Article ID Journal Published Year Pages File Type
5860989 Toxicology in Vitro 2016 10 Pages PDF
Abstract

•Selenadiazoloquinolone E2h is a new potent photosensitizer.•E2h inhibited the growth of HeLa cells and induced S and G2/M arrest and apoptosis.•UVA irradiation (dose 0.359 J cm− 2) increased derivative cytotoxicity.•Changes in ROS level, mitochondrial potential and caspase 3 activity were found.

7- ethyl 9-ethyl-6-oxo-6,9-dihydro[1,2,5]selenadiazolo [3,4-h]quinoline-7-carboxylate (E2h) is a new synthetically prepared quinolone derivative, which in our primary study showed cytotoxic effects towards tumor cells. The aim of the present study was to examine the antiproliferative and apoptosis inducing activities of E2h towards human cervical cancer cell line HeLa with/without the presence of UVA irradiation. Further, the molecular mechanism involved in E2h-induced apoptosis in HeLa cells was investigated. Our results showed that both non-photoactivated and photoactivated E2h caused morphological changes and inhibited the cell growth of HeLa cells in a time- and dose-dependent manner. Irradiation increased the sensitivity of HeLa cells to E2h. Quinolone induced S and G2/M arrest and apoptosis in HeLa cells, as characterized by DNA fragmentation and flow cytometry. In addition, E2h elevated the level of reactive oxygen species and activated caspases 3. In conclusions, E2h alone/in combination with UVA irradiation induced apoptosis in HeLa cells through the ROS-mitochondrial/caspase 3-dependent pathway.

Graphical abstractProposed model of molecular mechanism of selenadizoloquinolone-induced apoptotic death in HeLa cellsDownload full-size image

Related Topics
Life Sciences Environmental Science Health, Toxicology and Mutagenesis
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