2-Methoxyestradiol

Abstract

http://hyper.ahajournals.org/ Downloaded from Figure.The ying-yang balance between deleterious and beneficial 17β-estradiol and testosterone metabolites generated by cytochrome-P1B1 (CYP1B1) and catechol-O-methyltransferase (COMT) in the vasculature. Exogenous 2-methoxyestradiol (2-ME) overrides the deleterious actions of endogenous metabolites of testosterone 2 and estrogen(s) on hypertension and cardiovascular/renal dysfunction. 3 Moreover, it depicts the conversion of 2-hydroxyestradiol (2OHE2) to 2-ME by COMT, the factors modulating CYP1B1 and COMT activity, and the multiple protective effects 2-ME induces and the potential receptors involved. ┴ indicates inhibition; ↑ increase; ↓ decrease; and ↔ bidirectional. 17β-HSD indicates 17β-hydroxysteroid dehydrogenase; 6β-OH-T, 6β-hydroxytestosterone; AhR, arylhydrocarbon receptor; E1, estrone; and E2, estradiol. by guest on April 23, 2017 http://hyper.ahajournals.org/ Downloaded from

Dietary Magnesium Insufficiency Induces Salt-Sensitive Hypertension in Mice Associated With Reduced Kidney Catechol-O-Methyl Transferase Activity

“…The compound 2-methoxyestradiol (2-ME), an estrogen metabolite of COMT generated from hydroxyestradiol, is a biologically active compound that improves glucose/lipid metabolism and possesses anti-inflammatory, antivasoconstrictive, antiangiogenic, and antitumor effects. 1,2 COMT activity is determined by various factors, as described in Figure 1A. Among genetic factors, single nucleotide polymorphisms, which determine the stability of the COMT protein, are the best-known factors.…”