RESUMEN
Human serum albumin (HSA) has a very significant role in the transport of drugs, in their pharmacokinetic and pharmacodynamic properties, as well as the unbound concentration of drugs in circulating plasma. The aim of this study was to look into the competition between tigecycline (TGC) and alkaloid (ALK) (caffeine (CAF)), and flavonoids (FLAVs) (catechin (CAT), quercetin (QUE), and diosmin (DIO)) in binding to HSA in simulated physiological conditions using multiple spectroscopic measurements and docking simulations. Fluorescence analysis was used to find the binding and quenching properties of double HSA-TGC and triple HSA-TGC-CAF/FLAV systems. The conformational change of the HSA was analyzed using synchronous fluorescence spectroscopy, Fourier transform infrared spectroscopy, and circular dichroism. Obtained results of spectroscopic analyses indicate that triple complexes of HSA-TGC-CAF/FLAVs are formed without problems and have higher binding affinities than double HSA-TGC. In addition, TGC does not change the microenvironments around the tryptophan (Trp) and tyrosine (Tyr) residues in the presence of ALK and FLAVs. Ultimately, the binding affinity, competition, and interaction nature were explored by docking modeling. Computational outcomes are in good accordance with experimentally obtained results. Accordingly, concluding remarks may be very useful for potential interactions between common food components and drugs.
RESUMEN
The aim of this study was to identify some of the secondary metabolites present in acetonic, methanolic, and hexanic extracts of lichen Xanthoparmelia stenophylla and to examine their antioxidant, antimicrobial, and cytotoxic activity. Compounds of the depsid structure of lecanoric acid, obtusic acid, and atranorin as well as usnic acid with a dibenzofuran structure were identified in the extracts by HPLC. The acetone extract was shown to have the highest total phenolic (167.03 ± 1.12 mg GAE/g) and total flavonoid content (178.84 ± 0.93 mg QE/g) as well as the best antioxidant activity (DPPH IC50 = 81.22 ± 0.54). However, the antimicrobial and antibiofilm tests showed the best activity of hexanic extract, especially against strains of B. cereus, B. subtilis, and S. aureus (MIC < 0.08, and 0.3125 mg/mL, respectively). Additionally, by using the MTT method, the acetonic extract was reported to exhibit a strong cytotoxic effect on the HeLa and HCT-116 cell lines, especially after 72 h (IC50 = 21.17 ± 1.85 and IC50 = 21.48 ± 3.55, respectively). The promising antioxidant, antimicrobial, and cytotoxic effects of Xanthoparmelia stenophylla extracts shown in the current study should be further investigated in vivo and under clinical conditions.
RESUMEN
BACKGROUND: The purpose of this study is to determine the effect of L-ascorbic acid and alpha-tocopherol as well as combination of these vitamins with or without exposure to physical exercise on intensity of lipid peroxidation, activity of xanthine oxidase, activity of total antioxidative system, concentration of glutathione, and activity of catalase in the serum of guinea pigs. MATERIALS AND METHODS: The experimental measurements of intensity of lipid peroxidation, activity of xanthine oxidase, activity of total antioxidative system, concentration of glutathione, and activity of catalase were done in the serum of guinea pigs. The animals were exposed to the test load to achieve exhaustion and the test was terminated when the animal for the third time to sink into the water. RESULTS: The results of this study demonstrated that endurance exercise of guinea pigs induced oxidative stress response in terms of increased lipid peroxidation and activity of xanthine oxidase in the serum of experimental animals. Our study investigated the antioxidant activity of L-ascorbic acid and alpha-tocopherol also measuring three protective markers in the serum: total antioxidant activity, content of glutathione and activity of catalase. The results obtained show that the vitamins influence the concentrations of above mentioned biochemical parameters, which points out their protective effect of swimming-induced oxidative stress. CONCLUSION: Single or combined administration of L-ascorbic acid and alpha-tocopherol caused significant inhibition of these markers indicating the important antioxidant activity of the vitamins. Results lead to conclude that the combined treatments with vitamins with or without exposure to physical exercise showed the clear synergistic effect..