2-Methoxyjuglone-生命科学试剂-MCE

Hotline:400-820-3792Inhibitors • ScreeningLibraries • Proteinswww.MedChemE2-MethoxyjugloneCat.No.:HY-N17440CASNo.:15127-94-3分子式:C₁₁H₈O₄分子量:204.18作用靶点:Apoptosis;Caspase;Bcl-2Family;DNA/RNASynthesis;Bacterial;Fungal作用通路:Apoptosis;CellCycle/DNADamage;Anti-infection储存方式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY生物活性2-Methoxyjuglone是一种萘醌类化合物，为细胞凋亡(apoptosis)诱导剂。2-Methoxyjuglone可通过线粒体细胞色素c依赖的内源性凋亡级联反应激活caspase-9和caspase-3。2-Methoxyjuglone可上调促凋亡蛋白Bax的表达水平，下调抗凋亡蛋白Bcl-2的表达水平，并促进线粒体细胞色素c的释放。2-Methoxyjuglone可诱导细胞凋亡形态学特征、早期凋亡、S期和G2/M期细胞周期阻滞以及DNA双链断裂。2-Methoxyjuglone对革兰氏阳性菌、致病真菌和植物病原真菌具有活性。2-Methoxyjuglone可用于肝细胞癌、骨肉瘤、结肠腺癌、乳腺癌、真菌感染及细菌感染的相关研究[2]。IC50&TargetCaspase3Caspase9BaxBcl-2体外研究2-Methoxyjuglone(1.6-8.0μg/mL;24,48,72h)reducesHepG2humanhepatocellularcarcinomacellviabilityinadose-andtime-dependentmanner,withIC50valuesof3.8,3.7,and2.7μg/mLafter24,48,and72hoftreatment,respectively[1].2-Methoxyjuglone(4.8-8.0μg/mL;24h)inducesapoptoticmorphologicalchanges(cellshrinkage,membraneblebbing)inHepG2humanhepatocellularcarcinomacells[1].2-Methoxyjuglone(1.6-8.0μg/mL;24,48h)inducesSphasecellcyclearrestinHepG2humanhepatocellularcarcinomacellsafter24and48hoftreatmentat1.6-8.0μg/mL,andcausesDNAfragmentation(sub-G1phaseaccumulation)at6.4and8.0μg/mLafter48h[1].2-Methoxyjuglone(1.6-4.8μg/mL;24h)inducesHepG2humanhepatocellularcarcinomacellapoptosisviathemitochondrialcytochromec-dependentintrinsicpathway,withdose-dependentincreasesincytochromecrelease,caspase-9andcaspase-3activation,PARPcleavage,andBax/Bcl-2ratioafter24hoftreatmentat1.6-4.8μg/mL[1].2-Methoxyjuglone(10μM;1.25μM,24h)potentlyinhibitsDNAtopoisomeraseIIat10μMandinducesDNA1/3 MasterofBioactiveMolecules—您身边的抑制剂大师www.MedChemEdouble-strandbreaksinhumanosteosarcomaU2OScellsat1.25μM,contributingtoitscytotoxicactivity[2].2-Methoxyjuglone(62.5μg/mL;100μM)exhibitspotentinvitroantibacterialactivityagainstmultipleGram-positivebacterialstrains,with100%growthinhibitionofBacillussubtilisat100μM,strongactivityagainstBacillussubtilisat62.5μg/mL[2].2-Methoxyjuglone(0.25%-4%;250μg/mL;8μg/mL;0.1-0.5mg/mL)exhibitsbroad-spectruminvitroantifungalactivityagainstpathogenicandphytopathogenicfungi,with100%inhibitionofFusariumgraminearumsporegerminationat0.5mg/mL[2].2-MethoxyjuglonepotentlyinhibitstheviabilityofhumancoloncarcinomaHT-29cells(IC50=2.6μg/mL)andhumanbreastcarcinomaMCF-7cells(IC50=1.2μg/mL)[3].CellViabilityAssay[1]CellLine:HepG2humanhepatocellularcarcinomacellsConcentration:1.6,3.2,4.8,6.4,8.0μg/mLIncubationTime:24,48,72hResult:Induceddose-dependentandtime-dependentdecreasesincellviability.ReachedIC50valuesof3.8μg/mL(24h),3.7μg/mL(48h),and2.7μg/mL(72h).ApoptosisAnalysis[1]CellLine:HepG2humanhepatocellularcarcinomacellsConcentration:4.8,8.0μg/mLIncubationTime:24hResult:Causedcellshrinkageandmembraneblebbingat4.8μg/mL.Inducedalmostallcellstoshrinkwithnonormalmorphologicalfeaturesat8.0μg/mL.\nReducedthenumberofcellsoncoverslipssignificantlyandinducednuclearcondensationwithyellowstaining(earlyapoptosis)at4.8μg/mL.Causedalmostallcellstodetachfromcoverslips,withorangestainingandapoptoticbodyformation(lateapoptosis)at8.0μg/mL.CellCycleAnalysis[1]CellLine:HepG2humanhepatocellularcarcinomacellsConcentration:1.6,3.2,4.8,6.4,8.0μg/mLIncubationTime:24,48hResult:IncreasedthefractionofcellsintheSphase(62%,64%,62%,61%,59%at1.6,3.2,4.8,6.4,8.0μg/mL,respectively)anddecreasedfractionsinG1andG2/Mphasesafter24h.IncreasedthefractionofcellsintheSphase(49%,64%,66%,52%,46%at1.6,3.2,4.8,6.4,8.0μg/mL,respectively)after48h.2/3 MasterofBioactiveMolecules—您身边的抑制剂大师www.MedChemEInduceddramaticincreasesinsub-G1phasefraction(18%and33%,respectively)at6.4and8.0μg/mLfor48h,indicatingDNAfragmentationassociatedwithapoptosis.WesternBlotAnalysis[1]CellLine:HepG2humanhepatocellularcarcinomacellsConcentration:1.6,3.2,4.8μg/mLIncubationTime:24hResult:Increasedcytoplasmiccytochromeclevelsinadose-dependentmanner.Activatedcaspase-9viaproteolyticcleavageofthe47kDapro-enzymetothe35kDaactiveform,increasingthecleaved/uncleavedratio.Activatedcaspase-3viaproteolyticcleavageofthe35kDapro-enzymetothe17kDaactiveform,increasingthecleaved/uncleavedratio.Increasedthecleaved/uncleavedPARPratio.Elevatedpro-apoptoticBaxproteinlevelsandreducedanti-apoptoticBcl-2proteinlevelsinadose-dependentmanner,resultinginanelevatedBax/Bcl-2ratio.体内研究2-Methoxyjuglone(0.25-1.0mg/kg;i.p.;daily;8days)exhibitsstatisticallysignificantinvivoantitumoractivityagainstH22mousehepatocellularcarcinoma,reducingtumormassby56%and67%atdosesof0.5mg/kgand1.0mg/kg,respectively,withoutimpairingnormalmouseweight[1].AnimalModel:Kunmingmice(male,SPF,6weeksold,18-22g,subcutaneousinoculationofH22hepatocellularcarcinomacells)[1]Dosage:0.25mg/kg;0.5mg/kg;1.0mg/kgAdministration:i.p.;daily;8daysResult:Reducedtumormassinmice.Didnotreducethenormalweight(totalweightminustumorweight)ofmiceatanytesteddose.REFERENCESYuHY,etal.2-methoxyjugloneinducesapoptosisinHepG2humanhepatocellularcarcinomacellsandexhibitsinvivoantitumoractivityinaH22mousehepatoc