简介：Thepresentstudywasdesignedtosynthesize2-Cyano-3,12-dioxooleana-1,9(11)-en-28-oate-13β,28-olide(1),alactonederivativeofoleanolicacid(OA)andevaluateitsanti-inflammatoryactivity.Compound1significantlydiminishednitricoxide(NO)productionanddown-regulatedthemRNAexpressionofiNOS,COX-2,IL-6,IL-1β,andTNF-αinlipopolysaccharide(LPS)-stimulatedRAW264.7cells.FurtherinvivostudiesinmurinemodelofLPS-inducedacutelunginjury(ALI)showedthat1possessedmorepotentprotectiveeffectsthanthewell-knownanti-inflammatorydrugdexamethasonebyinhibitingmyeloperoxidase(MPO)activity,reducingtotalcellsandneutrophils,andsuppressinginflammatorycytokinesexpression,andthusamelioratingthehistopathologicalconditionsoftheinjuredlungtissue.Inconclusion,compound1couldbedevelopedasapromisinganti-inflammatoryagentforinterventionofLPS-inducedALI.

简介：Alpiniapurpurata的目的Ethylacetate摘录在vitro抗氧化剂和anticancer活动为它的潜力被评估。抗氧化剂活动被1评估的方法，1-diphenyl-2-picrylhydrazyl(DPPH)免费激进的清除方法，氢氧根基活动，superoxide基清除活动，氮的氧化物基清除活动，氢过氧化物基清除活动和减少的力量活动。OAW42房间的生存能力被MTT试金评估。结果A。purpurata与一种集中依赖者方式展出了潜在的抗氧化剂活动。摘录与130.20g的IC50在第48小时显示出潜在的anticancer活动?潴??祥獥吗？

简介：目的这研究被设计评估tanshinone的反癌症行动我和tanshinoneIIA，和正常、癌的冒号房间上的tanshinoneIIA的六衍生物。结构活动关系(SAR)分析被进行描出为改进反癌症的tanshinones的结构的修正的意义行动。方法Tanshinone衍生物根据文学被设计并且综合。结肠癌房间上的不同混合物的cytotoxicity被MTT试金决定。tanshinones的Apoptotic活动被流动cytometry(FCM)测量。结果Tanshinone我和tanshinoneIIA两个都在结肠癌房间上展出了重要cytotoxicity。他们在p53+/+结肠癌房间线是更有效的。这也被注意我是的tanshinone的反癌症活动更多的有势力并且选择。tanshinoneIIA(N1和N2)的二衍生物也在结肠癌房间上展出了cytotoxicity。结论tanshinone的反冒号癌症活动我是更多的有势力并且比tanshinoneIIA选择，并且p53依赖者。tanshinoneIIA的结构的修正获得的衍生物在正常和结肠癌房间上展出了更低的cytotoxicity。从位、电子的特征观点，戒指A和呋喃或dihydrofuran的结构的修正在tanshinones影响的基本结构上包围D，这被结束这项活动。A和B戒指的delocalization的增加能提高如此的混合物的cytotoxicity，当一个非平面、小的大小的D戒指区域将提供改进反癌症活动时。

简介：Danshensu[3-(3,4-dihydroxyphenyl)lacticacid,DSS],oneofthesignificantcardioprotectivecomponents,isextractedfromtherootofSalviamiltiorrhiza.Inthepresentstudy,anesterprodrugofDanshensu(DSS),palmitoylDanshensu(PDSS),wassynthesizedwiththeaimtoimproveitsoralbioavailabilityandprolongitshalf-life.TheinvitroexperimentswerecarriedouttoevaluatethephysicochemicalpropertiesandstabilityofPDSS.AlthoughthesolubilityofPDSSinwaterwasonly0.055mg·mL~(-1),itssolubilityinFaSSIFandFeSSIFreached4.68and9.08mg·mL~(-1),respectively.Octanol-waterpartitioncoefficient(logP)wasincreasedfrom-2.48ofDSSto1.90ofPDSS.PDSSwasrelativelystableintheaqueoussolutioninpHrangefrom5.6to7.4.Furthermore,thepharmacokineticsinratswasevaluatedafteroraladministrationofPDSSandDSS.AUCandt1/2ofPDSSwereenhancedupto9.8-foldand2.2-fold,respectively,comparedtothatofDSS.Cmaxwas1.67±0.11μg·mL~(-1)forPDSSand0.81±0.06μg·mL-1forDSS.Thus,theseresultsdemonstratedthatPDSShadmuchhigheroralbioavailabilityandlongercirculationtimethanitsparentdrug.

