69 research outputs found
State and Perspectives of Information System Student at the Technical University of Kosice, Slovakia
The paper describes functions of pedagogic information system (IS Student) and presents vision of new pedagogic information system as a part of complex solution of university information system. Present system involves all faculties and is based on modern technologies (SQL, client/server architecture, WWW interface). Due to increasing requirements of the users we decided to redesign pedagogic information system. Based on more than six years experience of the maintenance of the system, it gives us imagination, how to cover all information needs of academic community of the Technical University in Košice. The paper gives a brief characteristics of the modules of the integrated information system of the Technical University in Košice which, except the maintenance of the IS STUDENT, are the subject of our study with an effective cooperation of users. It outlines the use of modelling tools and realization of project aims consisting of new PIS generation
Synthesis and biological evaluation of benzochromenopyrimidinones as cholinesterase inhibitors and potent antioxidant, non-hepatotoxic agents for Alzheimer’s disease
We report herein the straightforward two-step synthesis and biological assessment of novel racemic benzochromenopyrimidinones as non-hepatotoxic, acetylcholinesterase inhibitors with antioxidative properties. Among them, compound 3Bb displayed a mixed-type inhibition of human acetylcholinesterase (IC50 = 1.28 ± 0.03 μM), good antioxidant activity, and also proved to be non-hepatotoxic on human HepG2 cell line.JMC thanks Government of Spain for support (SAF2016-65586-R), JJ and OS thank
MH CZ- DRO (UHHK 00179906).We acknowledge support by the CSIC Open Access Publication Initiative through its Unit of Information Resources for Research (URICI)
Design, synthesis and in vitro evaluation of benzothiazole-based ureas as potential ABAD/17β-HSD10 modulators for Alzheimer’s disease treatment
This work was supported by the Ministry of Health of the Czech Republic (no. NV15-28967A), Charles University in Prague (no. GAUK B-CH/992214, SVV 260 291) and the Alzheimer’s Society (specifically The Barcopel Foundation). This research is part-funded by the MSD Scottish Life Sciences fund.Amyloid-beta peptide (Aβ) has been recognized to interact with numerous proteins, which may lead to pathological changes in cell metabolism of Alzheimer’s disease (AD) patients. One such known metabolic enzyme is mitochondrial amyloid-binding alcohol dehydrogenase (ABAD), also known as 17β-hydroxysteroid dehydrogenase type 10 (17β-HSD10). Altered enzyme function caused by the Aβ-ABAD interaction, was previously shown to cause mitochondrial distress and a consequent cytotoxic effect, therefore providing a feasible target in AD drug development. Based on previous frentizole derivatives studies, we report two novel series of benzothiazolyl ureas along with novel insights into the structure and activity relationships for inhibition of ABAD. Two compounds ( 37 , 39 ) were identified as potent ABAD inhibitors, where compound 39 exhibited comparable cytotoxicity with the frentizole standard; however, one-fold higher cytotoxicity than the parent riluzole standard. The calculated and experimental physical chemical properties of the most potent compounds showed promising features for blood-brain barrier penetration.PostprintPeer reviewe
Modelling Tools for Life Cycle of Pedagogic Information System at Tu Kosice, Slovakia
The contribution presents a brief characteristic of structural and object models used for development and maintenance of information systems. It also describes utilisation of these models for generation of pedagogic information system IS STUDENT at the Technical University in Košice. It describes possibility of application of UML language (Unified modelling language) in life cycle of pedagogic information system. On practical examples it demonstrates the importance of modelling of such a system
Acridine-decorated cyclometallated gold(III) complexes: synthesis and anti-tumour investigations
(C^N) and (C^N^C) cyclometalated Au(III) represent a highly promising class of potential anticancer agents. We report here the synthesis of seven new cyclometalated Au(III) complexes with five of them bearing an acridine moiety attached via (N^O) or (N^N) chelates, acyclic amino carbenes (AAC) and N-heterocyclic carbenes (NHC). The antiproliferative properties of the different complexes were evaluated in vitro on a panel of cancer cells including leukaemia, lung and breast cancer cells. We observed a trend between the cytotoxicity and the intracellular gold uptake of some representative compounds of the series. Some of the acridine-decorated complexes were demonstrated to interact with ds-DNA using FRET-melting techniques
Synthesis and evaluation of frentizole-based indolyl thiourea analogues as MAO/ABAD inhibitors for Alzheimer’s disease treatment
