Abstract
Peroxisome proliferator-activated receptor-γ (PPAR-γ) is a major receptor responsible for the pathogenesis of type 2 diabetes mellitus (T2DM). Deficiency in the human body of ligands binding to PPAR-γ causes the disorder of expression of many genes in adipose tissue and contributes to reducing tissue sensitivity to insulin, making it difficult to maintain glucose homeostasis, which consequently leads to T2DM. Therefore, natural non-toxic PPAR-γ ligands are sought. The aim of the research was to assess the affinity of single hydroxycinnamic or chlorogenic acids, coffee extracts and bioactive isolates from various coffee extracts of green, light and dark roasted Arabica and Robusta for PPAR-γ. This allows determining what type of coffee extract or its fraction can be used for therapy of T2DM. The research was carried out by means of isothermal titration calorimetry and molecular docking simulation. The studies have shown that caffeine and dihydrocaffeic acid had the highest affinity for PPAR-γ, which amounted ΔG = − 39.46 kJ mol−1 and − 33.60 kJ mol−1, respectively.
Highlights
The high percentage of the world’s population suffers from metabolic disorders such as diabetes mellitus (DM) or is at high risk of becoming ill
Peroxisome proliferator-activated receptor-γ (PPAR-γ) is a hormone mainly responsible for gene expression involved in fats and carbohydrates metabolism, which causes increasing the level of insulin sensitivity, contributing to maintenance of glucose homeostasis [12, 13]
We checked whether the compounds contained in coffee are potential activators of the PPAR-γ receptor to help prevention and therapy of type 2 diabetes mellitus (T2DM)
Summary
The high percentage of the world’s population suffers from metabolic disorders such as diabetes mellitus (DM) or is at high risk of becoming ill. Type I diabetes is a genetic disease and affects young people, and the main feature of the development of the disease is the destruction of insulin-producing pancreatic β-cells by the immune system, until the pancreas stops producing insulin completely, Peroxisome proliferator-activated receptor-γ (PPAR-γ) is a hormone mainly responsible for gene expression involved in fats and carbohydrates metabolism, which causes increasing the level of insulin sensitivity, contributing to maintenance of glucose homeostasis [12, 13]. The activation of PPAR-γ by their ligands induces the expression of proteins, such as lipoprotein lipase, reduces inflammation and thereby controls fatty acid metabolism,
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