Description
PiceatannolisapolyphenolichydroxystilbenederivativeofresveratrolwithincreasedbioavailABIlityandbioactivitycomparedtoitsparentcompound.Piceatannolexhibitspro-angiogenic,anticancer,antioxidative,andanti-obesityproperties.PiceatannoldirectlyinhibitsHIF-prolylhydroxylase-2(HPH-2),increasinglevelsofHIF-1α,VEGF,andhemeoxygenase-1(HO1).Whencomplexedwithcopper(II),thepiceatannol-CucomplexincreasesROSlevelsanddamagesDNA.Additionally,piceatannolsuppressesnucleartranslocationofp65andp50,preventingactivationofNF-κBanddownregulatingexpressionofmatrixmetalloproteinase9(MMP9).PiceatannolalsodownregulatesphosphorylationofAktinprostatecancercells.Inotherinvitromodels,thiscompoundincreaseslevelsoftissueinhibitorofmetalloproteinase2(TIMP2)andinhibitsphosphorylationofSTAT3;italsodownregulatesBcl-xlandinhibitsphosphorylationofJNK.Inprostatecancercells,piceatannoldecreaseslevelsofcyclinsAandD1andalsodecreasescyclin-dependentkinase2and4(CDK2,CDK4)activity,inhibitingcellgrowth.ThehydroxylgroupsonpiceatannolfunctionasrADIcalscavengers,preventingaccumulationofROSandRNS.Thiscompoundnoncompetitivelyinhibitstheinsulinreceptor(IR),preventingphosphorylationofthereceptor,IRsubstrate-1andAkt,inhibitingAdipogenesisofpreadipocytes;itmayalsodirectlyinhibitPI3KandJAK1.