3 research outputs found

    PROSPECTIVE BIOLOGICAL ACTIVE COMPOUNDS AMONG 7-SUBSTITUTED OF 3-BENZYL-8-PROPYLXANTHINES FOR TREATMENT OF METABOLIC SYNDROME PATHOLOGIES

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    Aim â€“ the search for biologically active compounds with diuretic and hypoglycemic action among 7-substituted of 3-benzyl-8-propylxanthines, which can be used for the treatment of pathologies of “metabolic syndrome”. Materials and methods. 30 new chemical compounds among derivatives of 7-substituted of 3-benzyl-8-propylxanthines by PASS prediction filter were chosen for diuretic and hypoglycemic activity researches. Diuretic, hypoglycemic activity and for the most active compounds – the acute toxicity were studied in vivo. The molecular docking, which is based on EADock DSS mechanism of the modulation displayed the interaction between some of functional groups inside discovered xanthine ligands and known receptors and enzymes presented in Ligand-protein Database of Swiss Institute of Bioinformatics. Results. It has been shown that synthesized compounds displayed strong diuretic and medium hypoglycemic activities. The molecular docking modulation (SwissDock) of interaction of xanthine derivatives hits with proposed receptors and enzymes revealed prospective of using 7-substituted of 3-benzyl-8-propylxanthines as potential drugs for treatment of metabolic syndrome pathologies. Conclusion. The diuretic activity of the new 23 compounds of 7-substituted of 3-benzyl-8-propylxanthines and hypoglycemic activity of the new 7 derivatives of 7-substituted of 3-benzyl-8-propylxanthines was studied. Results of performed investigation illustrate that 7-substituted of 3-benzyl-8-propylxanthines demonstrate biological activity comparable to standard drugs. We also proposed probable molecular targets for the most active compounds by molecular docking method. It was shown that derivatives of 7-substituted of 3-benzyl-8-propylxanthines can be used for metabolic syndrome disorders prevention

    PROSPECTIVE BIOLOGICAL ACTIVE COMPOUNDS AMONG 7-SUBSTITUTED OF 3-BENZYL-8-PROPYLXANTHINES FOR TREATMENT OF METABOLIC SYNDROME PATHOLOGIES

    Get PDF
    Aim â€“ the search for biologically active compounds with diuretic and hypoglycemic action among 7-substituted of 3-benzyl-8-propylxanthines, which can be used for the treatment of pathologies of “metabolic syndrome”. Materials and methods. 30 new chemical compounds among derivatives of 7-substituted of 3-benzyl-8-propylxanthines by PASS prediction filter were chosen for diuretic and hypoglycemic activity researches. Diuretic, hypoglycemic activity and for the most active compounds – the acute toxicity were studied in vivo. The molecular docking, which is based on EADock DSS mechanism of the modulation displayed the interaction between some of functional groups inside discovered xanthine ligands and known receptors and enzymes presented in Ligand-protein Database of Swiss Institute of Bioinformatics. Results. It has been shown that synthesized compounds displayed strong diuretic and medium hypoglycemic activities. The molecular docking modulation (SwissDock) of interaction of xanthine derivatives hits with proposed receptors and enzymes revealed prospective of using 7-substituted of 3-benzyl-8-propylxanthines as potential drugs for treatment of metabolic syndrome pathologies. Conclusion. The diuretic activity of the new 23 compounds of 7-substituted of 3-benzyl-8-propylxanthines and hypoglycemic activity of the new 7 derivatives of 7-substituted of 3-benzyl-8-propylxanthines was studied. Results of performed investigation illustrate that 7-substituted of 3-benzyl-8-propylxanthines demonstrate biological activity comparable to standard drugs. We also proposed probable molecular targets for the most active compounds by molecular docking method. It was shown that derivatives of 7-substituted of 3-benzyl-8-propylxanthines can be used for metabolic syndrome disorders prevention

    Metaphor and gender in discourse on climate change

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    Die Metapher als kognitives Phänomen ist in verschiedenen Diskursen ausführlich untersucht worden. Der Rolle des Geschlechts bei der Bildung von Metaphern wurde jedoch nicht genügend Aufmerksamkeit geschenkt. Ziel dieser Studie war es, die Faktoren zu untersuchen, die die Verwendung von Metaphern im Diskurs über den Klimawandel bestimmen. Insbesondere wird analysiert, ob Faktoren wie Geschlecht und politische Orientierung die Wahl der Quellenbereiche beeinflussen, in denen auf den Klimawandel Bezug genommen wird. Meinungsartikel aus drei britischen Online-Zeitungen mit unterschiedlicher politischer Orientierung wurden im Hinblick auf sprachliche und konzeptuelle Metaphern analysiert, die zur Beschreibung des Klimawandels verwendet werden. Für die Analysen wurde eine Kombination aus kognitiven und datenbasierten korpuslinguistischen Ansätzen angewandt. Die Ergebnisse legten nahe, dass es Unterschiede in der Art und Weise gibt, wie die vorherrschenden konzeptuellen Metaphern von Frauen und Männern verwendet werden. Insbesondere bei der Wahl der sprachlichen Metaphern zeigten sich die größten Unterschiede. Die Analyse der verwendeten Metaphern in unterschiedlichen Zeitungen, zeigte signifikante Unterschiede in den Präferenzen bestimmter Quellbereiche. Diese Arbeit fördert das Verständnis der Art und Weise, wie konzeptuelle Metaphern den Diskurs über den Klimawandel prägen. Darüber hinaus zeigte sie, wie kognitive und Diskursansätze kombiniert werden können, um Gender und politische Zugehörigkeit als Einflussfaktoren für die Wahl von Metaphern im Zusammenhang mit dem Klimawandel, zu analysieren.Metaphor as a cognitive phenomenon has been extensively investigated in different discourses. However, the role of gender in production of metaphor has received insufficient attention. This study aimed to investigate the factors that determine metaphor use in the discourse on climate change. Specifically, it analyses whether such factors as gender and political orientation influence the choice of source domains to refer to climate change. Opinion articles from three online British newspapers with different political orientation were analysed with regard to linguistic and conceptual metaphor employed to describe climate change. The combination of cognitive and discourse corpus-based approaches was implemented for the analyses. The results suggested that there are differences in the way prevailing conceptual metaphors were used by women and men. However, investigation of a more specific level, the linguistic metaphors, demonstrated a wider gap concerning the choice of metaphors. Regarding the results obtained in the comparative analysis of metaphors employed in different newspapers, it can be argued that there are significant differences in the preferences of particular source domains between the media under investigation. This research provided an important opportunity to advance the understanding of the way conceptual metaphor frame the climate change discourse. Moreover, it demonstrated the way cognitive and discourse approaches can be applied to explore factors, like gender and political affiliation, that can influence the choice of metaphors for climate change
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