简介：由于存在止痛剂的低效率和副作用，长期的疼痛在诊所成为了最复杂、困难的问题之一。Monoacylglycerol脂肪分解酵素(MAGL)是在endocannabinoid系统的必要hydrolase并且为疼痛的治疗作为一个潜在的目标被识别了。在现在的学习，我们设计了并且综合12tanshinoneIIA类似物并且对MAGL屏蔽了他们的活动。选择混合物在vivo为止痛活动被测试，与扭曲测试模型的醋酸。在测试混合物之中，加重III-3(IC50120nmol

简介：ThepresentstudywasdesignedtodeterminetheeffectsofatraditionalChinesemedicine,calledQishenYiqiDroppingPillonchronichypoxia-inducedmyocardialinjury.ToestablisharatchronichypoxiamodeltobeusedintheevaluationofthetherapeuticeffectsoftheQishenYiqiDroppingPill,Sprague-Dawley(SD)ratswererandomlydividedintothreegroups:thecontrol,model,andtreatmentgroups(n=10pergroup).Theanimalswerehousedinaplexiglasscontainer.Thecontrolanimalswereundernormaloxygenconcentrationandthemodelandtreatmentgroupswereexposedtoairandnitrogenfor5weeks.TheratsinthetreatmentgroupwereorallyadministeredtheQishenYiqiDroppingpill(35mg·kg-1·d-1)for5weeks.Afterthetreatment,thecardiacfunctionandmorphologywereanalyzed,andtheexpressionlevelsofhypoxia-induciblefactor1α(HIF-1α)weredeterminedusingWesternblotting.Ourresultsindicatedthatthecardiacfunctionwasimpaired,cellapoptosiswasenhanced,andHIF-1αexpressionwasup-regulatedinthemodelgroup,comparedtothecontrolgroup.ThesechangeswereamelioratedbythetreatmentwiththeQishenYiqiDroppingPill.Inconclusion,QishenYiqiDroppingpillcanamelioratemyocardialinjuryinducedbychronichypoxia,improvecardiacfunction,anddecreasemyocardialcellapoptosis,whichmayprovideabasisforitsclinicaluseforthetreatmentofchroniccardiovasculardiseases

简介：Sheng-Mai-San(SMS),awell-knownChinesemedicinalplantformula,iswidelyusedforthetreatmentofcardiacdiseasescharacterizedbydeficiencyofQiandYinsyndrome.Amousechronicintermittenthypoxia(CIH)modelwasestablishedtomimictheprimaryclinicalfeaturesofdeficiencyofQiandYinsyndrome.MiceexperiencedCIHfor28days(nadir7%topeak8%oxygen,20minperday),resultinginleftventricle(LV)dysfunctionandstructureabnormalities.AfteradministrationofSMS(0.55,1.1,and5.5g·kg-1·d-1)forfourweeks,improvedcardiacfunctionwasobserved,asindicatedbytheincreaseintheejectionfractionfromtheLVonechocardiography.SMSalsopreservedthestructuralintegrityoftheLVagainsteccentrichypotrophy,tissuevacuolization,andmitochondrialinjuryasmeasuredbyhistology,electronmicroscopy,andultrasoundassessments.Mechanistically,theantioxidanteffectsofSMSweredemonstrated;SMSwasabletosuppressmitochondrialapoptosisasindicatedbythereductionofseveralpro-apoptoticfactors(Bax,cytochromec,andcleavedcaspase-3)andup-regulationoftheanti-apoptosisfactorBcl-2.Inconclusion,theseresultsdemonstratethatSMStreatmentcanprotectthestructureandfunctionoftheLVandthattheprotectiveeffectsofthisformulaareassociatedwiththeregulationofthemitochondrialapoptosispathway.

简介：ThepresentstudywasdesignedtoevaluatetheprotectiveeffectsofethanolextractsofRabdosiajaponicavar.glaucocalyx(Maxim.)Hara(RJ)onlipopolysaccharide(LPS)-inducedacutelunginjury(ALI)inmiceandthepossibleunderlyingmechanismsofaction.ThemicewereorallyadministratedwithRJextract(16,32or64mg?kg–1)dailyforconsecutive7daysbeforeLPSchallenge.Theungspecimensandthebronchoalveolarlavagefluid(BALF)werecollectedforhistopathologicalexaminationsandbiochemicalanalyses.PretreatmentwithRJsignificantlyenhancedsuperoxidedismutase(SOD)activityandreducedthewet-to-dryweight(W/D)ratio,thelevelsofnitricoxide(NO)andproteinleakage,andmyeloperoxidase(MPO)activityinmicewithALI,inadose-dependentmanner.RJreducedcomplementdepositionandsignificantlyattenuatedLPS-inducedALIbyreducingproductionsofinflammatorymediators,suchastumornecrosisfactor-α(TNF-α),interleukin-6(IL-6),andinterleukin-1β(IL-1β).TheresultsdemonstratedthatRJmayattenuateLPS-inducedALIviareducingtheproductionofpro-inflammatorymediators,andreducingcomplementdepositionandradicals.

