Pregled bibliografske jedinice broj: 88495
4,9-Diazapyrenium derivatives as inducers of apoptosis and topoisomerase II poisons
4,9-Diazapyrenium derivatives as inducers of apoptosis and topoisomerase II poisons // Apoptosis 2003; From signaling pathways to therapeutic tools / Marc Diederich (ur.).
Luxembourg, 2003. str. 275-275 (poster, međunarodna recenzija, sažetak, znanstveni)
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Naslov
4,9-Diazapyrenium derivatives as inducers of apoptosis and topoisomerase II poisons
Autori
Marczi, Saška ; Glavaš-Obrovac, Ljubica ; Karner, Ivan
Vrsta, podvrsta i kategorija rada
Sažeci sa skupova, sažetak, znanstveni
Izvornik
Apoptosis 2003; From signaling pathways to therapeutic tools
/ Marc Diederich - Luxembourg, 2003, 275-275
Skup
Apoptosis 2003; From signaling pathways to therapeutic tools
Mjesto i datum
Luksemburg, 29.01.2003. - 01.02.2003
Vrsta sudjelovanja
Poster
Vrsta recenzije
Međunarodna recenzija
Ključne riječi
4;9-Diazapyrenium derivatives; topoisomerase II
Sažetak
4,9-Diazapyrenium derivatives (BzDAP, FDAP, GDAP, JDAP, MDAP, m-MOST, p-MOST) are synthetic compounds acting on DNA level by double strand DNA intercalation between adjacent base pairs. Recently studied 4,9-diazapyrenium derivatives (FDAP, GDAP and MDAP) showed antitumor activity against human malignant cell lines MIA PaCa-2, Hep-2, SKBr3, HeLa and SW620. Morpholigical changes and ladder DNA fragmentation indicated apoptosis as mode of cell death. The main objective of this study was to determine whether the FDAP, GDAP and m-MOST induce apoptosis in human tumor MIA PaCa-2 and Caco-2 cells, and to determine whether the all seven 4,9-diazapyrenium derivatives stimulate topoisomerase II-mediated DNA cleavage. For detection of phosphatydilserine exposure from interior side of plasma membrane to the outher leaflet Annexin-V-fluorescein was used. In situ detection of DNA fragmentation was analyzed by TUNEL method. For screening of topisomerase II-targeted effects of 4,9-diazapyrenium derivatives the cell-free assay was used. Strategy was based on alterations of electrophoretic mobility of pBR322 plasmid DNA due to connected action of Drosophila melanogaster topisomerase II and tested intercalative compounds. The results of phosphatidylserine exposure and DNA fragmentation investigations indicated apoptosis as mode of treated tumor cell's death. Examination of mechanism of action of 4,9-diazapyrenium derivatives showed that tested compounds stimulate topoisomerase II-mediated DNA-cleavage. Hence, 4,9-diazapyrenium derivatives can be considered as topoisomerase II poisons.
Izvorni jezik
Engleski
Znanstvena područja
Kliničke medicinske znanosti
