Health and Fitness in a Bottle: Big Pharma Discovers their Holy Grail

Scientists from the Salk Institute’s Gene Expression Laboratory may have discovered Big Pharma’s Holy Grail of Pharmaceuticals.

A pill that would allow you to reap all of the benefits of vigorous exercise while sitting on the couch watching re-runs of Seinfeld.

How about that!

Scientists from the Salk Institute’s Gene Expression Laboratory have reported (in the July 31 advance edition of the journal Cell) that they have discovered two drugs (GW1516 and AICAR) that were able to transform regular ole’ lab mice into freaky running machines.

AICAR increased the mice’s endurance on a treadmill by 44 percent after just four weeks of treatment.

GW1516 produced a 77% increase in endurance, but sadly, had to be combined with exercise to have any effect.

The Study

Lead researcher, Ronald M. Evans, Ph.D, had previously discovered that by permanently activating a genetic switch known as PPAR delta, he could turn lab mice into miniature Olympic marathon champs.

In addition to their improvements in aerobic endurance, these super mice didn’t gain weight while being fed a diet high in pizza and beer. In addition to their ripped physiques, they experienced improved insulin sensitivity and lowered levels of blood sugar.

This led Dr. Evans to hypothesize whether a drug specific for PPAR delta would have the same beneficial effects.

So, they doped the mice with GW1516.
After four weeks, the researchers were in for a bit of a disappointment.

The mice were leaner, had an improved fatty acid profile, improved insulin sensitivity and lowered levels of blood sugar, but there was no effect on their exercise performance.

So, like a personal trainer, they upped the mice’s cardio and had them run up to 50 minutes on a treadmill.

And after a few more weeks, the GW1516 mice were lapping the non-doped mice.

In fact, the GW1516 mice improved their exercise endurance 77% higher than the control mice. They also saw a 38% increase in slow twitch muscle fibers.

But wait, the researchers weren’t finished yet. GW1516 looks pretty great, but they were looking for a drug that would provide the benefits of exercise without actually having to do the exercise.

Enter AICAR.

The researchers fed untrained mice AICAR, (a synthetic AMP analog that directly activates AMPK).

After four weeks, the AICAR mice were pushed onto the treadmill and boy did they perform. On average, they ran 44% longer than the control mice. According to the researchers, “That’s as much improvement as we get with regular exercise.”

So there we go, exercise in a pill.

So, How Does it Work?

Well, according to Dr. Evans, “GW1516 activates the PPAR-delta protein, but the mice must also exercise to show increased endurance. It seems that PPAR-delta switches on one set of genes, and exercise another, and both are needed for endurance”.

AICAR however, “activates the PPAR-delta protein and mimics the effects of exercise, thus switching on both sets of genes needed for the endurance signal”. It “signals the cell that it has burned off energy and needs to generate more. It is pretty much pharmacological exercise”.
Conclusion

Theirs: “This is not just a free lunch,” Dr. Evans said. “It’s pushing your genome toward a more enhanced genetic tone that impacts metabolism and muscle function. So instead of inheriting a great set-point you are using a drug to move your own genetics to a more activated metabolic state.”

“The drugs’ effect on muscle opens a window to a world of medical problems,” he said. “This paper will alert the medical community that muscle can be a therapeutic target.”

Mine: I wonder if we are not straying a leeetle bit too far down the Eugenics path with this research.

Forgetting the potential moral argument of switching our genes on and off, my concern is purely medical. While it will take years and years of animal and human testing before a commercially viable GW1516 or AICAR is available on the market, I still think that I would prefer to improve my body the old fashioned way.

Thanks to EurekAlert! for the original source material.

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