120 research outputs found
Influence of superior-subordinate communication on employee satisfaction
The paper concentrates on the review of the research carried out in the field of the relation between superior-subordinate communication in a company and its influence on employee job satisfaction in the last decade. The purpose of the paper has been to identify the possibilities of further research in that field in Poland. International research confirms direct and strong impact of good superiorsubordinate communication on employee satisfaction. In future studies in that field a qualitative component should be included as the studies carried so far were primarily correlational. Implications for further research in Poland cover checking Motivating Language Theory in Polish environment, directionality of behaviours, how employees form their perception on communication satisfaction, influence of gender on the perception of employee satisfaction and on managerial communication competence
OPTIMIZATION OF THE POSITION OF THE LOCAL DISTRIBUTION CENTRE OF THE REGIONAL POST LOGISTICS NETWORK
Loliolide – the most ubiquitous lactone
It is extremely interesting that this lactone also affects the behavior of ants as well as the development of certain plants (allelopathic activity). However, sometimes there are side effects as in the case of structural analogues of loliolide contributing to extinction of tropical coral.Niezmiernie interesujący jest fakt, że lakton ten wywiera również wpływ na zachowanie mrówek jak i na rozwój niektórych roślin (aktywność alleplopatyczna). Czasami jednak można zaobserwować również działania niepożądane jak w przypadku analogów strukturalnych loliolidu mających swój udział w wymieraniu raf tropikalnych
Diketopiperazine-Based, Flexible Tadalafil Analogues: Synthesis, Crystal Structures and Biological Activity Profile
Phosphodiesterase 5 (PDE5) is one of the most extensively studied phosphodiesterases
that is highly specific for cyclic-GMP hydrolysis. PDE5 became a target for drug development based
on its efficacy for treatment of erectile dysfunction. In the present study, we synthesized four novel
analogues of the phosphodiesterase type 5 (PDE5) inhibitor—tadalafil, which differs in (i) ligand
flexibility (rigid structure of tadalafil vs. conformational flexibility of newly synthesized
compounds), (ii) stereochemistry associated with applied amino acid building blocks, and (iii)
substitution with bromine atom in the piperonyl moiety. For both the intermediate and final
compounds as well as for the parent molecule, we have established the crystal structures and
performed a detailed analysis of their structural features. The initial screening of the cytotoxic effect
on 16 different human cancer and non-cancer derived cell lines revealed that in most cases, the
parent compound exhibited a stronger cytotoxic effect than new derivatives, except for two cell
lines: HEK 293T (derived from a normal embryonic kidney, that expresses a mutant version of SV40
large T antigen) and MCF7 (breast adenocarcinoma). Two independent studies on the inhibition of
PDE5 activity, based on both pure enzyme assay and modulation of the release of nitric oxide from
platelets under the influence of tadalafil and its analogues revealed that, unlike a reference
compound that showed strong PDE5 inhibitory activity, the newly obtained compounds did not
have a noticeable effect on PDE5 activity in the range of concentrations tested. Finally, we
performed an investigation of the toxicological effect of synthesized compounds on Caenorhabditis
elegans in the highest applied concentration of 6a,b and 7a,b (160 μM) and did not find any effect
that would suggest disturbance to the life cycle of Caenorhabditis elegans. The lack of toxicity
observed in Caenorhabditis elegans and enhanced, strengthened selectivity and activity toward the
MCF7 cell line made 7a,b good leading structures for further structure activity optimization and
makes 7a,b a reasonable starting point for the search of new, selective cytotoxic agents
Biotransformation of Bicyclic Halolactones with a Methyl Group in the Cyclohexane Ring into Hydroxylactones and Their Biological Activity
The aim of this study was the chemical synthesis of a series of halo- and unsaturated lactones, as well as their microbial transformation products. Finally some of their biological activities were assessed. Three bicyclic halolactones with a methyl group in the cyclohexane ring were obtained from the corresponding γ,δ-unsaturated ester during a two-step synthesis. These lactones were subjected to screening biotransformation using twenty two fungal strains. These strains were tested on their ability to transform halolactones into new hydroxylactones. Among the six strains able to catalyze hydrolytic dehalogenation, only two (Fusarium equiseti, AM22 and Yarrowia lipolytica, AM71) gave a product in a high yield. Moreover, one strain (Penicillium wermiculatum, AM30) introduced the hydroxy group on the cyclohexane ring without removing the halogen atom. The biological activity of five of the obtained lactones was tested. Some of these compounds exhibited growth inhibition against bacteria, yeasts and fungi and deterrent activity against peach-potato aphid
Synthesis and Physico-Chemical Properties in Aqueous Medium of All Possible Isomeric Bromo Analogues of Benzo-1H-Triazole, Potential Inhibitors of Protein Kinases.
