Skip to content
Home
About Us
Resources
Profiles Metrics
Authors Directory
Institutions Directory
Top Authors
Top Institutions
Top Sponsors
AI Digest
Contact Us
Menu
Home
About Us
Resources
Profiles Metrics
Authors Directory
Institutions Directory
Top Authors
Top Institutions
Top Sponsors
AI Digest
Contact Us
Home
About Us
Resources
Profiles Metrics
Authors Directory
Institutions Directory
Top Authors
Top Institutions
Top Sponsors
AI Digest
Contact Us
Menu
Home
About Us
Resources
Profiles Metrics
Authors Directory
Institutions Directory
Top Authors
Top Institutions
Top Sponsors
AI Digest
Contact Us
Publication Details
AFRICAN RESEARCH NEXUS
SHINING A SPOTLIGHT ON AFRICAN RESEARCH
Sulphamoylated 2-Methoxyestradiol Analogues Induce Apoptosis in Adenocarcinoma Cell Lines
PLoS ONE, Volume 8, No. 9, Article e71935, Year 2013
Notification
URL copied to clipboard!
Description
2-Methoxyestradiol (2ME2) is a naturally occurring estradiol metabolite which possesses antiproliferative, antiangiogenic and antitumor properties. However, due to its limited biological accessibility, synthetic analogues have been synthesized and tested in attempt to develop drugs with improved oral bioavailability and efficacy. The aim of this study was to evaluate the antiproliferative effects of three novel in silico-designed sulphamoylated 2ME2 analogues on the HeLa cervical adenocarcinoma cell line and estrogen receptor-negative breast adenocarcinoma MDA-MB-231 cells. A dose-dependent study (0.1-25 μM) was conducted with an exposure time of 24 hours. Results obtained from crystal violet staining indicated that 0.5 μM of all 3 compounds reduced the number of cells to 50%. Lactate dehydrogenase assay was used to assess cytotoxicity, while the mitotracker mitochondrial assay and caspase-6 and -8 activity assays were used to investigate the possible occurrence of apoptosis. Tubulin polymerization assays were conducted to evaluate the influence of these sulphamoylated 2ME2 analogues on tubulin dynamics. Double immunofluorescence microscopy using labeled antibodies specific to tyrosinate and detyrosinated tubulin was conducted to assess the effect of the 2ME2 analogues on tubulin dynamics. An insignificant increase in the level of lactate dehydrogenase release was observed in the compounds-treated cells. These sulphamoylated compounds caused a reduction in mitochondrial membrane potential, cytochrome c release and caspase 3 activation indicating apoptosis induction by means of the intrinsic pathway in HeLa and MDA-MB-231 cells. Microtubule depolymerization was observed after exposure to these three sulphamoylated analogues. © 2013 Visagie et al.
Authors & Co-Authors
Visagie, Michelle Helen
South Africa, Pretoria
University of Pretoria
Mercier, Anne Elisabeth
South Africa, Pretoria
University of Pretoria
Mqoco, Thandi
South Africa, Pretoria
University of Pretoria
Vieira, Warren Antonio
South Africa, Pretoria
University of Pretoria
Prudent, Renaud
France, La Tronche
Albert Bonniot Institute Iab: Ontogenesis and Molecular Oncogenesis
Martinez, Anne
France, La Tronche
Albert Bonniot Institute Iab: Ontogenesis and Molecular Oncogenesis
Lafanechère, Laurence
France, La Tronche
Albert Bonniot Institute Iab: Ontogenesis and Molecular Oncogenesis
Joubert, Anna Margaretha
South Africa, Pretoria
University of Pretoria
Statistics
Citations: 24
Authors: 8
Affiliations: 2
Identifiers
Doi:
10.1371/journal.pone.0071935
e-ISSN:
19326203
Research Areas
Cancer
Health System And Policy