简介：调查的目的在里面vitro抗氧化剂活动和methanolic叶的全部的酉分的内容Nyctanthesarbor-tristisL提取。(NA)。样品在vitro抗氧化剂方法用五被测试的方法(1，1-diphenyl-2-picryl肼基清除活动(DPPH)，氢氧根激进清除的活动(-OH),氮的氧化物清除活动(没有)，superoxide激进清除的活动，并且总计抗氧化剂活动)评估在里面NA和全部的酉分的内容(Folin-Ciocalteu方法)的vitro抗氧化剂潜力。摘录看好免费激进的清除性质哪个作为IC50价值计算。methanolic摘录的结果IC50(半最大的禁止的集中)被发现是57.93?g牴慥整?慲獴愠?潢桴搠獯獥

简介：Schisandrachinensis,atraditionalChinesemedicine(TCM),hasbeenusedtotreatsleepdisorders.Zebrafishsleep/wakebehavioralprofilingprovidesahigh-throughputplatformtoscreenchemicals,buthasneverbeenusedtostudyextractsandcomponentsfromTCM.Inthepresentstudy,theethanolextractofSchisandrachinensisanditstwomainlignincomponents,schisandrinandschisandrinB,werestudiedinzebrafish.Wefoundthattheethanolextracthadbidirectionalimprovementinrestandactivityinzebrafish.SchisandrinandschisandrinBwerebothsedativeandactivecomponents.WepredictedthatschisandrinwasrelatedtoserotoninpathwayandtheenthanolextractofSchisandrachinensiswasrelatedtoseoroninanddomapinepathwaysusingadatabaseofzebrafishbehaviors.ThesepredictionswereconfirmedinexperimentsusingCaenorhabditiselegans.Inconclusion,zebrafishbehaviorprofilingcouldbeusedasahigh-throughputplatformtoscreenneuroactiveeffectsandpredictmolecularpathwaysofextractsandcomponentsfromTCM.

简介：Thepresentstudywasdesignedtoestablishamulti-wavelengthquantitativefingerprintingmethodforSan-HuangTablets(SHT),awidelyusedandcommerciallyavailableherbalpreparation,wherehighperformanceliquidchromatography(HPLC)withadiodearraydetector(DAD)wasemployedtoobtainthefingerprintprofiles.Asimplelinearquantitativefingerprintmethod(SLQFM)coupledwithmulti-ingredientsimultaneousdeterminationwasdevelopedtoevaluatethequalityconsistencyofthetestedsamplesqualitativelyandquantitatively.Additionally,thecomponent–activityrelationshipbetweenchromatographicfingerprintsandtotalradical-scavengingcapacityinvitro(asassessedusingthe1,1-diphenyl-2-picrylhydrazyl(DPPH)assay)wasinvestigatedbypartialleastsquaresregression(PLSR)analysistopredicttheantioxidantcapacityofnewsamplesfromthechromatographicfingerprintsandidentifythemainactiveconstituentsthatcanbeusedasthetargetmarkersforthequalitycontrolofSHT.Inconclusion,thestrategydevelopedinthepresentstudywaseffectiveandreliable,whichcanbeemployedforholisticevaluationandaccuratediscriminationforthequalityconsistencyofSHTpreparationsandothertraditionalChinesemedicine(TCM)andherbalpreparationsaswell.

简介：Inthepresentstudy,aseriesofnovelnitricoxide-hydrogensulfidereleasingderivativesof(S)-3-n-butylphthalide((S)-NBP)weredesigned,synthesized,andevaluatedaspotentialantiplateletagents.CompoundNOSH-NBP-5displayedthestrongestactivityininhibitingthearachidonicacid(AA)-andadenosinediphosphate(ADP)-inducedplateletaggregationinvitro,with3.8-and7.0-foldmoreeffectivenessthan(S)-NBP,respectively.Furthermore,NOSH-NBP-5couldreleasemoderatelevelsofNOandH2S,whichwouldbebeneficialinimprovingcardiovascularandcerebralcirculation.Moreover,NOSH-NBP-5couldrelease(S)-NBPwhenincubatedwithratbrainhomogenate.Inconclusion,thesefindingsmayprovidenewinsightsintothedevelopmentofnovelantiplateletagentsforthetreatmentofthrombosis-relatedischemicstroke.