This work was supported by the Ministry of Health of the Czech Republic (no. NV15-28967A), the Charles University in Prague (SVV 260 291), COST Action CM1103 (STSM 15879 and 17487) and CA15135, University of Hradec Kralove (Faculty of Informatics and Management, project Excellence 2015), University of St Andrews (undergraduate project funding to D.Z.), Biotechnology and Biological Sciences Research Council (BBSRC; no. BB/J01446X/1), the Alzheimer’s Society and the Barcopel Foundation.Alzheimer’s disease (AD) is a neurodegenerative disorder associated with an excessive accumulation of amyloid-beta peptide (Aβ). Based on the multifactorial nature of AD, preparation of multi-target-directed ligands presents a viable option to address more pathological events at one time. A novel class of asymmetrical disubstituted indolyl thioureas have been designed and synthesized to interact with monoamine oxidase (MAO) and/or amyloid-binding alcohol dehydrogenase (ABAD). The design combines the features of known MAO inhibitors scaffolds (e.g. rasagiline or ladostigil) and a frentizole moiety with potential to interact with ABAD. Evaluation against MAO identified several compounds that inhibited in the low to moderate micromolar range. The most promising compound ( 19 ) inhibited human MAO-A and MAOB with IC50 values of 6.34 μM and 0.30 μM, respectively. ABAD activity evaluation did not show any highly potent compound, but the compound series allowed identification of structural features to assist the future development of ABAD inhibitors. Finally, several of the compounds were found to be potent inhibitors of horseradish peroxidase (HRP), preventing the use of the Amplex™ Red assay to detect hydrogen peroxide produced by MAO, highlighting the need for serious precautions when using an enzyme-coupled assay.PostprintPeer reviewe
Perspektywy zastosowania technologii składowania dwutlenku węgla w formacjach geologicznych
The aim of this paper is to show perspectives of using technologies for geological storage of carbon dioxide. Carbon dioxide gets into the atmosphere by increasing energy consumption, mainly by combustion of solid, liquid and gaseous fuels. Most of the emissions are produced from oil, coal and gas. Despite the fact, that carbon dioxide is one of the less harmful gases, it is necessary to consider the problem that may arise by increased production of gas, which can disrupt the balance of the ecosystem on the Earth.Celem artykułu jest przedstawienie perspektyw zastosowania technologii składowania dwutlenku węgla w formacjach geologicznych. Zwiększenie emisji dwutlenku węgla jest spowodowane przede wszystkim rosnącym zużyciem energii, produkowanej głównie w procesach spalania paliw stałych, ciekłych i gazowych. Większość emisji powstaje ze spalania ropy naftowej, węgla oraz gazu ziemnego. Zwiększona produkcja dwutlenku węgla zakłócić bilans ekosystemu Ziemi
Consumer choices of international mountaineering holiday: A perspective of Slovak mountaineering market towards Slovak tourism providers
The main purpose of this study was to critically analyze consumer choices of Slovak mountaineersfor purchasing international mountaineering holiday from Slovak outbound travel agencies/tour-operators. To increase the probability of the respondents’ geographic, age and gender varieties,qualitative questionnaires were distributed among 80 respondents using the method of clustersampling. The preferences of mountaineering holiday arrangement of the analysed market werefound to be through personal communication with Slovak travel intermediaries, which was perceivedmore safe and time-saving then independent purchase or/and purchase through international travelintermediaries. An individually tailored holiday was preferred as it provides safety andsimultaneously satisfies the desired elements of freedom and independence. The main issuesregarding the provided services by the Slovak outbound travel agencies/tour-operators have beenrelated to lack of mountaineering expertise and an inappropriate service delivery.</jats:p
Characterization and Therapeutic Use of Extracellular Vesicles Derived from Platelets
Autologous blood products, such as platelet-rich plasma (PRP), are gaining increasing interest in different fields of regenerative medicine. Although growth factors, the main components of PRP, are thought to stimulate reparation processes, the exact mechanism of action and main effectors of PRP are not fully understood. Plasma contains a high amount of extracellular vesicles (EVs) produced by different cells, including anucleated platelets. Platelet-derived EVs (PL-EVs) are the most abundant type of EVs in circulation. Numerous advantages of PL-EVs, including their ability to be released locally, their ease of travel through the body, their low immunogenicity and tumourigenicity, the modulation of signal transduction as well as the ease with which they can be obtained, has attracted increased attention n. This review focuses briefly on the biological characteristics and isolation methods of PL-EVs, including exosomes derived from platelets (PL-EXOs), and their involvement in the pathology of diseases. Evidence that shows how PL-EVs can be used as a novel tool in medicine, particularly in therapeutic and regenerative medicine, is also discussed in this review.</jats:p
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