Description
2-HydroxyestrADIol(2-OHE2)isacytochromeP450metaboliteofestradiolwithlowaffinityforestrogenreceptors.2-OHE2exhibitsanti-inflammatory,neuroprotective,mitogenic,andpotentiallyanti-angiogenicactivities.Invitro,2-OHE2decreasesreleaseofprostaglandinE2(PGE2).InhippocampalHT22cells,2-OHE2decreasescellularlipidperoxidationandcelldeathinducedbyhydrogenperoxide.Additionally,2-OHE2displaysmitogeniceffectsonvascularsmoothmusclecellsafterconversiontomethoxyestradiolsandcatecholestradiolsviacytochromeP450andcatechol-O-methyltransferase(COMT)enzymes.Similarcompound2-methoxyestradiol(2-ME2)hasachievedconsiderableattentionasananticancerchemotherapeuticandanti-angiogenicagentthroughinhibitionoftheHIF-1αpathway.
References
PavanB,PaganettoG,DalpiazA,etal.Estrogenmetabolitesinthereleaseofinflammatorymediatorsfromhumanamnion-derivedcells.LifeSci.2011Mar14;88(11-12):551-8.PMID:21277863.
BeckerCM,RohwerN,FunakoshiT,etal.2-methoxyestradiolinhibitshypoxia-inducIBLefactor-1{alpha}andsuppressesgrowthoflesionsinamousemodelofendometriosis.AmJPathol.2008Feb;172(2):534-44.PMID:18202195.
DubeyRK,JacksonEK,GillespieDG,etal.Catecholaminesblocktheantimitogeniceffectofestradiolonhumancoronaryarterysmoothmusclecells.JClinEndocrinolMetab.2004Aug;89(8):3922-31.PMID:15292328.
ZachariaLC,PichéCA,FieldingRM,etal.2-hydroxyestradiolisaprodrugof2-methoxyestradiol.JPharmacolExpTher.2004Jun;309(3):1093-7.PMID:14872091.
TeepkerM,AnthesN,KriegJC,etal.2-OH-estradiol,anendogenoushormonewithneuroprotectivefunctions.JPsychiatrRes.2003Nov-Dec;37(6):517-23.PMID:14563383.