Abstract:
Recent findings revealed that 2-ethyl-17-oxoestra-1,3,5(10)-trien-3-yl sulfamate (ESE-one)
induces antiproliferative activity and cell rounding dependent on the generation of superoxide anion,
hydrogen peroxide and peroxyl radical. In the current study, the role of these reactive oxygen species
was assessed in the activity exerted by ESE-one on cell cycle progression, mitochondrial membrane
potential and cell death induction in breast tumorigenic cells. The influence of ESE-one was also
investigated on superoxide dismutase and catalase activity. ESE-one induced a time-dependent
accumulation of cells in the G1 phase and G2/M phase that is partially impaired by tiron and
trolox and N,N0-dimethylthiourea suggesting that superoxide anion, hydrogen peroxide and peroxyl
radical are required for these effects exerted by ESE-one. Flow cytometry data in MCF-7 cells
demonstrated that tiron decreased depolarization of the membrane potential in ESE-one exposed
cells, indicating that superoxide anion plays a role in the depolarization effects induced by ESE-one.
Spectrophotometry data showed that ESE-one decreased catalase activity in both cell lines. This study
contributes towards pertinent information regarding the effects of an in silico-designed sulfamoylated
compound on antioxidant enzymes leading to aberrant quantities of specific reactive oxygen species
resulting in antimitotic activity culminating in the induction of cell death in breast cancer cell lines.
