2-methoxy Estrone is an active metabolite of the endogenous estrogen estrone .1 It is formed from estrone by catechol-O-methyltransferase (COMT). 2-methoxy Estrone inhibits the proliferation of isolated bovine brain-derived capillary endothelial cells (IC50 = 11.5 ?M).2 It increases the levels of 6-keto prostaglandin F1α in human umbilical vein endothelial cells (HUVECs) when used at concentrations of 0.001, 0.01, and 0.1 ?M.3 2-methoxy Estrone (0.5 mg/kg) reduces ovariectomy-induced increases in serum cholesterol in rats.4
1.Dawling, S., Roodi, N., Mernaugh, R.L., et al.Catechol-O-methyltransferase (COMT)-mediated metabolism of catechol estrogens: Comparison of wild-type and variant COMT isoformsCancer Res.61(18)6716-6722(2001) 2.Fotsis, T., Zhang, Y., Pepper, M.S., et al.The endogenous oestrogen metabolite 2-methoxyoestradiol inhibits angiogenesis and suppresses tumour growthNature368(6468)237-239(1994) 3.Seeger, H., Mueck, A.O., and Lippert, T.H.Effect of estradiol metabolites on prostacyclin synthesis in human endothelial cell culturesLife Sci.65(13)PL167-PL170(1999) 4.Liu, D., and Bachmann, K.A.An investigation of the relationship between estrogen, estrogen metabolites and blood cholesterol levels in ovariectomized ratsJ. Pharmacol. Exp. Ther.286(1)561-568(1998)