Piperine-Bioperine-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEPiperineCat.No.:HY-N0144CASNo.:94-62-2Synonyms:Bioperine;1-Piperoylpiperidine分⼦式:C₁₇H₁₉NO₃分⼦量:285.34作⽤靶点:P-glycoprotein;Autophagy;EndogenousMetabolite作⽤通路:MembraneTransporter/IonChannel;Autophagy;MetabolicEnzyme/Protease储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:50mg/mL(175.23mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM3.5046mL17.5230mL35.0459mL5mM0.7009mL3.5046mL7.0092mL10mM0.3505mL1.7523mL3.5046mL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)1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE1.请依序添加每种溶剂：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.5mg/mL(8.76mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(8.76mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(8.76mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性Piperine从胡椒中分离的天然⽣物碱，可以抑制P-glycoproteinandCYP3A4的活性，在HeLa细胞中的IC50值为61.94±0.054μg/mL。IC50&TargetIC50:61.94±0.054μg/mL(P-glycoprotein,HeLacell)[1]体外研究Piperinehasshowntopossessinvitrocytotoxicactivityandinsilicostudies.TheIC50valueisfoundtobe61.94±0.054μg/mLandinsilicostudies,ithasmorenumberofhydrogenbondswithminimumbindinganddockingenergyandmaybeconsideredasinhibitorofEGFRtyrosinekinase[1].Piperinehasbeenfoundtohaveimmunomodulatory,anti-oxidant,anti-asthmatic,anti-carcinogenic,anti-inflammatory,anti-ulcer,andanti-amoebicproperties[2].Piperinecouldenhancethebioavailabilitiesofotherdrugsincludingrosuvastatin,peurarinanddocetaxel(DOX)viainhibitionofCYP3AandP-glycoproteinactivity[3].体内研究Atthedoseof3.5mg/kg,thebioavailabilityofpiperineiscalculatedtobe25.36%.ItsAUC0→tisunproportionallyincreasedwithdoses,indicatingapotentialnon-linearpharmacokineticsprofileofpiperine.ItisfoundthattheAUC0→tandC0ofdocetaxelandt1/2ofpiperinearesignificantlyincreasedaftertheircombinationuse,suggestingpotentialenhancedbioavailabilityofnotonlydocetaxelbutalsopiperine,whichmayleadtotheoverallenhancedpharmacologicaleffects[3].ThephosphorylationofI-κB,p65,p38,ERK,andJNKisinhibitedbypiperineinadose-dependentmanner,indicatingthatpiperinemaybeapotentialanti-inflammatorydrugbothinendometritisandinotherS.aureus-induceddiseases[4].PROTOCOLCellAssay[1]Standardsolutionispreparedbydissolving10mgofpiperinein100mLofmethanol.TheMTTassayiscarriedouttomeasurecellviability.Tenthousandcellsin100μLofDMEMmediaareseededinthewellsofa96-wellplate.After24h,existingmediaisremovedand100μLofvariousconcentrationsofpiperine(20–100μg/mL)areaddedandincubatedfor48hat37°CinaCO2incubator.Controlcellsaresupplementedwith0.05%DMSOvehicle.Atthe48thhourofincubation,MTT(10μLof5mg/mL)isaddedtotheplate.Thecontentsoftheplatearepipettedoutcarefully,theformazancrystalsformedaredissolvedin100μLofDMSO,andtheabsorbanceismeasuredat550nminamicroplatereader[1].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.AnimalRats:Thestocksolutionsofpiperine(PIP)anddocetaxel(DOX)arepreparedbydissolvingappropriateAdministration[3][4]amountofeachauthenticcompoundinDMSOseparatelyat1mg/mL.Thestandardsolutionscontaining2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEbothPIPandDOXarepreparedbyserialdilutionofthestocksolutionswith0.2%formicacidandacetonitrile(50:50,v/v)toyieldconcentrationsof25,50,100,200,400,800,1600,3200,6400,12800ng/mL.25Sprague-DawleyratsaredividedintofivegroupsreceivingDOX(GroupDOX7iv,7mg/kg,i.v.),PIP(GroupPIP35po,35mg/kg,p.o.)andtheircombinedadministration(GroupDOX+PIP)aswellasPIP(GroupPIP3.5po,3.5mg/kg,p.o.)andPIP(GroupPIP3.5iv,3.5mg/kg,i.v.)[3].Mice:Piperineisdissolvedin5mLoftrisbufferedsaline(TBS)atconcentrationscorrespondingto25,50,and100mg/kg,basedontheweightofthemice.After24hofS.aureusinfectionintheuterus,thepiperinesolutionisinjectedintraperitoneallythreetimesevery6h.Atotalof60femaleBALB/cmiceareusedinthisstudy.Allmicearemaintainedona12hlight/darkcycleandcafeteriafeeding[4].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.户使⽤本产品发表的科研⽂献•PLoSBiol.2018Jul12;16(7):e2004921.•PhytotherRes.2022Sep17.•IntImmunopharmacol.2018Oct30;65:448-457.•JNeurosciRes.2019Dec;97(12):1689-1705.•BiochemBiophysResCommun.2019Aug20;516(2):365-372.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].PaarakhPM,etal.InvitrocytotoxicandinsilicoactivityofpiperineisolatedfromPipernigrumfruitsLinn.InSilicoPharmacol.2015Dec;3(1):9.Epub2015Oct29.[2].MeghwalM,etal.Pipernigrumandpiperine:anupdate.PhytotherRes.2013Aug;27(8):1121