Chemotherapy is one of the main strategies for reducing the rate of
cancer progression or, in some cases, curing the tumour. Since a great number of chemotherapeutic agents are cytotoxic compounds, i. e. similarly affect normal and neoplastic cells, application of antitumour drugs is preferred in
cancer management and
therapy. In this study, the cytotoxicity of
diversin was evaluated in 5637 cells, a
transitional cell carcinoma (TCC) subline (bladder
carcinoma), and normal human fibroblast cells using the
3-(4,5-dimethyl-2-thiazolyl)-2,5-diphenyl-2H-tetrazolium bromide (MTT) assay.
Chromatin condensation and DNA damage induced by
diversin were also determined by means of
4',6-diamidino-2-phenylindole (
DAPI) staining and the comet assay, respectively. In addition, the mechanism of action of
diversin was studied in more detail by the
caspase 3 colourimetric assay and flow cytometry-based cell-cycle analyses (PI staining). Our results revealed that
diversin has considerable cytotoxic effects in 5637 cells, but not on HFF3 (human foreskin fibroblast) and HDF1 (human dermal fibroblast) cells. Further studies showed that
diversin exerts its cytotoxicity via induction of
chromatin condensation, DNA damage, and activation of
caspase 3 in 5637 cells. In addition, flow cytometric analyses revealed that 5637 cells are mostly arrested at the G2 phase of the cell cycle in the presence of
diversin.