Browsing by Author "Ebensperger, Roberto"

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    Evaluation of new natural compound formulations on the modification of metabolic syndrome components among overweight adults
    (2022) Ebensperger, Roberto; Moreno, Manuel; Plaza, Cristian; Bridi, Raquel
    Overweight and obesity, increasingly frequent conditions in Chile and the world, are defined as chronic diseases characterized by the excessive accumulation of body fat, that can be detrimental to health. Excess body fat is the main pathogenic factor for the development of insulin resistance and metabolic syndrome, the latter characterized by a cluster of metabolic abnor-malities that increase risk of metabolic diseases and cardiovascular mortality. The objective of this preliminary cross-sectional, observational study was to evaluate a new formulation of natural compounds, Delphinol (R), resveratrol and oleanolic acid, against metabolic syndrome components in a young population with excess weight, through the intake during 22 weeks of the new formulation. The evaluation was carried out based on the clinical and anthropometric status of 20 volunteer subjects (both gender, 18 to 30 years and BMI26 to 42), medical evaluation and laboratory tests using each metabolic syndrome component (abdominal obesity, triglycerides, HDL, blood pressure y fasting glicaemia). It was observed that with the daily intake of this formulation there was a significant reduction in blood glucose levels, HOMA-IR index, triglycerides and an increase in HDL-cholesterol. These preliminary results would translate into a benefit in the health status of overweight and obese individuals, which would impact on reducing rates of metabolic syndrome. Thus, slowing down the progression of chronic diseases such as diabetes and dyslipidemia, and also contributing to decreasing the associated cardiometabolic risk.
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    New NADPH Oxidase 2 Inhibitors Display Potent Activity against Oxidative Stress by Targeting p22phox-p47phox Interactions
    (2023) Treuer, Adriana V.; Faundez, Mario; Ebensperger, Roberto; Hovelmeyer, Erwin; Vergara-Jaque, Ariela; Perera-Sardina, Yunier; Gutierrez, Margarita; Fuentealba, Roberto; Gonzalez, Daniel R.
    NADPH oxidase (NOX2) is responsible for reactive oxygen species (ROS) production in neutrophils and has been recognized as a key mediator in inflammatory and cardiovascular pathologies. Nevertheless, there is a lack of specific NOX2 pharmacological inhibitors. In medicinal chemistry, heterocyclic compounds are essential scaffolds for drug design, and among them, indole is a very versatile pharmacophore. We tested the hypothesis that indole heteroaryl-acrylonitrile derivatives may serve as NOX2 inhibitors by evaluating the capacity of 19 of these molecules to inhibit NOX2-derived ROS production in human neutrophils (HL-60 cells). Of these compounds, C6 and C14 exhibited concentration-dependent inhibition of NOX2 (IC50-1 mu M). These molecules also reduced NOX2-derived oxidative stress in cardiomyocytes and prevented cardiac damage induced by ischemia-reperfusion. Compound C6 significantly reduced the membrane translocation of p47(phox), a cytosolic subunit that is required for NOX2 activation. Molecular docking analyses of the binding modes of these molecules with p47(phox) indicated that C6 and C14 interact with specific residues in the inner part of the groove of p47(phox), the binding cavity for p22(phox). This combination of methods showed that novel indole heteroaryl acrylonitriles represent interesting lead compounds for developing specific and potent NOX2 inhibitors.
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    Photophysical characterization of atorvastatin (Lipitor (R)) ortho-hydroxy metabolite : role of hydroxyl group on the drug photochemistry
    (2010) Alarcón Abarzúa, Emilio Isaac; González Béjar, María; Gorelsky, Serge; Ebensperger, Roberto; López Alarcón, Camilo Ignacio; Carlos Netto Ferreira, José; Scaiano, Juan C.