The in vitro effects of a sulphamoylated derivative of 2-methoxyestradiol on cell number, morphology and alpha-tubulin disruption in cervical adenocarcinoma (HeLa) cells

Abstract

2-Methoxyestradiol (2ME2) is an endogenous metabolite of estrogen that has both antiangiogenic and antitumor effects. However, the shortcoming with 2ME2 is that it is rapidly inactivated by 17β-hydroxysteroid dehydrogenase type 2. Thus a bis-sulphamoylated derivative of 2ME2, 2-Methoxyestradiol-bis-sulphamate (2MEBM) was synthesized in order to address the shortcoming of 2ME2. The aim of this in vitro study was to investigate the influence of 2MEBM on cell growth, morphology and tubulin structure in a cervical cancer (HeLa) cell line. Dose-dependent studies revealed that 0.55μM of 2MEBM inhibited cell growth by 50%. 2MEBM-treated cells showed an increase in the number of metaphase cells, apoptotic cells, and disrupted tubulin structure after 48 hours of exposure to 0.55μM of 2MEBM. Future studies will be conducted to further investigate the mechanism of action of 2MEBM in cervical carcinoma cells.