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简介：为阐明β榄香烯的抗血小板作用，本文分别采用比浊法和放免法测定大鼠连续ｉｐ７ｄβ榄香烯乳６．２５～１２．５ｍｇ·ｋｇ－１·ｄ－１后对血小板聚集、血浆ｋｅｔｏＰＧＦ１α和ＴＸＢ２水平的影响。结果表明，本品分别使凝血酶、花生四烯酸和ＡＤＰ诱导血小板最大聚集率下降３８．３％～４２．６％，１４．７％～１９．１％和７．２％～１０．８％，血浆ＴＸＢ２从８８ｎｇ·Ｌ－１下降至７２ｎｇ·Ｌ－１，ｋｅｔｏＰＧＦ１α从１７．５ｎｇ·Ｌ－１增加至２０．９ｎｇ·Ｌ－１。提示ＴＸＢ２降低和ｋｅｔｏＰＧＦ１α值增加是其抑制血小板聚集的作用机制之一。

简介：Aim:Methodforthedeterninationoferythromycinethylsuccinale(EES)byionsuppressionchromatography(ISC)wasdevelopedandtheinfluencfactorsonISCwereinvestigated.Methods:AZorbaxSB-C18columnwasusedwith0.02mol.L^-1potassiumdihydrogenphosphate-acetonitrile(45:55)asmobilephase,ThepHandproportionofthemobilephaseshowedthegreatestinfluencesonretentionandselectivity.Therefore,thepHofmobilewasadjustedto6.8,thebhestacetonitrileproportionwas55%.Thecolumntemperaturewasmaintainedat(300±0.5)℃.AcetonitrilewasusedassolventforthesamplepreparationbecauseEESismorestableinit.Theflowratewas1.2mL.min^-1andUVdetectionwasperformedat210nm.Results:Underthesechromatographicconditions,themaincomponent(erythromycinAethylsuccinate)anditsrelatedsubstanceswereseparated.Thecalibrationcurveshowedgoodlinearityovertherangeof0.1-1.0mg.mL^-1,anditscorrelationcoefficientwas0.9998.Conclusion:Themethodisverysuitablefortheanalysisoferythromycinethylsuccinate.

简介：Aconitumspecies(Ranunculaceae),whichdistributewidelyinmiddleandlowerreachesoftheYangziRiver,northandsouthwestofChina,containhighlytoxicdiesterditerpeneAconitumalkaloids,especiallyhighcontentofaconitine.

简介：3α-bromo-epipicropodophyllinwaspreparedanditsinhibitionactivitiesagainstKBcellsandL1210leukemiacellsinvitroarehigherthanthoseofVP-16,awidelyuseddruginclinicatpresent.ThisisthefirsttimetointroducesubstitutionatC-3ofring-Cintheworkofmodifyingstructureofpodophyllotoxin.Itcanbetransformedeasilyto4β-hydroxy-2,3-ene-apopicropodophyllinunderbasiccondition,sothat,correspondingderivativesof2,3-ene-apopicropodophyllinwithsubstitutiononcarbon-4couldbesynthesized.Thiscompoundcanberegardednotonlyasaleadingcompoundtobemodifiedbecauseofitsantitumoractivities,butalsoasanintermediateforthestructuretransformation.

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简介：Lornoxicam(6-chloro-4-hydroxy-2-methyl-N-2-pyridyl-2H-thieno-[2,3-e]-1,2-thiazine-3-carboxamide-1,1-dioxide)ispersistasanon-steroidalanti-inflammatorydrugoftheoxicamclasswithanalgesic,anti-inflammatoryandantipyreticproperties.Afast,accurateandsensitivechromatographicmethodforestimationofLornoxicamwasdevelopedasnoofficialmethodavailablefordetection.ThechromatographicseparationemploysisocraticelutionbyutilizinganinertsilODS-C18,250mm×4.6mm,5μmcolumns.Mobilephaseconsistingofsolvent(40mLacetonitrileand60mL0.1Mphosphatebuffer(pH6.8wasadjustedwithtriethylamine))endowedataflowrateof1.0mL/min.Theanalytewasdetectedandquantifiedat290nmusingUVdetector.ThemethodwasvalidatedaccordingtoICHguidelines,illustratingtobeaccurate(recovery99.08%-101.13%)andprecise(intraday(0.27-1.32)andinterday(0.59-1.59))withinthecorrespondinglinearrange(10-60μg/mL)withr20.9992.

