Molecular targets of exercise mimetics and their natural activators

Jang, Young Jin; Byun, Sun‐Sig

doi:10.5483/bmbrep.2021.54.12.151

Cited by 10 publications

(4 citation statements)

References 126 publications

(135 reference statements)

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“…However, exercise adherence tends to be generally low, and various factors such as illness, injuries and aging can often limit or hinder mobility. This is where “exercise-mimetic pills” can assume a pivotal role in replicating in the SM some of the beneficial effects of exercise on human health: improving oxidative metabolism, mitochondrial biogenesis and activity, insulin sensitivity and the cellular stress response among several other in vivo mechanisms [ 45 , 46 , 47 ].…”

Section: Discussionmentioning

confidence: 99%

Syrah Grape Polyphenol Extracts Protect Human Skeletal Muscle Cells from Oxidative and Metabolic Stress Induced by Excess of Palmitic Acid: Effect of Skin/Seed Ripening Stage

Capozzi,

Dudoit,

Garcia

et al. 2024

Antioxidants

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Metabolic skeletal muscle (SM) dysfunction, triggered by increased oxidative stress and mitochondrial impairment, is a pivotal contributor to obesity-associated insulin resistance (IR). Addressing obesity and SM IR demands substantial lifestyle changes including regular exercise and dietary adjustments that are difficult to follow over time. This prompted exploration of alternative approaches. Grape polyphenols (GPPs) have demonstrated a positive impact on metabolism, although few studies have focused on SM. Since grape polyphenolic content and composition depend on tissue and ripening, we explored the antioxidant potential of GPPs from skin (Sk) and seeds (Sd) extracted before veraison (Bv) and at mature (M) stages, on palmitate-induced IR in primary human SM cells. Despite their important difference in polyphenol (PP) content: Sd-BvPP > Sd-MPP/Sk-BvPP > Sk-MPP, all extracts reduced lipid peroxidation by 44–60%, up-regulated the heme-oxygenase 1 protein level by 75–132% and mitochondrial activity by 47–68%. Contrary to the other extracts, which improved insulin response by 50%, Sd-BvPP did not. Our findings suggest that compounds other than stilbenoids or anthocyanin-type molecules, present only in grape Sk, could play an active role in regulating SM oxidative and metabolic stress and insulin sensitivity, paving the way for further exploration of novel bioactive compounds.

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Section: Discussionmentioning

confidence: 99%

Syrah Grape Polyphenol Extracts Protect Human Skeletal Muscle Cells from Oxidative and Metabolic Stress Induced by Excess of Palmitic Acid: Effect of Skin/Seed Ripening Stage

Capozzi,

Dudoit,

Garcia

et al. 2024

Antioxidants

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“…Some compounds, such as 5-aminoimidazole-4-carboxamide ribonucleotide (AICAR), have been shown to activate AMPK and improve muscle function [ 185 ]. In addition to PPARδ agonist and AICAR, there have been numerous studies on exercise mimetics utilizing peroxisome proliferator-activated receptor γ coactivator-1α (PGC-1α) modulators, nuclear factor erythroid 2–related factor 2 (Nrf2) modulators, irisin, and others [ 186 , 187 , 188 ]. However, currently, there are no exercise mimetics that are used in clinical practice, and further research is needed to clarify the molecular mechanisms and other aspects.…”

Section: Exercise Mimeticsmentioning

confidence: 99%

Pathogenesis, Intervention, and Current Status of Drug Development for Sarcopenia: A Review

Jang

Kim

2023

Biomedicines

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Sarcopenia refers to the loss of muscle strength and mass in older individuals and is a major determinant of fall risk and impaired ability to perform activities of daily living, often leading to disability, loss of independence, and death. Owing to its impact on morbidity, mortality, and healthcare expenditure, sarcopenia in the elderly has become a major focus of research and public policy debates worldwide. Despite its clinical importance, sarcopenia remains under-recognized and poorly managed in routine clinical practice, partly owing to the lack of available diagnostic testing and uniform diagnostic criteria. Since the World Health Organization and the United States assigned a disease code for sarcopenia in 2016, countries worldwide have assigned their own disease codes for sarcopenia. However, there are currently no approved pharmacological agents for the treatment of sarcopenia; therefore, interventions for sarcopenia primarily focus on physical therapy for muscle strengthening and gait training as well as adequate protein intake. In this review, we aimed to examine the latest information on the epidemiology, molecular mechanisms, interventions, and possible treatments with new drugs for sarcopenia.

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“…Another target for exercise-mimetics in ERRγ, which regulates mitochondrial oxidative genes. GSK4716, a synthetic agonist of ERRγ led to upregulation of genes of mitochondrial biogenesis, fatty acid oxidation and TCA cycle (43); the in vivo effects are not known.…”

Section: Sirt1 Activators and Other Agentsmentioning

confidence: 99%

Exercise Mimetics: Fact Or Fantasy?

Lakshmi¹,

Sridhar²

2021

Adipobiology

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The abundant health benefits of physical exercise are not being translated into practice. In an effort to short circuit the need for physical activity to promote health, exercise-mimetic agents are being developed; they mimic the action of peptide molecules released from exercised muscles. The intention is to mimic biochemical responses even without performing exercise. Technologies have advanced to identify various exercise-induced proteins, called myokines, and to develop ligands which bind to the myokine receptors. A number of such chemicals exist that mimic the effects of activating Peroxisome proliferator-activated receptor-γ (PPARγ) coactivator 1α (PGC-1 α), Peroxisome proliferator-activated receptor β/δ (PPAR β/δ) and AMP-activated protein kinase (AMPK). Most such agents were tested in animal models with varying degrees of success and mostly undesirable adverse effects. The increasing complexity of exercise response is being recognized, making the development and use of single 'exercise-mimetics' ineffective, except for some narrow indications. In addition, some of the performance enhancing exercise-mimetics are being misused by endurance athletes, with the chemicals being banned as doping agents. In a fascinating interaction between physiology and pharmacology, agents that can mimic the beneficial effects of physical exercise are an enticing possibility over the distant horizon.

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Molecular targets of exercise mimetics and their natural activators

Cited by 10 publications

References 126 publications

Syrah Grape Polyphenol Extracts Protect Human Skeletal Muscle Cells from Oxidative and Metabolic Stress Induced by Excess of Palmitic Acid: Effect of Skin/Seed Ripening Stage

Syrah Grape Polyphenol Extracts Protect Human Skeletal Muscle Cells from Oxidative and Metabolic Stress Induced by Excess of Palmitic Acid: Effect of Skin/Seed Ripening Stage

Pathogenesis, Intervention, and Current Status of Drug Development for Sarcopenia: A Review

Exercise Mimetics: Fact Or Fantasy?

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