.

The most obvious solution is to add a methyl group to the molecule. And ehem, designer supplements manufacturers came up with this idea a few years ago already as well. To do this, in good supplement industry tradition, they ripped off an existing patent. A company like HollisEden can't afford to do this. That's why HollisEden decided to add not a methyl but an ethynyl group to the seventeenth carbon atom in bAET.

And thus: Triolex was born. Scientific name: 17-alpha-ethynyl-5-androstene-3beta, 7-beta, 17-beta-triol. In cells, Triolex probably doesn't react with a steroid receptor, but it does react with an as-yet unknown receptor on the cell membrane. As a result, the cell probably produces more of the inflammation inhibitor eicosanoid 15d-PGJ2, the researchers think. If Triolex does indeed do this, it could turn out to be a pretty interesting anti-ageing drug.

A hundred people were given Triolex in phase I and II trials. No side-effects were observed.

Sources:
Autoimmunity Reviews doi:10.1016/j.autrev.2008.11.011.