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Pregled bibliografske jedinice broj: 44033

Časopis

Autori: Roknić, Saška; Glavaš-Obrovac, Ljubica; Karner, Ivan; Piantanida, Ivo; Žinić, Mladen; Pavelić, Krešimir
Naslov: In vitro cytotoxicity of three 4,9-diazapyrenium hydrogensulfate derivatives on different human tumor cell lines
Izvornik: Chemotherapy (0009-3157) 46 (2000), 2; 143-149
Vrsta rada: članak
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.
Projekt / tema: 00980703, 00981104, 127009
Izvorni jezik: ENG
Rad je indeksiran u
bazama podataka:
Current Contents Connect (CCC)
MEDLINE
Scopus
SCI-EXP, SSCI i/ili A&HCI
Science Citation Index Expanded (SCI-EXP) (sastavni dio Web of Science Core Collectiona)
Kategorija: Znanstveni
Znanstvena područja:
Kemija
URL cjelovitog teksta:
Google Scholar: In vitro cytotoxicity of three 4,9-diazapyrenium hydrogensulfate derivatives on different human tumor cell lines



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