Exercise in Pill Form May Answer Prayers of Many
Most of us would have a hard time trying to discern the links between world-class athletes, veterans suffering from physical disabilities, couch potatoes, and the frail, the elderly, and the obese but researchers at the Salk Institute for Biological Studies would tell us they’re all likely candidates for a new drug they’ve been investigating that mimics the healthful effects of exercise. Tested only on laboratory mice, the mice getting the drug dramatically increased endurance during exercise, did not gain weight on a high-fat diet, and their body’s response to insulin improved as well.
This exercise-in-a-pill is not available commercially but the potential it poses for athletes participating in endurance-type sports, such as long-distance running, is so strong that the research team is working with the World Anti-Doping Association to develop a test that detects the drug in the blood and urine. They hope to have the test ready before the Summer Olympics games begin next week.
Adenosine Triphosphate (ATP) is the main form of energy stored in the muscle. During times of high physical demand ATP gets converted to a new chemical, Adenosine Monophosphate (AMP). AMP alerts AMPK, which works like a master regulator for the metabolism. AMP signals a genetic switch, PPAR delta, to increase endurance levels.
A drug used for investigational purposes only, GW1516, acts like a direct switch to the PPAR delta, causing it to switch to endurance performance even when no exercise or physical exertion is in progress. The Salk research team wanted to know if the exercise-induced health benefits would be produced by the GW1516 alone.
When lab mice were treated with GW1516 for four weeks, invisible benefits were documented. Blood glucose and fatty acids levels dropped but there was no visible evidence of improved physical performance although the mice were not required to exercise at this stage of the study.
Switching tactics, however, the research team subjected the mice to 50 minutes a day on a treadmill plus the GW1516. The dramatic result of the exercise/drug combo increased endurance by as much as 77% over mice who underwent the same exercise program without the added drug. A specific type of muscle tissue, called “slow twitch” and “non-fatiguing,” increased, too, by about 38%.
Further research revealed that the exercise/drug combo worked best because the exercise causes the cytoplasm, which surrounds the nucleus of the cell, to release AMPK molecules, some of which enter the nucleus, where the PPAR delta is found. Once activated by the AMPK molecules, the PPAR delta becomes turbo-charged in the presence of GW1516, which explains how the mice were able to exercise 44% longer than mice not treated with the drug and not trained for exercising.
The story of the exercise in a pill is in the July 31 online advance edition of the medical journal, Cell. The Howard Hughes Medical Institute, the National Institute of Health, and the Hillblom Foundation all provided support for the study.
Source: Salk Institute for Biological Studies
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