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Korelacija bioloških aktivnosti sintetisanih derivata 4-hidroksikumarina i njihovih fizičko-hemijskih parametara

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2011
Disertacija.pdf (9.626Mb)
Author
Mladenović, Milan
Mentor
Solujić, Slavica
Committee members
Mihailović, Mirjana
Vrvić, Miroslav
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Abstract
Serija od sedamnaest derivata 4-hidroksikumarina, supstituisanih u položaju 3 polarnim funkcionalnim grupama, testirani su kao antimikrobni, antioksidativni i antikoagulativni agensi. Antimikrobna aktivnost testiranih derivata 1-10s određena je dilucionom metodom u in vitro uslovima pri čemu su derivati pokazali umerenu aktivnost. Antioksidativna aktivnost in vitro derivata 1-10s određena je konstatovanjem totalnog antioksidativnog kapaciteta, sposobnosti neutralizacije DPPH, peroksidnog i hidroksi radikala i helatizacionog kapaciteta testiranih agenasa, pri čemu su svi derivati pokazali izrazitu antioksidativnu aktivnost. Antikoagulativna aktivnost in vivo derivata 1-10s ispitivana je nakon intraperitonealne aplikacije derivata na laboratorijskim pacovima Wistar soja i merenjem protrombinskog vremena. Derivati 1-10s pokazali su odličnu antikoagulativnu aktivnost nakon višednevne aplikacije, nisu izazvali inflamaciju niti promene na jetri životinja.
The series of seventeen 4-hydroxycoumarin derivatives, substituted at C-3 position with high polar scaffolds, were evaluated as antimicrobial, antioxidant and anticoagulant agents. The in vitro antimicrobial activity of compounds 1-10с was determined using the dilution method. During the evaluation of antimicrobial activity, coumarin derivatives showed moderate potential. The compounds 1-10с antioxidant activity in vitro was determined using Total antioxidant capacity assay, DPPH radical scavenging assay, Lipid peroxidation in linoleic acid emulsion inhibition assay, Hydroxyl radical scavenging activity assay and Ferrous ion chelating ability assay. During the evaluation of antioxidant activity, coumarin derivatives presented excellent activity. The anticoagulant activity in vivo was evaluated after the continuous intraperitoneal administration of compounds 1-10с to adult Albino Wistar rats and by measuring the prothrombin time. Administrated compounds presented excellent anticoagulant... activity and induced no inflammation or change to the animal liver.

Faculty:
University of Kragujevac, Faculty of Science
Date:
28-12-2011
Projects:
  • Simultaneous Bioremediation and Soilification of Degraded Areas to Preserve Natural Resources of Biologically Active Substances, and Development and Production of Biomaterials and Dietetic Products (RS-43004)
Keywords:
Kumarin / Hidroksikumarin
[ Google Scholar ]
URI
http://eteze.kg.ac.rs/application/showtheses?thesesId=309
http://nardus.mpn.gov.rs/handle/123456789/3576
https://fedorakg.kg.ac.rs/fedora/get/o:222/bdef:Content/download

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