Brassinolide-d5-Brassin-lactone-d-sub-5-sub-DataSheet-生命科学试剂-MCE

Hotline:400-820-3792Inhibitors • ScreeningLibraries • Proteinswww.MedChemEBrassinolide-d5Cat.No.:HY-N0273SSynonyms:Brassinlactone-d5分子式:C₂₈H₄₃D₅O₆分子量:485.71作用靶点:Isotope-LabeledCompounds;Apoptosis作用通路:Others;Apoptosis储存方式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY生物活性Brassinolide-d5是氘代标记的Brassinolide(HY-N0273)。Brassinolide是一种主要的植物生长调节剂，可调节植物细胞生长。IC50&Targetplantgrowthmodulator[1]体外研究Brassinolideisaplantsterolfirstisolatedfrompollenofrape(BrassicanapusL.).Brassinolidecaninduceatimeandconcentration-dependentcytotoxicityinPC-3cells.Themodeofcelldeathappearstobepredominatelyapoptosis,asshownbyflow-cytometricanalysis,fluorescenceandtransmissionelectronmicroscopes.Caspase-3activityisobviouslyincreasedafterBrassinolidetreatment.WesternblotstudiesindicatethattreatmentwithBrassinolidetriggeredatime-dependentdecreaseintheexpressionofanti-apoptoticproteinBcl-2,whichsuggeststhatBrassinolidecaninducecytotoxicityinPC-3cellsbytriggeringapoptosis.Brassinolidemightthereforebeapromisingcandidateforthetreatmentofprostatecancer[1].Brassinolideisaplantgrowthmodulator,onmultidrugresistance(MDR)ofhumanTlymphoblastoidcelllineCCRF-VCR1000whichisobtainedbyprogressivelyadditionofvincristine(VCR)tosensitiveCCRF-CEMcells,andtoexplorepreliminarilythemechanismofreversingaction.AftertreatmentofBrassinolideundertheconcentrationof0.001-10μg/mL,theresistanceofCCRF-VCRisreversedpartlywiththereversingfoldsrespectivelyas4.4-11.6.Theintracellularaccumulationofrhodamine123issignificantlyreducedintheresistantcells.AftertreatmentofBrassinolide,theaccumulationincreased,theleveloffluorescentdyeissituatedbetweenresistantcellsandsensitivecells.NoalterationofthecatalyticactivityoftopoisomeraseIIisfoundamongthreegroups.Thelevelofproteinexpressionofp53inresistantcellsishigherthanthatofsensitivecells.AfterBrassinolidetreatment,theexpressionofp53inCCRF-VCRcellsrestoredtothelevelofsensitivecells.BrassinolidecaneffectivelyreversetheresistanceofCCRF-VCRcellsbyinhibitingtheeffusionofdrugtransportedbyP-glucoprotein.Todownregulatetheabnormalexpressionofp53maybeone1/2 MasterofBioactiveMolecules—您身边的抑制剂大师www.MedChemEofthemechanismsofreversingMDRforBrassinolide[2].Stableheavyisotopesofhydrogen,carbon,andotherelementshavebeenincorporatedintodrugmolecules,largelyastracersforquantitationduringthedrugdevelopmentprocess.Deuterationhasgainedattentionbecauseofitspotentialtoaffectthepharmacokineticandmetabolicprofilesofdrugs[3].REFERENCESXianLJ,etal.Reversingeffectofbrassinolideonmultidrugresistanceof-CCRF-VCR1000cellsandapreliminaryinvestigationonitsmechanisms.YaoXueXueBao.2005Feb;40(2):117-21.WuYD,etal.Brassinolide,aplantsterolfrompollenofBrassicanapusL.,inducesapoptosisinhumanprostatecancerPC-3cells.Pharmazie.2007May;62(5):392-5.McePdfHeightCaution:Producthasnotbeenfullyvalid