简介：Pyrimidinederivativeshavebeenreportedasneuroprotectiveagentsusefulforthetreatmentofvariousneurodegenerativedisorders.Inthepresentstudy,severalpyrimidineanalogueshavebeenevaluatedasneuroprotectiveagentsinMorriswatermazemodel.Itwasobservedthatpyrimidinederivatives8–17considerablyimprovelearning,memory,andmovementdeficitsinanimalmodels.Biochemicalestimationsofbrainserumoftreatedanimalsrevealedsuppressionofoxidativeandnitrosativestress,acetylcholinesteraseactivity,andotherparameterswhichleadstoneurodegenerationofbrain.Ofallthepyrimidinederivatives,thiomorpholinederivative8andpiperazineethanolderivative17werefoundtobethemostactiveneuroprotectiveagentsandproducedeffectscomparabletostandarddrugrivastigmineintermsofbehavioral,biochemical,andmolecularaspects.

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简介：Objective:Tostudytheanti-inflammatoryactivityandtissuedistributionpatternsofintravenousemulsionofdexamethasoneacetateinmice.Methods:Theanti-inflammatorysolutionforinjectionandLimethasone(Jepaneseproduct)givenintravenouslywereevaluatedbyusingthepreformedcarrageenangranulomapouchmethodinrats.Results:Theanti-inflammatoryactivityofdexamethasoneacetateemulsionatlowdoseof0.05mg.kg1wasaspotentasdexamethasonesodiumphosphatesolutionathighdoseof0.3mg.kg1.Thedistributionpatternsinmicetissuesof[^3H]dexamethasoneacetateemulsionand[^3H]dexamethasonesodiumphosphatesolutioninmiceweremarkedlydifferent.Dexamethasoneacetateemulsionshowedamuchhigherconcentrationintheliver,spleen,lung,andinflamedtissues,whereasdexamethasonesodiumphosphatehadahighconcenti,moninthemusclesofvastuslateralis.Theseresultsmayindicatethatdexamethasoneincoporatedinlipidemulsionwastakenupbythereticuloendothelialsystemandinflammatorycellsmuchmorethandexamethasonesodiumphosphatesolution.Conclusion:Whendexamethasoneacetatewasincorporatedinemulsion,thedistributionpatternsintissueswerechangedandtheyhadastrongeranti-inflammatoryactivity.

简介：Ｔｈｅｓｙｎｔｈｅｓｉｓｏｆｐｏｒｐｈｙｒｉｎｎｉｔｒｏｇｅｎｍｕｓｔａｒｄｓｆｒｏｍｄｅｕｔｅｒｏｐｏｒｐｈｙｒｉｎａｎｄ３，８ｄｉａｌｋｙｌｏｘｙｈｅｍａｔｏｐｏｒｐｈｙｒｉｎｍｅｔｈｙｌｅｓｔｅｒｓｔｈｒｏｕｇｈｒｅｄｕｃｔｉｏｎ，ｂｒｏ...

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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：AIMMacrophagemigrationinhibitoryfactor(MIF)isapro-inflammatorycytokineinvolvedinthepathogenesisofavarietyofautoimmuneandinflammatorydiseases,includingarthritis,glomerulonephritis,Gram-positiveandGram-negativesepsis,andatherogenesis.RecentstudiesshowedthatCD74(antigen-associatedinvariantchainⅡ)isahigh-affinitymembrane-bindingproteinforMIF.ThepurposeofthepresentstudywastoexpresstherecombinanthumanCD74inE.coliandinhibittheactivityofMIFbyusingrecombinantCD74invitro.

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简介：Recently,ithasbeenreportedthattheluteolyticac-tionwasthemainmechanismoftheterminationofearlypregnancybycontraceptivest.Inaddition,someestro-genreceptorligandssuchasdroloxifenehavebeenshowntoinhibitthegrowthofculturedratlutealcells.Ithasbeenknownthat2-phenylindolederivativescouldcompetewithestradiolfortheestrogenreceptor.Theseresultspromptedustodesignandsynthesizethefollow-ingsixnew3-oxamoyl-2-phenylindolecompounds1a-fandtesttheireffectsonthegrowthoflutealcells,aimingatseekingnewleadcompoundspossessingantifertilityactivities.