2-Methoxyestradiol (2ME) is a major non-oestrogenic metabolite of oestradiol. Our previous studies, performed in several models of cardiac and/or vascular injury, suggest that 2ME strongly inhibits both pressure-dependent and pressure-independent cardiac and vascular remodelling. Furthermore, recently we have shown that in male rats 2ME attenuates the development and retards the progression of ...

2-Methoxyestradiol (2ME), a promising anti-tumor agent, is currently tested in phase I/II clinical trial to assess drug tolerance and clinical effects. 2ME is known to affect microtubule (MT) polymerization rather than act through estrogen receptors. We hypothesized that 2ME, similar to other MT inhibitors, disrupts endothelial barrier properties. We show that 2ME decreases transendothelial ele...

Levels of 2-methoxyestradiol (2ME(2)), an endogenous metabolite of estradiol, are highly elevated during late stages of pregnancy when mammary glands have differentiated with the formation of alveolar structures producing milk proteins. Based upon our previous demonstration that 2ME(2) induces mammary ductal dilation associated with expression of mammary differentiation markers when administere...

This study aims to evaluate the potential benefit of combination therapy of 2-methoxyestradiol (2ME) and magnetic nanoparticles of Fe(3)O(4) (MNPs-Fe(3)O(4)) on myelodysplastic syndrome (MDS) SKM-1 cells and its underlying mechanisms. The effect of the unique properties of tetraheptylammonium-capped MNPs-Fe(3)O(4) with 2ME on cytotoxicity was tested by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenylt...

UNLABELLED Aims/Introduction:  2-Methoxyestradiol (2ME) is an estradiol metabolite with little estrogenic activity. Previous data identified its anti-carcinogenic properties and possible cardiovascular benefits. However, its effect on diabetes mellitus has not been fully elucidated. The aim of the present study was to determine the effects of 2ME on glucose metabolism in the diabetic state. M...

The aim of this study was to prepare a novel targeting drug delivery system for 2-Methoxyestradiol (2ME) in order to improve the clinical application of this antitumor drug. It is based in nanoparticles (NPs) of titanium dioxide (TiO2) coated with polyethylene glycol (PEG) and loaded with 2ME. A complete IR and Raman characterization have been made to confirm the formation of TiO2–PEG–2ME compo...

CONTEXT Development of optimal medicinal treatments of uterine leiomyomas represents a significant challenge. 2-Methoxyestradiol (2ME) is an endogenous estrogen metabolite formed by sequential action of CYP450s and catechol-O-methyltransferase (COMT). Our previous study demonstrated that 2ME is a potent antiproliferative, proapoptotic, antiangiogenic, and collagen synthesis inhibitor in human l...

2-Methoxyestradiol (2ME(2)), a physiologic metabolite of 17beta-estradiol (estrogen), has emerged as a promising cancer therapy because of its potent growth-inhibitory and proapoptotic effects on both endothelial and tumor cells. 2ME(2) also suppresses osteoclast differentiation and induces apoptosis of mature osteoclasts, and has been shown to effectively repress bone loss in an animal model o...

The interaction between the potent anticancer agent 2-methoxyestradiol (2ME) and a series of cyclodextrins (CDs) was investigated in the solid state using thermal analysis and X-ray diffraction, while the possibility of enhancing its poor aqueous solubility with CDs was probed by means of equilibrium solubility and dissolution rate measurements. Single crystal X-ray diffraction studies of the i...