Synthesis and structure-activity relationship studies of theophylline analogs on population responses in the rat hippocampus in vitro.

We synthesized several theophylline analogs and tested the hypothesis that these compounds may be nootropic or cognitive enhancers by examining their effects on evoked population spikes recorded extracellularly in the CA1 region of the rat hippocampus. Whereas the length of the carbon chain on N7 had no effect, different size of the terminal lactam ring strongly influenced neuroactivity. Our results suggest that hexahydroazepin-2-one analogs have potential for further development as cognitive enhancers.

Spatio-Temporal Modelling of Dust Transport over Surface Mining Areas and Neighbouring Residential Zones.

Projects focusing on spatio-temporal modelling of the living environment need to manage a wide range of terrain measurements, existing spatial data, time series, results of spatial analysis and inputs/outputs from numerical simulations. Thus, GISs are often used to manage data from remote sensors, to provide advanced spatial analysis and to integrate numerical models. In order to demonstrate the integration of spatial data, time series and methods in the framework of the GIS, we present a case study focused on the modelling of dust transport over a surface coal mining area, exploring spatial data from 3D laser scanners, GPS measurements, aerial images, time series of meteorological observations, inputs/outputs form numerical models and existing geographic resources. To achieve this, digital terrain models, layers including GPS thematic mapping, and scenes with simulation of wind flows are created to visualize and interpret coal dust transport over the mine area and a neighbouring residential zone. A temporary coal storage and sorting site, located near the residential zone, is one of the dominant sources of emissions. Using numerical simulations, the possible effects of wind flows are observed over the surface, modified by natural objects and man-made obstacles. The coal dust drifts with the wind in the direction of the residential zone and is partially deposited in this area. The simultaneous display of the digital map layers together with the location of the dominant emission source, wind flows and protected areas enables a risk assessment of the dust deposition in the area of interest to be performed. In order to obtain a more accurate simulation of wind flows over the temporary storage and sorting site, 3D laser scanning and GPS thematic mapping are used to create a more detailed digital terrain model. Thus, visualization of wind flows over the area of interest combined with 3D map layers enables the exploration of the processes of coal dust deposition at a local scale. In general, this project could be used as a template for dust-transport modelling which couples spatial data focused on the construction of digital terrain models and thematic mapping with data generated by numerical simulations based on Reynolds averaged Navier-Stokes equations.

Influence of antioxidant effect of stobadine derivative in condition of kidney ischemia-reperfusion in a pre-clinical experiment (effect in therapy).

The goal of the study was to monitor the antioxidative effect of stobadine derivative under conditions of ischemia-reperfusion of laboratory rat kidney tissue. 40 animals were subjected to kidney tissue ischemia (60 min) followed by reperfusion (10 min). After that, the animals were divided by random selection into 4 groups (n = 10). The treated groups were given stobadine derivative in peroral doses of 5, 10 and 20 mg/kg in 0.5% solution of Avicel once a day, the placebo group was given only the solution of Avicel. One group (n = 10) was an intact group (without ischemia-reperfusion and without treatment), for comparison. Once a week, selected laboratory parameters were determined in all animals. On the 15th day the animals were exsanquined and organs were recovered for histopathological examination. We discovered a statistically significant changes of the superoxiddismutase and glutathione peroxidase catalytic activity; changes of total antioxidative capacity and malondialdehyde in the treated groups compared to the groups of placebo and intact. Other examined laboratory parameters (creatinine, urea and uric acid in blood; creatinine, urea, total protein in urine; diuresis) exhibited significant changes too. The results of biochemical examination show a protective antioxidative effect of the compound studied. The results of histopathological examination support this assumption.

Influence of antioxidant effect of stobadine derivative in condition of kidney ischemia-reperfusion in a pre-clinical experiment (effect in prophylaxis).

The goal of the study was to monitor the antioxidative effect of stobadine derivative in the conditions of ischemia-reperfusion of laboratory rat kidney tissue. The animals were divided by random selection into 5 groups (n = 10). The treated groups were given stobadine derivate in peroral doses of 5, 10 and 20 mg/kg in 0.5 % solution of Avicel once a day; the placebo group was given only the solution of Avicel. The last group was an intact group (without ischemia-reperfusion and without treatment). After conclusion of medication on the 15th day all animals were subjected to kidney tissue ischemia (60 min.) followed by reperfusion (10 min.). All animals were subsequently exsanquined and single identification of superoxiddismutase, glutathion peroxidase, total antioxidative capacity, and malondialdehyde level in the blood were determined. Kidneys were recovered for histopathological examination. A statistically significant decrease of the superoxiddismutase and statistically significant increase of the glutathione peroxidase catalytic activity in the treated groups compared to the groups of placebo and intact was discovered. There was also a statistically highly significant increase of total antioxidative capacity in the treated groups compared to the groups of placebo and intact. A statistically significant decrease of malondialdehyde level was identified in the treated groups compared to the groups of placebo and intact. The results of biochemical examination show a protective antioxidative effect of stobadine derivative. The results of histopathological examination support this assumption.