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简介：Naturalproductshavegainedpopularityworldwideforpromotinghealthcare,aswellasdiseaseprevention.Alkaloidsareimportantchemicalcompoundsthatserveasarichreservoirfordrugdiscovery.Severalalkaloidsisolatedfromnaturalherbsexhibitantiproliferation,antibacterial,antiviral,insecticidal,andantimetastaticeffectsonvarioustypesofcancersbothinvitroandinvivo.Thispaperfocusesonthenaturally-derivedalkaloidssuchasberberine,matrine,piperine,fritillarine,andrhynchophylline,etc.,andsummarizestheactionmechanismsofthesecompounds.Basedontheinformationintheliteraturethatissummarizedinthispaper,theuseofalkaloidsasdrugsisverypromising,butmoreresearchandclinicaltrialsarenecessarybeforefinalrecommendationsonspecificalkaloidscanbemade.Followingthis,itishopedthatasaresultofthisreview,therewillbeagreaterawarenessoftheexcellentpromisethatnaturalalkaloidsshowforuseinthetherapyofdiseases.

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：CymbopogoncitratusisawidelydistributedperennialherbbelongingtothePoaceaefamilyandhasbeenextensivelyconsumedforitsmedicinal,cosmetic,andnutritionaleffectsforcenturies.Alargenumberofreportshavebeenpublisheddescribingthepharmacological,biological,andtherapeuticactionsofthisherb.Inthisreview,wesummarizedtheliteraturesonrelatedstudies(uptoJanuary,2014)thathighlightedthepharmacologicandbiologicaleffectsofthemajorphytochemicalsisolatedfromC.citratusextractsanditsessentialoil.ThecomponentsoftheessentialoilsfoundinC.citratushaveasimilarpharmacokineticproperties,includingabsorption,distribution,metabolism,andexcretion.Theyarequicklyabsorbedfollowingoral,pulmonary,anddermaladministration.Basedonthepublishedreports,itcanalsobeinferredthat,afterabsorptionfromthesmallintestine,somephytochemicalsinC.citratuscanundergooxidation,glucuronidation,sulfation,and/orO-methylation.Excretionisthroughurine,fecesand/orexpiredvolatiles.ThebiotransformationreactionsofC.citratusbioactiveconstituentsareessentialforitsrelativelysafeconsumptionandtherapeuticapplications.ThedataavailablesofarwarrantfurtherstudiesevaluatingC.citratuspharmacokinetics.ReliablepharmacokineticdatainhumanswouldbecriticalforabetterunderstandingofthethesystemichandlingofC.citratus.

简介：Acompetitiveenzyme-linkedimmunosorbentassay(ELISA)wasdevelopedtodetermineruscogenin(RUS)byusingthemonoclonalantibody(McAb).ThemonoclonalantibodyagainstRUS,secretedfromtheestablishedhybridomacelllines,wasidentifiedasbeingoftheIgG1isotype.TheMcAbexhibitedhighspecificitytoRUS,showingaveryslightcrossreactivitywithdiosgenin(15.7%),andnocross-reactivitytosarsasapogenin,diammoniumglycyrrhizinate,oleanolicacidandnotoginsenosideR1.TheestablishedELISA,atanIC50valueof157.55ng.mL-1andadetectionlimit(IC20)of20.57ng.mL-1,wascomparedwithHPLCanalyses,andagoodcorrelationbetweenELISAandHPLC-ELSDanalysesofRUSintheextractofRadixOphiopogoniswasobtained.TheexperimentaldataindicatedthattheELISAmethodexhibitsmoreadvantagesoverHPLC-ELSD,suchaslowdetectionlimit,highspecificity,lowbackground,andnorequirementforsamplepre-treatment,andismoresuitableforthedeterminationofnaturalcomponentsinChinesetraditionalmedicinesandinbiologicalsamplesforpharmacokineticstudies.

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.