Abstract

VORSTER, Chris  and  JOUBERT, Annie. In vitro effects of 2-methoxyestradiol-bis-sulphamate on cell growth, morphology and cell cycle dynamics in the MCF-7 breast adenocarcinoma cell line. Biocell [online]. 2010, vol.34, n.2, pp.71-79. ISSN 0327-9545.

In the search for new and improved anticancer therapies, researchers have identified several potentially useful compounds. One of these agents is 2-methoxyestradiol-bis-sulphamate (2ME-BM), a sulphamoylated derivative of 2-methoxyestradiol. The objective of this study was to evaluate 2ME-BM's in vitro efficacy as antiproliferative agent in the MCF-7 breast adenocarcinoma cell line. Light- and fluorescent microscopy showed decreased cell density, increased apoptotic characteristics and significant ultrastructural aberrations indicative of autophagic cell death after 24 hours of exposure at a concentration of 0.4µM. In addition, mitotic indices revealed that 2ME-BM induces a G₂M block. The latter was confirmed by flow cytometric analyses where increased sub-G₁ and G₂/M fractions, as well as an increase in cyclin B1 levels were observed. Further in vitro research into the mechanism of this potentially useful anticancer compound is thus warranted.

Keywords : Cancer; 2-methoxyestradiol; Sulphamoylated estradiol derivative; Apoptosis; Autophagy.

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