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Pregled bibliografske jedinice broj: 44033

In vitro cytotoxicity of three 4,9-diazapyrenium hydrogensulfate derivatives on different human tumor cell lines


Roknić, Saška; Glavaš-Obrovac, Ljubica; Karner, Ivan; Piantanida, Ivo; Žinić, Mladen; Pavelić, Krešimir
In vitro cytotoxicity of three 4,9-diazapyrenium hydrogensulfate derivatives on different human tumor cell lines // Chemotherapy, 46 (2000), 2; 143-149 (međunarodna recenzija, članak, znanstveni)


Naslov
In vitro cytotoxicity of three 4,9-diazapyrenium hydrogensulfate derivatives on different human tumor cell lines

Autori
Roknić, Saška ; Glavaš-Obrovac, Ljubica ; Karner, Ivan ; Piantanida, Ivo ; Žinić, Mladen ; Pavelić, Krešimir

Izvornik
Chemotherapy (0009-3157) 46 (2000), 2; 143-149

Vrsta, podvrsta i kategorija rada
Radovi u časopisima, članak, znanstveni

Ključne riječi
4;9-Diazapyrenium hydrogensulfate; Tumor cells; Antitumor activity

Sažetak
DNA intercalating agents interfere with DNA’s role as a template in replication and transcription by inserting of intercalator molecule between adjacent base-pairs. We have synthesized three potential novel intercalators, 4,9-diazapyrenium hydrogensulphate derivatives: 5,10-diphenyl-4,9-dimethyl-4,9-diazapyrenium hydrogensulphate (FDAP), 4,9-dimethyl-4,9-diazapyrenium hydrogensulphate (GDAP) and 2,4,7,9-tetramethyl-4,9-diazapyrenium hydrogensulphate (MDAP) and tested for their biological effects in vitro on four human tumor cell lines (SKBr3 - breast carcinoma, HeLa - cervical carcinoma, CaCo2 - colon carcinoma and SW620 - poorly differentiated cells from lymph node metastasis of colon carcinoma). Cytotoxic effects on cell growth and viability were determined using tetrazolium dye (MTT) assay. DNA synthesis and proliferation of treated cells were studied by [3H]-thymidine incorporation test. DNA fragmentation was analysed by agarose gel electrophoresis. Growth inhibitory effect was cell-specific and dose-dependent. The most pronounced antiproliferative effect was observed on SKBr3 cells for FDAP (10-5 M) 91.8%, for MDAP (10-5 M) 85.3% and on SW620 cells for GDAP (10-5 M) 65.3%. The DNA-ladder fragmentation of treated HeLa and SKBr3 cells, as hallmark of apoptosis, was observed. Based on specific DNA fragmentation, morphological changes (reduced cell volume, round cell shape, condensed chromatin) and growth inhibition of treated human tumor cells we conclude that tested substances induced apoptotic cell death.

Izvorni jezik
Engleski

Znanstvena područja
Kemija



POVEZANOST RADA


Projekt / tema
00980703
00981104
127009

Ustanove
Institut "Ruđer Bošković", Zagreb,
Klinički bolnički centar Osijek

Časopis indeksira:


  • Current Contents Connect (CCC)
  • Web of Science Core Collection (WoSCC)
    • Science Citation Index Expanded (SCI-EXP)
    • SCI-EXP, SSCI i/ili A&HCI
  • Scopus
  • MEDLINE


Uključenost u ostale bibliografske baze podataka:


  • Biological Abstracts