Mar 24, 2018

The in vitro effects of a novel estradiol analog on cell proliferation and morphology in human epithelial cervical carcinoma

Cellular & Molecular Biology Letters
Laura Susan BoydAnna Margaretha Joubert

Abstract

The majority of novel chemotherapeutics target the cell cycle, aiming to effect arrest and cause apoptosis. One such agent, 2-methoxyestradiol (2ME), has been shown to possess anticancer properties against numerous cancer types, both in vitro and in vivo. Despite its promise, 2ME has exhibited limitations, including low oral bioavailability and rapid hepatic enzymatic inactivation in vivo. A novel sulphamoylated estrogen analog, 2-ethyl-3-O-sulphamoyl-estra-1,3,5(10)16-tetraene (ESE-16), was in silico-designed in our laboratory to overcome these issues. It was then synthesized by a pharmaceutical company and used in an in vitro antiproliferative effect study on a human cervical carcinoma (HeLa) cell line. Cell proliferation data obtained from the crystal violet assay and real-time cell analysis demonstrated that 0.2 μM of ESE-16 had a significant inhibitory effect on the HeLa cells 24 h post-exposure. Immunofluorescence showed that ESE-16 is a microtubule disruptor that causes cells to undergo a mitotic block. Qualitative morphological studies using polarization-optical transmitted light differential interference contrast (PlasDIC) and light microscopy revealed a decrease in cell density and an increase in the number of cells a...Continue Reading

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Mentioned in this Paper

Cell Cycle Progression
Study
In Vivo
Flow Cytometry
Immunofluorescence Assay
Antineoplastic Agents
Research
Endocrine Disruptors
Exertion
Apoptosis, Intrinsic Pathway

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