Bifunctional Opioid/Melanocortin Peptidomimetics for Use in Neuropathic Pain: Variation in the Type and Length of the Linker Connecting the Two Pharmacophores

Based on the mechanism of neuropathic pain induction, a new type of bifunctional hybrid peptidomimetics was obtained for potential use in this type of pain. Hybrids consist of two types of pharmacophores that are connected by different types of linkers. The first pharmacophore is an opioid agonist, and the second pharmacophore is an antagonist of the pronociceptive system, i.e., an antagonist of the melanocortin-4 receptor. The results of tests in acute and neuropathic pain models of the obtained compounds have shown that the type of linker used to connect pharmacophores had an effect on antinociceptive activity. Peptidomimetics containing longer flexible linkers were very effective at low doses in the neuropathic pain model. To elucidate the effect of linker lengths, two hybrids showing very high activity and two hybrids with lower activity were further tested for affinity for opioid (mu, delta) and melanocortin-4 receptors. Their complexes with the target receptors were also studied by molecular modelling. Our results do not show a simple relationship between linker length and affinity for particular receptor types but suggest that activity in neuropathic pain is related to a proper balance of receptor affinity rather than maximum binding to any or all of the target receptors.     

Hydrostatic pressure influence on electric relaxation response of bismuth manganite ceramics

Electrical impedance of bismuth manganite ceramics was studied under ambient and high hydrostatic pressure. Local disorder of crystal lattice was confirmed using XRD and DSC. Two relaxation processes were discerned. One was attributed to small polarons, which showed a changeover from variable range hopping features related to Fermi glass and structural disorder to the nearest neighbor hopping behavior in higher temperature range related to uniform distribution of energy levels. Hydrostatic pressure shortened relaxation times that would be interesting for applications. The second process, which was assigned to the nearest neighbor hopping of polarons, also exhibited a changeover to glassy features in a high-temperature range.     

High resolution SEM characterization of nano‐precipitates in ODS steels

The performance of the present‐day scanning electron microscopy (SEM) extends far beyond delivering electronic images of the surface topography. Oxide dispersion strengthened (ODS) steel is on of the most promising materials for the future nuclear fusion reactor because of its good radiation resistance, and higher operation temperature up to 750°C. The microstructure of ODS should not exceed tens of nm, therefore there is a strong need in a fast and reliable technique for their characterization. In this work, the results of low‐kV SEM characterization of nanoprecipitates formed in the ODS matrix are presented. Application of highly sensitive photo‐diode BSE detector in SEM imaging allowed for the registration of single nm‐sized precipitates in the vicinity of the ODS alloys. The composition of the precipitates has been confirmed by TEM‐EDS.     

The Uneven Rate of the Molecular Evolution of Gene Sequences of DNA-Dependent RNA Polymerase I of the Genus Lamium L

RNA polymerase type I (plastid-encoded polymerase, PEP) is one of the key chloroplast enzymes. However, the rpo genes that encode its subunits (rpoA, rpoB, rpoC1 and rpoC2) are relatively rapidly evolving sequences. The aim of this study was to investigate the rate of the molecular evolution of rpo genes and to evaluate them as phylogenetic markers on the example of the genus Lamium L. (Lamiaceae). The analyzed genes were shown to differ in the level of variation, rate of intragenic mutations, phylogenetic informativeness, and in the impact of these mutations on the properties of encoded peptides. Destabilizing effects of the positive pressure were observed in all genes examined coding for PEP enzyme. We have demonstrated the relationship between mutations fixed by positive selection and the separation of phylogenetic lines within the genus Lamium. The study showed also that the rpo genes were reliable phylogenetic markers, useful in the reconstruction of interconnections of species belonging to the same genus. Of the four tested genes, the most promising phylogenetic marker was rpoA gene, while the least useful gene appeared to be rpoC1.     

Novel conventional and chelating anion exchange resins with amino ligands for sorption of silver

ABSTRACT

The polymeric resins containing diethylenetriamine, tetraethylenepentamine, 2-(diethylamino)ethanol, 1-methylimidazole, and 1,2-dimethylimidazole ligands have been synthesized from vinylbenzyl chloride-divinylbenzene copolymers and used in the removal of Ag(I) from chloride solution. The best Ag(I) sorption was reached in the case of 1-methylimidazole resin. Resins retain their capacity towards Ag(I) in five consecutive sorption/desorption cycles. The resins with imidazole ligands were highly selective for Ag(I) from synthetic chloride solution and they did not sorb chloride complexes of Cu(II). Additionally, the recovery of Ag(I) was tested from real chloride solution coming from leaching of the copper concentrate from Lubin Concentrator (KGHM Polska Mied? S.A.).     

