Xanthohumol-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEXanthohumolCat.No.:HY-N1067CASNo.:6754-58-1分⼦式:C₂₁H₂₂O₅分⼦量:354.4作⽤靶点:COX;Acyltransferase;Apoptosis;HSV;CMV;InfluenzaVirus作⽤通路:Immunology/Inflammation;MetabolicEnzyme/Protease;Apoptosis;Anti-infection储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:83.33mg/mL(235.13mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.8217mL14.1084mL28.2167mL5mM0.5643mL2.8217mL5.6433mL10mM0.2822mL1.4108mL2.8217mL请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。储备液的保存⽅式和期限：-80°C,6months;-20°C,1month。-80°C储存时，请在6个⽉内使⽤，-20°C储存时，请在1个⽉内使⽤。体内实验请根据您的实验动物和给药⽅式选择适当的溶解⽅案。以下溶解⽅案都请先按照InVitro⽅式配制澄的储备液，再依次添加助溶剂：(为保证实验结果的可靠性，澄的储备液可以根据储存条件，适当保存；体内实验的⼯作液，建议您现⽤现配，当天使⽤；以下溶剂前显⽰的百分⽐指该溶剂在您配制终溶液中的体积占⽐；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的⽅式助溶)1.请依序添加每种溶剂：10%DMSO>>40%PEG300>>5%Tween-80>>45%saline1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemESolubility:≥2.08mg/mL(5.87mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.08mg/mL(5.87mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性Xanthohumol从啤花中分离到的酮类化合物，DGAT，COX-1和COX-2的抑制剂，具有抗肿瘤，抗⾎管⽣成的作⽤。Xanthohumol还具有抗⽜病毒性腹泻病毒(BVDV)，⿐病毒，HSV-1，HSV-2和巨细胞病毒(CMV)的抗病毒活性。IC50&TargetCOX-1COX-2HSV-1HSV-2DGAT1DGAT2CMV40μM(IC50)40μM(IC50)体外研究XanthohumolsignificantlyattenuatesADP-inducedbloodplateletaggregation,andsignificantlyreducestheexpressionoffibrinogenreceptor(activatedformofGPIIbIIIa)onplatelets'surface[1].Xanthohumol(5-50nM)reducesthefrequencyofspontaneouslyoccurringCa2+sparksandCa2+wavesin

controlmyocytesandincellssubjectedtoCa2+overloadcausedby:(1)exposuretolowK+solutions,(2)

periodsofhighfrequencyelectricalstimulation,(3)exposurestoisoproterenolor(4)caffeine.Xanthohumol

(50-100nM)reducestherateofrelaxationofelectrically-orcaffeine-triggeredCa2+transients,without

suppressingICa,butthiseffectissmallandreversedbyisoproterenolatphysiologicaltemperatures.

XanthohumolalsosuppressestheCa2+contentoftheSR,anditsrateofrecirculation[2].

TreatmentofendothelialcellswithXanthohumolleadstoincreasedAMPKphosphorylationandactivity.

FunctionalstudiesusingbiochemicalapproachesconfirmthatAMPKmediatesXanthohumolanti-angiogenic

activity.AMPKactivationbyXanthohumolismediatedbyCAMMKβ,butnotLKB1.Analysisofthe

downstreammechanismsshowsthatXanthohumol-inducedAMPKactivationreducesnitricoxide(NO)levels

inendothelialcellsbydecreasingeNOSphosphorylation.Finally,AKTpathwayisinactivatedby

Xanthohumolaspartofitsanti-angiogenicactivity,butindependentlyfromAMPK,suggestingthatthesetwo

signalingpathwaysproceedautonomously[3].Xanthohumolsignificantlyreducescellviabilityandinducesapoptosisviapro-caspase-3/8cleavageand

poly(ADPribose)polymerase(PARP)degradation.Pro-caspase-9cleavage,Bcl2familyexpression

changes,mitochondrialdysfunction,andintracellularROSgenerationalsoparticipateinXanthohumol-

inducedgliomacelldeath.Xanthohumol'sinhibitionoftheIGFBP2/AKT/Bcl2pathwayviamiR-204-3p

targetingplaysacriticalroleinmediatinggliomacelldeath[4].PROTOCOLCellAssay[3]Invitrocellproliferation/viabilityismeasuredbytheMTTtestatdifferenttimepoints.1000cells/wellareplatedinto96-multiwellplatesincompletemedium.Followingadhesion,mediumisreplacedwithfreshmediumcontainingthedifferenttreatmentsorvehicle(DMSOinmedium).XanthohumolandEGCGareusedinaconcentrationrangefrom2.5to40μM,upto96hours.3hoursbeforeeachtimepoint,MTTreagent(3-2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazoliumbromide)isaddedtothewellsandplatesareincubatedat37°C.Attheindicatedtimepoints,absorbanceat540nmisthenmeasuredbyaFLUOstarspectrophotometer.MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.户使⽤本产品发表的科研⽂献•ActaPharmSinB.2021Jan;11(1):143-155.•BiomedPharmacother.2020Sep;129:110369.•FoodFunct.2019Dec11;10(12):7865-7874.•Neuroreport.2021May19;32(8):651-658.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].LuzakB,etal.Xanthohumolfromhopcones(HumuluslupulusL.)preventsADP-inducedplateletreactivity.ArchPhysiolBiochem.2016Nov18:1-7[2].Arnaiz-CotJJ,etal.Xanthohumolmodulatescalciumsignalinginratventricularmyocytes:PossibleAntiarrhythmicproperties.JPharmacolExpTher.2016Nov4.pii:jpet.116.236588[3].GalloC,etal.HopderivedflavonoidxanthohumolinhibitsendothelialcellfunctionsviaAMPKactivation.Oncotarget.2016Aug1[4].ChenPH,etal.ThemiR-204-3p-targetedIGFBP2pathwayisinvolvedinxanthohumol-inducedgliomacellapoptoticdeath.Neuropharmacology.2016Nov;110(PtA):362-75.[5].BuckwoldVE,etal.AntiviralactivityofhopconstituentsagainstaseriesofDNAandRNAviruses.AntiviralRes.2004Jan;61(1):57-62.[6].InokoshiJ,etal.Expressionoftwohumanacyl-CoA:diacylglycerolacyltransferaseisozymesinyeastandselectivityofmicrobialinhibitors