| Summary: | <p>Abstract</p> <p>Background</p> <p>In the search for anticancer agents, a promising 17-β-estradiol metabolite, 2-methoxyestradiol (2ME2) was found that exerts antiproliferative <it>in vitro </it>and <it>in vivo </it>activity. Since 2ME2 has limited biological accessibility and rapid metabolic degradation, the purpose of this study was to investigate the <it>in vitro </it>influence exerted by an analogue of 2ME2 namely 2-methoxyestradiol-bis-sulphamate (2MEBM) in a breast adenocarcinoma cell line (MCF-7).</p> <p>Methods</p> <p>This was conducted by investigating 2MEBM's <it>in vitro </it>influence on cell cycle progression, mitochondrial membrane potential and possible production of reactive oxygen species (ROS) generation. <it>In vitro </it>effects of 2MEBM on cell cycle progression was demonstrated by means of flow cytometry using propidium iodide. Hydrogen peroxide and superoxide production was investigated using 2,7-dichlorofluorescein diacetate and hydroethidine, respectively. The probable reduction in the mitochondrial membrane potential was demonstrated using a MitoCapture™ kit.</p> <p>Results</p> <p>Cell cycle progression revealed the presence of a sub-G<sub>1 </sub>apoptotic peak. Reduction of mitochondrial membrane potential after exposure to 2MEBM was demonstrated and an increase in ROS production was also observed.</p> <p>Conclusion</p> <p>This study verified that 2MEBM exposure resulted in apoptosis induction, increased ROS production and reduced mitochondrial membrane potential in a tumorigenic breast epithelial cell line. Data obtained from this project contributes to the unravelling of the <it>in vitro </it>signal transduction of 2MEBM in tumorigenic cell lines.</p>
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