In ongoing studies on the role of the individual bromine atoms of 4,5,6,7-tetrabromobenzotriazole (TBBt) in its relatively selective inhibition of protein kinase CK2α, we have prepared all the possible two mono-, four di-, and two tri- bromobenzotriazoles, and determined their physico-chemical properties in aqueous medium. They exhibited a general trend of a decrease in solubility with an increase in the number of bromines on the benzene ring, significantly modulated by the pattern of substitution. For a given number of attached bromines, this was directly related to the electronic effects resulting from different sites of substitution, leading to marked variations of pKa values for dissociation of the triazole proton. Experimental data (pKa, solubility) and ab initio calculations demonstrated that hydration of halogenated benzotriazoles is driven by a subtle balance of hydrophobic and polar interactions. The combination of QM-derived free energies for solvation and proton dissociations was found to be a reasonably good predictor of inhibitory activity of halogenated benzotriazoles vs CK2α. Since the pattern of halogenation of the benzene ring of benzotriazole has also been shown to be one of the determinants of inhibitory potency vs some viruses and viral enzymes, the present comprehensive description of their physico-chemical properties should prove helpful in efforts to elucidate reaction mechanisms, including possible halogen bonding, and the search for more selective and potent inhibitors
A Comparative Study of Interannual Oscillation Models for Determining Geophysical Polar Motion Excitations
Similar to seasonal and intraseasonal variations in polar motion (PM), interannual variations are also largely caused by changes in the angular momentum of the Earth’s geophysical fluid layers composed of the atmosphere, the oceans, and in-land hydrologic flows (AOH). Not only are inland freshwater systems crucial for interannual PM fluctuations, but so are atmospheric surface pressures and winds, oceanic currents, and ocean bottom pressures. However, the relationship between observed geodetic PM excitations and hydro-atmospheric models has not yet been determined. This is due to defects in geophysical models and the partial knowledge of atmosphere–ocean coupling and hydrological processes. Therefore, this study provides an analysis of the fluctuations of PM excitations for equatorial geophysical components χ1 and χ2 at interannual time scales. The geophysical excitations were determined from different sources, including atmospheric, ocean models, Gravity Recovery and Climate Experiment (GRACE) and GRACE Follow-On data, as well as from the Land Surface Discharge Model. The Multi Singular Spectrum Analysis method was applied to retain interannual variations in χ1 and χ2 components. None of the considered mass and motion terms studied for the different atmospheric and ocean models were found to have a negligible effect on interannual PM. These variables, derived from different Atmospheric Angular Momentum (AAM) and Oceanic Angular Momentum (OAM) models, differ from each other. Adding hydrologic considerations to the coupling of AAM and OAM excitations was found to provide benefits for achieving more consistent interannual geodetic budgets, but none of the AOH combinations fully explained the total observed PM excitations
Synthesis and Biotransformation of Bicyclic Unsaturated Lactones with Three or Four Methyl Groups
The aim of this study was to obtain new unsaturated lactones by chemical synthesis and their microbial transformations using fungal strains. Some of these strains were able to transform unsaturated lactones into different hydroxy or epoxy derivatives. Strains of Syncephalastrum racemosum and Absidia cylindrospora gave products with a hydroxy group introduced into a tertiary carbon, while the Penicillium vermiculatum strain hydroxylated primary carbons. The Syncephalastrum racemosum strain hydroxylated both substrates in an allylic position. Using the Absidia cylindrospora and Penicillium vermiculatum strains led to the obtained epoxylactones. The structures of all lactones were established on the basis of spectroscopic data
Phosphorylation of Thymidylate Synthase and Dihydrofolate Reductase in Cancer Cells and the Effect of CK2α Silencing
Our previous research suggests an important regulatory role of CK2-mediated phosphorylation of enzymes involved in the thymidylate biosynthesis cycle, i.e., thymidylate synthase (TS), dihydrofolate reductase (DHFR), and serine hydroxymethyltransferase (SHMT). The aim of this study was to show whether silencing of the CK2α gene affects TS and DHFR expression in A-549 cells. Additionally, we attempted to identify the endogenous kinases that phosphorylate TS and DHFR in CCRF-CEM and A-549 cells. We used immunodetection, immunofluorescence/confocal analyses, reverse transcription–quantitative polymerase chain reaction (RT-qPCR), in-gel kinase assay, and mass spectrometry analysis. Our results demonstrate that silencing of the CK2α gene in lung adenocarcinoma cells significantly increases both TS and DHFR expression and affects their cellular distribution. Additionally, we show for the first time that both TS and DHFR are very likely phosphorylated by endogenous CK2 in two types of cancer cells, i.e., acute lymphoblastic leukaemia and lung adenocarcinoma. Moreover, our studies indicate that DHFR is phosphorylated intracellularly by CK2 to a greater extent in leukaemia cells than in lung adenocarcinoma cells. Interestingly, in-gel kinase assay results indicate that the CK2α’ isoform was more active than the CK2α subunit. Our results confirm the previous studies concerning the physiological relevance of CK2-mediated phosphorylation of TS and DHFR
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