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2,4-dibencilaminoquinazoline induced apoptosis in three human cancer cell lines

ABSTRACT: In the search of new symmetrical derivatives with anticancer activity, we have looked for novel compounds able to induce a selective proapoptotic mechanism in cancer cells. The potential antitumoral activity of several quinazoline derivatives was evaluated in vitro examining their cytotoxic effects against human breast (HTB26), colon (HT29) and bladder (T24) cancer cell lines. Non-tumoral human cell lines were used to test the selectivity of the cytotoxic compounds against cancer cells. Several compounds showed selectivity for cancer cell lines; among them, 2,4-dibencilaminoquinazoline was chosen as the best candidate and its mechanism of action was studied in more detail. This compound was tested for its ability to induce caspase-3 activation and nuclear chromatin degradation in the three cancer cell lines. A time dependent evaluation of apoptosis was performed in the three cancer cell lines, including an expression microarray study at the points of caspase activation and chromatin degradation. 2,4-dibencilaminoquinazoline treatment produces few changes in the expression of genes as evaluated by using microarrays and RT-PCR assays. In conclusion, 2,4-di-p-bromofenilaminoquinazoline is a promising anticancer drug showing cytostatic and apoptotic effects mainly in a transcription independent manner. Keywords: Apoptosis induction, time course

ORGANISM(S): Homo sapiens

PROVIDER: GSE3329 | GEO | 2005/09/21

SECONDARY ACCESSION(S): PRJNA93231

REPOSITORIES: GEO

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Project description:Carica papaya leaf decoction, an Australian Aboriginal remedy, has been used widely for its healing capabilities against cancer, with numerous anecdotal reports. In this study we investigated its in vitro cytotoxicity on human squamous cell carcinoma cells followed by metabolomic profiling of Carica papaya leaf decoction and leaf juice/brewed leaf juice to determine the effects imparted by the long heating process typical of the Aboriginal remedy preparation. MTT assay results showed that in comparison with the decoction, the leaf juice not only exhibited a stronger cytotoxic effect on SCC25 cancer cells, but also produced a significant cancer-selective effect as shown by tests on non-cancerous human keratinocyte HaCaT cells. Furthermore, evidence from testing brewed leaf juice on these two cell lines suggested that the brewing process markedly reduced the selective effect of Carica papaya leaf on SCC25 cancer cells. To tentatively identify the compounds that contribute to the distinct selective anticancer activity of leaf juice, an untargeted metabolomic approach employing Ultra High Performance Liquid Chromatography-Quadrupole Time of Flight- Mass Spectrometry followed by multivariate data analysis was applied. Some 90 and 104 peaks in positive and negative mode respectively were selected as discriminatory features from the chemical profile of leaf juice and >1500 putative compound IDs were obtained via database searching. Direct comparison of chromatographic and tandem mass spectral data to available reference compounds confirmed one feature as a match with its proposed authentic standard, namely pheophorbide A. However, despite pheophorbide A exhibiting cytotoxic activity on SCC25 cancer cells, it did not prove to be the compound contributing principally to the selective activity of leaf juice. With promising results suggesting stronger and more selective anticancer effects when compared to the Aboriginal remedy, Carica papaya leaf juice warrants further study to explore its activity on other cancer cell lines, as well as investigation to confirm the identity of compounds contributing to its selective effect, particularly those compounds altered by the long heating process applied during the traditional Aboriginal remedy preparation.

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2,4-dibencilaminoquinazoline induced apoptosis in three human cancer cell lines

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