Hypoglycemic and antioxidant properties of extracts of medicinal plants Galega officinalis L. (aboveground part) and yacon (Smallanthus sonchifolius Poepp. & Endl.) (leaves) as potential sources of biologically active substances with antidiabetic action have been studied. The pronounced hypoglycemic effect of Galega officinalis extract, devoid of alkaloids, at a dose of 600 mg/kg in experimental diabetes mellitus (DM) has been proven. The established effect is evidenced by a decrease in the concentration of glucose and glycosylated hemoglobin in the blood, increase glucose tolerance of cells, increase C-peptide and insulin content in the plasma of rats’ blood. The effective hypoglycemic effect of the extract in the studied pathology was confirmed by histological examination of the pancreas. The cytoprotective effect of the studied extract on pancreatic cells at a dose of 1200 mg/kg was experimentally confirmed. In the standard cut area, an increase was found in the number of Langerhans islets, their average area, diameter, volume, and a number of β-cells relative to these indicators in animals with diabetes. Comparative screening of the antioxidant properties of 30, 50, 70, and 96% water–ethanol extracts of yacon indicates the highest potential of 50% water-ethanol extract to block free radicals in in vitro model experiments. The non-alkaloid fraction of Galega officinalis extract showed moderate antioxidant activity and was inferior to yacon extract in its ability to neutralize reactive oxygen species (ROS) and bind metal ions of variable valence. The level of antioxidant potential of the studied extracts is due to differences in the quantitative content of compounds of phenolic nature in their compositions. The obtained data on the biological effects of Galega officinalis extract on the structural and functional state of β-cells of the pancreas and antioxidant properties of Galega officinalis and yacon extracts substantiate the prospects of using these plants to create antidiabetic medicines and functional foods based on them.
The aim of this study was to evaluate the therapeutic effects of chlorogenic acid (CGA) in rats with advanced alcoholic steatohepatitis. The rats were fed on a high-fat diet and gavaged with ethanol (4 g/kg) for 8 weeks. The livers of ethanol-treated rats showed steatosis; necrosis and mononuclear infiltration; and significant upregulation of the mRNA expression of the prooxidant (Cyp2e1, iNos), lipogenic (Srebp1, Acc), proinflammatory (Tlr4, Nf-κb, TnfA, Il-1B, and Il-6), and profibrogenic (TgfB, Col1, VegfA) genes. Simultaneously, a downregulation of level of Sod and Nrf2 was observed, which was accompanied by increased serum transaminase, TnfA, and serum and liver triglycerides levels. CGA administration (40 and 80 mg/kg, 8 weeks) to ethanol-fed group reduced the liver expression levels of Cyp2e1 and iNos, whereas it markedly enhanced the expression of Sod, Nrf2, and Ho-1. CGA at both doses downregulated the expressions of lipogenic, proinflammatory, and profibrogenic genes, while the expression of Tlr4 was lowered only after the higher dose of CGA. The higher dose of CGA efficiently prevented the progression of alcohol-induced steatosis and reduced inflammation through regulation of the expression of genes encoding the proteins involved in the Tlr4/Nf-κB signaling pathway and fibrosis. The study revealed hepatoprotective and anti-inflammatory effects of CGA through the regulation of expression of genes encoding Cyp2e1/Nrf2 involved in oxidative stress modulation. These results demonstrate CGA as a therapeutic candidate for the prevention and treatment of alcoholic steatohepatitis.
The interaction between sertraline hydrochloride (SRT) and randomly methylated β-cyclodextrin (RMβCD) molecules have been investigated at 298.15 K under atmospheric pressure. The method used—Isothermal Titration Calorimetry (ITC) enabled to determine values of the thermodynamic functions like the enthalpy (ΔH), the entropy (ΔS) and the Gibbs free energy (ΔG) of binding for the examined system. Moreover, the stoichiometry coefficient of binding (n) and binding/association constant (K) value have been calculated from the experimental results. The obtained outcome was compared with the data from the literature for other non-ionic βCD derivatives interacting with SRT and the enthalpy-entropy compensation were observed and interpreted. Furthermore, the connection of RMβCD with SRT was characterized by circular dichroism spectroscopy (CD) and complexes of βCD derivatives with SRT were characterized through the computational studies with the use of molecular docking (MD).