EGCG-4-sulfate-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEEGCG-4″-sulfateCat.No.:HY-150526CASNo.:2708237-76-5分⼦式:C₂₂H₁₈O₁₄S分⼦量:538.43作⽤靶点:EndogenousMetabolite;Apoptosis作⽤通路:MetabolicEnzyme/Protease;Apoptosis储存⽅式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY⽣物活性EGCG-4″-sulfate绿茶中的⼀种主多酚，可抑制细胞增殖并诱导细胞凋亡。EGCG-4″-sulfate可抑制⾕氨酸脱氢酶1/2(GDH1/2,GLUD1/2)的活性。EGCG-4″-sulfate对结直肠癌、髓性⽩⾎病、甲状腺癌等多种癌症具有有效的抗癌、抗氧化和抗炎特性[1][2][3][4]。体外研究EGCG-4″-sulfate(10-60μM)inhibitsthegrowthofFB-2andWROcellsinadose-dependentmanner[1].EGCG-4″-sulfate(10-60μM,0-24h)reducescyclinD1andphosphorylationofAKTandERK1/2,andincreasesp21andp53expression[1].EGCG-4″-sulfate(10-60μM,12h)reducescellmotilityandmigration[1].EGCG-4″-sulfate(0-20μM,0-20minapproximately)inhibitsGLUD1/2andIDH1activityinaconcentrationandtime-dependentway(biochemicalassays)[2].EGCG-4″-sulfate(0-35μg/mL,24-72h)inhibitstheproliferationofcolorectalcancercells(LoVo,SW480,HT-29,HCT-8cells),increasescellapoptosisandblockscellsattheG0/G1phase[3].EGCG-4″-sulfate(30μM,3-24h)suppressestheexpressionofCOX-2andmPGES-1mRNAs,prostaglandinE2productioninLPS-inducedosteoblasts[4].CellProliferationAssay[1]CellLine:FB-2andWROcells(serum-starvedfor48h)Concentration:10,40,60μM.IncubationTime:4daysResult:Inhibitedbasalcellproliferation(40%inFB-2and35%inWRO)at10μM,inhibitedcellnumber(by68%to73%)at40and60μM).WesternBlotAnalysis[1]1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemECellLine:FB-2cellsConcentration:10,40,60μM.IncubationTime:24hResult:ReducedcyclinD1level,phosphorylationofAKTandERK1/2.Inducedtheexpressionofp21andp53,andE-cadherin,N-cadherin,Vimentinandα5-integrin.CellMigrationAssay[1]CellLine:FB-2andWROcells(serum-starvedfor48h)Concentration:10,40,60μM.IncubationTime:12hResult:ReducedmigrationactivityinFB-2andWROcells.RT-PCR[4]CellLine:Mouseprimaryosteoblasts(1ng/mlLPS-treated)Concentration:30μMIncubationTime:3,6,12,24hResult:SuppressedtheLPS-inducedexpressionofCOX-2andmPGES-1mRNAs,prostaglandinE2production.体内研究EGCG-4″-sulfate(Intragastricaladministration,5-20mg/kg,oncedailyfor14days,orthotopictransplantmodel)decreasestumorsgrowth[3].EGCG-4″-sulfate(Injectedintothemouselowergingiva,asingledoseof0.5mg/mouse,experimentalperiodontitismodel)decreasesinhibitstheLPS-inducedlossofbonemineraldensity(BMD)[3].AnimalModel:OrthotopictransplantBALB/cnudemicemodel[3]Dosage:5,10,and20mg/kg,oncedailyfor14days.Administration:Intragastricaladministration.Result:Inhibitedtumorsgrowthwithnoliverorlungmetastases.AnimalModel:Modelofexperimentalperiodontitis,LPS(25μg/mouse)[4]Dosage:0.5mg/mouse,asingledose.2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEAdministration:InjectedintothemouselowergingivaResult:InhibitedtheLPS-inducedlossofbonemineraldensity(BMD)inmice.REFERENCES[1].DeAmicisF,etal.EpigallocatechingallateinhibitsgrowthandEpithelial-to-MesenchymalTransitioninhumanthyroidcarcinomacelllines.JCellPhysiol.2013Apr1.[2].PeetersTH,etal.Isocitratedehydrogenase1-mutatedcancersaresensitivetothegreenteapolyphenolepigallocatechin-3-gallate.CancerMetab.2019May20;7:4.[3].JinH,etal.EpigallocatechingallateinhibitstheproliferationofcolorectalcancercellsbyregulatingNotchsignaling.OncoTargetsTher.2013;6:145-53.[4].TsukasaTominari,etal;Epigallocatechingallate(EGCG)suppresseslipopolysaccharide-inducedinflammatoryboneresorption,andprotectsagainstalveolarbonelossinmice.FEBSOpenBio.2015Jun12;5:522-7.McePdfHeightCauti