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简介：TherootbarkofMorusalbaL.orwhitemulberryiswidelyusedastraditionalmedicineinChina,JapanandKorea.Majorclassesandtypesofphenoliccompoundsisolatedfromtherootbarkareflavonoids(kuwanons,morusin,cyclomorusinandsanggenons),benzofurans(moracinsandmulberrofurans),andstilbenoids(mulberrosides).SomeoftheflavonoidsandbenzofuransareproductsofDiel-Aldertypeadducts.Otherclassesofcompoundsincludetriterpenes,phenolicacidsandcoumarins.Morusin,aprenylatedflavonoid,wasfirstisolatedfromtherootbarkofM.alba,andlaterfromtheleaf,stembarkandtwigoftheplant.Thepotentanti-cancerpropertiesofmorusinhaveattractedmuchattentionwithresearchon-goingandnewfindingsbeingpublished.Thecompoundinhibitsangiogenesis,tumourprogressionandtumourmigration,andtriggersapoptosis,cellcyclearrestandautophagyincolorectal,cervical,prostate,breast,hepatoma,pancreatic,glioblastoma,gastric,ovarianandlungcancercelllines.Theanti-canceractivitiesofmorusinareexecutedviavariousmoleculartargetsandsignallingpathways.Itisanticipatedthaton-goinginvitrostudieswillprogressgraduallytoinvivostudiesusinganimalmodelsbeforeeffortstowardsdrugdevelopmentcanbeinitiatedforclinicaltrials.

简介：AIMHumanglutathioneS-transferaseA1(GSTA1)isanimportantphaseⅡmetabolizingenzymeinvolvedinthemetabolismofmanytherapeuticdrugsandisresponsibleforthemetabolicdetoxificationofnumerouspromutagensandprocarcinogens.ThegeneticpolymorphismofGSTA1hasimportantimplicationsfordrugefficacyandcancersusceptibility.Inthisstudy,wedeterminedthedistributionofGSTA1geneticpolymorphisminMainlandChinese.Andwealsoinvestigatedwhetherthereexiststhepotentialphenotypealterationscausedbythegeneticpolymorphisminhuman.METHODSGenomicDNAwasex-tractedfromperipheralbloodof140Chinesepeopleand16livertissuesobtainedfromnon-liverishpatientswhounderwentpartialhepatectomy.AndthenthegenotypesofhumanGSTA1genewereanalyzedbypolymerasechainreaction-restrictedfragmentlengthpolymorphism(PCR-RFLP).

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简介：Lactivicin,anovelinhibitorofbacterialcellwallsynthesis,wasisolatedfromtheculturefil-tratesofmicroorganismYK-258andYK-422.Itexhibitsbiologicalactivitiessimilartothoseoftheβ-lactamantibiotics,althoughitdoesnothaveaβ-lactamringinitsmolecule.Sincethediscoveryoflactivicin,hundredsofitsderivativeshavebeensynthesized.Most

简介：AIMProstaglandinA1(PGA1)isacyclopentenoneprostaglandin.Recently,wereportedthatPGA1caninhibitexcitotoxin-inducedapoptosisofstriatalneuronsinvivoandrotenone-inducedapoptosisofculturedSH-SY5Ycells,suggestingthatPGA1mayhaveneuroprotectiveefficacy,possiblymediatedbyinhibitionofNF-kBactivation.ThepresentstudyevaluatedtheneuroprotectivepotentialofPGA1anditseffectonIKK/I(B/NF-kB/c-mycsignalingpathwayinratmodelsofpermanentfocalcerebralischemia.METHODSPermanentmiddlecerebralarteryocclusion(pMCAO)modelwasconstructedbyintraluminalsuturecannulationthroughtheinternalcarotidarteryinWistarrats.

简介：Aims：TotaltriterpenoidfromPrunellavulgarisL.（TTP）,knownasmedicinehad,hadapreventiveeffectagainsthepaticsteatosisinourpreviouswastoevaluatewhetherTTPcouldimproveliverfibrosisnismofactionofTTPonhepaticstellategrowthfactor（PDGF）.atraditionalChinesestudy.Ourobjectiveinratsandtoinvestigatethemecha-cell（HSC）proliferationinducedbyplatelet-derivedgrowthfactor（PDGF）.