Analysis of indole compounds in edible Basidiomycota species after thermal processing

Methanolic extracts of processed fruiting bodies of six edible mushroom species (Basidiomycota) - Armillaria mellea, Boletus badius, Boletus edulis, Cantharellus cibarius, Lactarius deliciosus collected from natural habitats and Pleurotus ostreatus of commercial origin - were analysed for the presence of non-hallucinogenic indole compounds. Thermal processing was designed in such a way that it mimicked conditions used for cooking of mushroom dishes, since only a narrow group of mushrooms can be eaten raw, while indole compounds are thermolabile. All processed extracts were shown to contain l-tryptophan (up to 8.92 mg/100 g dw). The contents of the remaining compounds, 5-methyltryptophan, tryptamine, melatonin, indoleacetonitrile and indole, varied in different species (from 0.71 to 6.55 mg/100 g dw). Extract of processed C. cibarius fruiting bodies contained l-tryptophan, 5-methyltryptophan, tryptamine, melatonin, indoleacetonitrile and indole (1.96-4.94 mg/100 g dw) whereas l-tryptophan (2.78 mg/100 g dw) and tryptamine (2.77 mg/100 g dw) were the only indole compounds identified in the processed fruiting bodies of A. mellea.     

Occurrence of Campylobacter spp. in poultry and poultry products for sale on the Polish retail market

In 2007 and 2008, a monitoring study was carried out in Poland to examine the occurrence of thermotolerant Campylobacter spp. in raw and cooked chicken products available on the retail market. A total of 912 samples were tested: 443 samples of raw chicken meat, 146 samples of giblets, and 323 ready-to-eat poultry products (150 samples of spit-roasted chicken, 56 samples of smoked chicken, and 117 samples of paté and cold meats). A high level of contamination of raw chicken meat (51.7% of samples) and chicken giblets (47.3% of samples) was detected. However, thermotolerant Campylobacter spp. were found in only 1.2% of the ready-to-eat poultry products.     

Effect of Cover Brine Type on the Quality of Meat from Herring Marinades

Effects of vinegar, oil, and sour cream brines on meat quality of 4 popular cold marinades from herring were investigated in the study. Cover brine type affected the composition and nutritive value of meat as well as the sensory and microbiological quality of marinated herring. Qualitative differences resulted from cover brine penetration into meat, and from diffusion of components from meat to vinegar brine. Compared to oil and sour cream, vinegar brine contributed to increased concentrations of salt and acetic acid, hardness, color brightness of marinades meat and to increased microbial contamination of meat. Furthermore, vinegar caused nitrogen losses to 15%, including valuable products of protein hydrolysis, enzymes, and total volatile bases. The rolling up of fillets reduced diffusion even by 50%. In turn, oil and sour cream were causing mainly a higher fat content and overall sensory evaluation of the marinades.     

Comparison of antimicrobial resistance of Campylobacter jejuni and Campylobacter coli isolated from humans and chicken carcasses in Poland

Campylobacter-associated gastroenteritis remains an important cause of morbidity worldwide, and some evidence suggests that poultry is an important source of this foodborne infection in humans. This study was conducted to analyze the prevalence and genetic background of resistance of 149 Campylobacter jejuni and 54 Campylobacter coli strains isolated from broiler chicken carcasses and from stool samples of infected children in Poland from 2003 through 2005. Nearly all isolates were susceptible to macrolides and aminoglycosides. The highest resistance in both human and chicken strains was observed for ciprofloxacin (more than 40%), followed by ampicillin (13 to 21%), and tetracycline (8 to 29%). Resistance to ampicillin and tetracycline rose significantly between 2003 and 2005. Slight differences in resistance between human and chicken isolates indicate that although chicken meat is not the only source of Campylobacter infection in our population, it can be involved in the transmission of drug-resistant Campylobacter strains to humans.