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Exercise pills: pills that simulate exercise ?

The benefits of physical exercise are widely known, with several metabolic and physiological benefits, as well as enabling the treatment of various metabolic diseases. However, the practice of physical activity is not something frequent in much of the world population, making it an environment more conducive to sedentary lifestyle.

The development of exercise science and the understanding of the molecular pathways that respond to sports practice led to the development of chemical interventions in order to simulate the physiological changes induced by physical exercise, without the practice of it. With this in mind, some substances that could have effects similar to physical exercise were guided.



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AICAR

AICAR, also known as AICA-ribonucleotide, is an intermediate metabolite in the synthesis pathway of new inosine monophosphate. It was first used in 1992 as a protective measure against heart disease. Aiming at exercise, AICAR has a pharmacological potential to activate the AMPK protein, this protein has a central role in cellular metabolism promoting greater beta-oxidation, better glucose uptake and an increase in mitochondrial biogenesis. In addition, AICAR has the potential to activate PGC-1 which also aids in mitochondrial biogenesis. Apparently, this metabolite is more involved with oxidative metabolism.

GSK4716

GSK4716 is an estrogen-related [EER]receptor agonist molecule. This molecule has effects on angiogenesis (greater formation of blood vessels), mitochondrial biogenesis and the transformation of muscle myofibrils, as well as a contribution in the activation of AMPK. This molecule is predominantly expressed in slow-twitch fibers, so GSK4716 plays a key role in regulating the phenotype of oxidative fibers.

GW501516

GW501516 is a PPAR agonist δ (Receptors activated by peroxisome proliferators), that is, it plays a role in the activation of this receptor. PPAR δ is a member of the nuclear receptor family that performs several vital functions in the regulation of skeletal muscle.

At first, GW501516 was used to increase the use of fatty acids in skeletal muscle, demonstrating a potential application in the treatment of diseases such as type 2 diabetes, dyslipidemias and metabolic syndrome.

SR9009

SR9009 is a synthetic agonist compound of REV-ERB α. REV-ERB α is a compound in the REV-ERB family of nuclear receptors. Some functions from SR9009 are a decrease in the flow of autophagy, an increased catabolism of fatty acids, an increase in mitochondrial biogenesis of skeletal muscle. Another point to note is that this compound apparently plays a role in regulating the circadian cycle.

MOTS-c

MOTS-c is a hormone encoded in the DNA of mitochondria. MOTS-c act on the folate cycle, which blocks the purine biosynthesis pathway, resulting in an accumulation of AICAR and consequently an increase in AMPK. Another effect of MOTS-c is the regulation of systemic glucose metabolism, restoring insulin sensitivity.

Irisin

Irisin is a myokine (a kind of cytokine) secreted by exercise-induced skeletal muscle and targets white adipose tissue. Basically, irisin stimulates the browning of white adipose tissue and increases protein expression (UCP-1), causing an increase in thermogenesis and energy expenditure, this effect has been reported as a possible additional in the treatment of obesity.

Epicatechins

Epicatechins are flavonoids found in teas, grapes, and plants. Some beneficial effects reported were, an increased availability of nitric oxide (increasing endothelial cells), angiogenesis in cardiac and skeletal muscles, in addition to promoting mitochondrial biogenesis. In addition, physiological properties have been reported to treat myocardial lesions.

Resveratrol

Resveratrol is a natural polyphenol, present in various foods, such as red wine, grapes and blueberries. The reported effects of this polyphenol were, increases in mitochondrial biogenesis, increased insulin sensitivity and greater angiogenesis. In addition, an optimized capacity in endurance exercise and potential for treatment in type II diabetes and obesity have been reported.

Clinical practice

As much as the physiological effects are potentially interesting, the amount and level of evidence on the substances mentioned above are very scarce and weak. In addition none of the substances showed significant effects compared to exercise.

With this in mind, more quality studies are needed to really elucidate the real magnitude of these substances, both in clinical and sports practice.

Bibliographic references

LI, Shunchang; LAHER, Ismail. Exercise Pills: at the starting line. Trends In Pharmacological Sciences, , v. 36, [S .L.]n. 12, p. 906-917, Dec. 2015. Http://dx.doi.org/10.1016/j.tips.2015.08.014 .

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