2-Methoxyestradiol – a unique blend of activities generating a new class of anti-tumour/anti-inflammatory agents

Sutherland, Tara E.; Anderson, Robin L.; Hughes, Richard A.; Altmann, Emile; Schuliga, Michael; Ziogas, James; Stewart, Alastair G.

doi:10.1016/j.drudis.2007.05.005

Cited by 77 publications

(75 citation statements)

References 48 publications

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“…Because of its potent antiangiogenic, antiproliferative and cytotoxic capacities, it is now under clinical evaluation as a new cancer therapeutic (see Table 1). 147 The ROS-generating capacities of 2ME reside in its potential to inhibit both the mitochondrial respiratory chain, resulting in the release of superoxide, 148 and SOD, the detoxifing enzyme for this ROS (Fig. 3B).…”

Section: Sod Catalase and Gsh Reductase Mimeticmentioning

confidence: 99%

ROS-mediated mechanisms of autophagy stimulation and their relevance in cancer therapy

Dewaele¹,

Maes²,

Agostinis³

2010

Autophagy

275

199

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Section: Sod Catalase and Gsh Reductase Mimeticmentioning

confidence: 99%

ROS-mediated mechanisms of autophagy stimulation and their relevance in cancer therapy

Dewaele¹,

Maes²,

Agostinis³

2010

Autophagy

275

199

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“…The 2-methoxyestradiol (2-ME), formerly regarded as an inactive metabolite of 17β-estradiol, is now known to be an antitumor agent in some animal models of solid tumor, by its antiangiogenic effect and antiproliferative effect (Sutherland et al, 2007;Wang et al, 2011). The 2-ME is currently being evaluated in Phase II clinical trials for the treatment of solid tumors, such as breast cancer (Dahut et al, 2006;Jehana et al, 2006).…”

Section: Introductionmentioning

confidence: 99%

Preparation and cytotoxicity of poly (DL-lactide-co-glycolide) microspheres encapsulating 2-methoxyestradiol

et al. 2012

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“…Presently, phase II clinical trials for 2ME2 (Panzem ® ) are being conducted for multiple myeloma [6], ovarian cancer [7], glioblastoma multiforme [8], breast-and prostate cancer [9]. Due to the limited biological availability and rapid metabolic breakdown of 2ME2 several promising analogues of 2ME2 have been developed in recent years.…”

mentioning

confidence: 99%

2-Methoxyestradiol-bis-sulfamate induces apoptosis and autophagy in a tumorigenic breast epithelial cell line

Visagie

Joubert

2011

Mol Cell Biochem

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In anticancer research where the focus is on finding agents that induces cell death while leaving nontumorigenic cells less affected, a novel 2-methoxyestradiol derivative has come forth. 2-Methoxyestradiol-bissulphamate (2-MeOE2bisMATE) is a 2-methoxyestradiol derivative produced by bis-sulphamoylation which possesses increased antiproliferative activity and biological availability. Several questions remain regarding the the type of cell death mechanisms and possible induction of autophagy by 2-MeOE2bisMATE. The aim of this in vitro study was to investigate the cell death mechanisms exerted by 2-MeOE2bisMATE in an adenocarcinoma cell line (MCF-7) by analyzing its influence on cell growth, morphology and possible induction of cell death. Spectrophotometry (crystal violet staining), transmission electron microscopy (TEM), light microscopy (haematoxylin and eosin staining) and fluorescent microscopy (Hoechst 33342, propidium iodide and acridine orange) were employed. Spectrophotometrical studies indicated that 2-MeOE2bisMATE decreased cell numbers to 75% in MCF-7 cells after 24 h and to 47% after 48 h of exposure. TEM demonstrated membrane blebbing, nuclear fragmentation and chromatin condensation indicating hallmarks of apoptosis. Light microscopy revealed the presence of several cells blocked in metaphase and apoptotic cells were also observed.Fluorescent microscopy demonstrated increased lysosomal staining; suggesting the induction of autophagy. 2-MeOE2bisMATE shows therapeutic potential as an anticancer agent and the investigation of the cell death mechanisms used by 2-MeOE2bisMATE thus warrants further investigation.

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2-Methoxyestradiol – a unique blend of activities generating a new class of anti-tumour/anti-inflammatory agents

Cited by 77 publications

References 48 publications

ROS-mediated mechanisms of autophagy stimulation and their relevance in cancer therapy

ROS-mediated mechanisms of autophagy stimulation and their relevance in cancer therapy

Preparation and cytotoxicity of poly (DL-lactide-co-glycolide) microspheres encapsulating 2-methoxyestradiol

2-Methoxyestradiol-bis-sulfamate induces apoptosis and autophagy in a tumorigenic breast epithelial cell line

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