Potential vascular actions of 2-methoxyestradiol.
2-Methoxyestradiol (2-ME) is a biologically active metabolite of 17beta-estradiol that appears to inhibit key processes associated with cell replication in vitro. The molecule has been suggested to have potent growth-inhibitory effects on proliferating cells, including smooth muscle cells and endothelial cells, and may be antiangiogenic. Because of these potential roles for 2-ME, its lack of cytotoxicity and low estrogenic activity, we hypothesize that 2-ME could be a valuable therapeutic molecule for prevention and treatment of cardiovascular diseases. Whether 2-ME is as effective in vivo as it is in vitro at modulating vascular processes remains controversial. Here we discuss recent developments regarding mechanisms by which 2-ME might regulate vascular activity and angiogenesis and speculate on the therapeutic implications of these developments.
Dubey
Raghvendra K
RK
Clinic for Reproductive Endocrinology, Department of Obstetrics and Gynecology, Zurich Center for Integrative Human Physiology, University Hospital Zurich, Frauenklinikstrasse, Zurich, Switzerland. Raghvendra.Dubey@usz.ch
Jackson
Edwin K
EK
D000077584:2-Methoxyestradiol; D000818:Animals; D002318:Cardiovascular Diseases / Q000188:drug therapy / Q000517:prevention & control; D004958:Estradiol / Q000031:analogs & derivatives* / Q000378:metabolism / Q000493:pharmacokinetics / Q000494:pharmacology / Q000627:therapeutic use; D006801:Humans; D008954:Models, Biological; D009131:Muscle, Smooth, Vascular / Q000166:cytology / Q000187:drug effects*; D032389:Myocytes, Smooth Muscle / Q000166:cytology / Q000187:drug effects; D009389:Neovascularization, Pathologic / Q000188:drug therapy; D050257:Tubulin Modulators / Q000493:pharmacokinetics / Q000494:pharmacology* / Q000627:therapeutic use
D050257:Tubulin Modulators; D004958:Estradiol; D000077584:2-Methoxyestradiol