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Background  2-Methoxyestradiol is known to have antitumour and antiproliferative action  in vitro  and  in vivo . However, when 2-methoxyestradiol is orally administered, it is rapidly oxidized by the enzyme 17Î²-hydroxysteriod dehydrogenase in the gastrointestinal tract. Therefore, 2-methoxyestradiol never reaches high enough concentrations in the tissue to be able to exert these antitumour properties. This resulted in the  in silico -design of 2-methoxyestradiol analogues in collaboration with the Bioinformatics and Computational Biology Unit (UP) and subsequent synthesis by iThemba Pharmaceuticals (Pty) Ltd (Modderfontein, Midrand, South Africa). One such a novelty-designed analogue is 2-ethyl-3- O -sulphamoyl-estra-1, 3, 5(10)16-tetraene (ESE-16).    Methods  This pilot study aimed to determine the morphological effect and possible generation of reactive oxygen species by ESE-16 on erythrocytes and platelet samples (with and without added thrombin) by means of scanning electron microscopy, transmission electron microscopy and flow cytometry.    Results  Erythrocytes and platelets were exposed to ESE-16 at a concentration of 180nM for 24Â hours. Scanning- and transmission electron microscopy indicated that ESE-16 did not cause changes to erythrocytes, platelets or fibrin networks. Flow cytometry measurements of hydrogen peroxide and superoxide indicated that ESE-16 does not cause an increase in the generation of reactive oxygen species in these blood samples.    Conclusion  Further  in vivo  research is warranted to determine whether this novel  in silico -designed analogue may impact on development of future chemotherapeutic agents and whether it could be considered as an antitumour agent.

cancer cell international

An estrogen analogue and promising anticancer agent refrains from inducing morphological damage and reactive oxygen species generation in erythrocytes, fibrin and platelets: a pilot study