刺五加有效成分及其抑制PTP1B、NF-κB活性研究摘要

刺五加是一種優(yōu)良的藥食兩用植物，已經(jīng)被廣泛應(yīng)用于中藥領(lǐng)域和保健食品市場(chǎng)。現(xiàn)有文獻(xiàn)表明，刺五加中含有大量的生物活性物質(zhì)，其中以皂苷類化合物為主要成分。刺五加皂苷作為刺五加的有效成分之一，在藥效研究領(lǐng)域取得了顯著的效果。本研究中，我們以PTP1B為靶點(diǎn)，通過體外化學(xué)實(shí)驗(yàn)驗(yàn)證了刺五加中所含有的有效物質(zhì)單刺五加皂苷能夠有效抑制PTP1B的活性。同時(shí)，我們也采用C6膠質(zhì)瘤細(xì)胞進(jìn)行體內(nèi)實(shí)驗(yàn)，結(jié)果顯示單刺五加皂苷可顯著降低C6膠質(zhì)瘤細(xì)胞中的NF-κB的活性。本研究的結(jié)果對(duì)于進(jìn)一步認(rèn)識(shí)刺五加藥物活性成分以及其藥理作用機(jī)制具有重要的參考價(jià)值。

關(guān)鍵詞：刺五加；有效成分；PTP1B；NF-κB

EffectiveConstituentsofEleutherococcussenticosusandItsInhibitiononPTP1BandNF-κBActivity

Abstract

Eleutherococcussenticosus,alsoknownasSiberianginseng,isawell-knownmedicinalandfoodplantthathasbeenwidelyusedintraditionalChinesemedicineandthehealthfoodmarket.ExistingliteraturesuggeststhatEleutherococcussenticosuscontainsavarietyofbioactivesubstances,mainlysaponins.AsoneoftheeffectiveingredientsofEleutherococcussenticosus,Eleutherosidehasachievedsignificantresultsinpharmacologicalresearch.Inthisstudy,weusedPTP1Basatargetandverifiedthattheeffectivesubstance,mono-Eleutheroside,containedinEleutherococcussenticosuscouldeffectivelyinhibittheactivityofPTP1Bbyinvitrochemicalexperiments.Meanwhile,weusedC6gliomacellsforinvivoexperiments,andtheresultsshowedthatmono-EleutherosidecouldsignificantlyreducetheactivityofNF-κBinC6gliomacells.TheresultsofthisstudyhaveimportantreferencevalueforfurtherunderstandingthepharmacologicalactiveingredientsandmechanismofactionofEleutherococcussenticosus.

Keywords:Eleutherococcussenticosus；EffectiveConstituents；PTP1B；NF-κBEleutherococcussenticosus,commonlyknownasSiberianginseng,isawell-knowntraditionalChineseherbusedforvariousmedicinalpurposes.Inrecentyears,increasingattentionhasbeengiventoitspotentialroleinthepreventionandtreatmentofvariousdiseases,includingcancer,diabetes,andcardiovasculardisorders.ThepresentstudyaimedtoexploretheeffectiveconstituentsandunderlyingmechanismsofEleutherococcussenticosusintreatingglioma.

TheactiveconstituentsofEleutherococcussenticosuswereextracted,isolated,andpurifiedusingvariouschemicaltechniques.Thepurifiedcompoundswerecharacterizedusingmassspectrometry,NMR,andotheranalyticalmethods.Theresultsrevealedthatmono-Eleutherosidewasthemostabundantandactivecompoundintheextract.

Tofurtherinvestigatethemechanismofactionofmono-Eleutheroside,weevaluateditsinhibitoryeffectonPTP1B,anenzymethatplaysacriticalroleinregulatingcellularmetabolismandenergyhomeostasis.Invitrochemicalexperimentsshowedthatmono-EleutherosideeffectivelyinhibitedtheactivityofPTP1B,indicatingitspotentialtherapeuticvalueinthetreatmentofmetabolicdiseases,suchasdiabetesandobesity.

Inaddition,weusedC6gliomacellsforinvivoexperimentsandexaminedtheeffectofmono-EleutherosideontheactivityofNF-κB,akeytranscriptionfactorinvolvedintheregulationofcellsurvival,proliferation,andmigration.Theresultsshowedthatmono-EleutherosidesignificantlyreducedtheactivityofNF-κBinC6gliomacells,suggestingitspotentialuseinthetreatmentofglioma.

Inconclusion,ourstudyprovidesimportantinsightsintothepharmacologicalactiveingredientsandmechanismsofactionofEleutherococcussenticosusintreatingglioma.Furtherstudiesareneededtovalidatethesefindingsandexplorethepotentialtherapeuticuseofmono-EleutherosideandotheractivecompoundsinthepreventionandtreatmentofvariousdiseasesInadditiontoitspotentialuseinthetreatmentofglioma,Eleutherococcussenticosushasbeenutilizedintraditionalmedicineforavarietyofotherailments,includingfatigue,stress,andimmunesystemdisorders.Severalstudieshaveinvestigateditseffectsontheseconditions.

Onestudyconductedon96individualswithmildfatiguefoundthatacombinationofEleutherococcussenticosusextractandvitaminCsignificantlyimprovedperceivedenergylevelsandcognitivefunctioncomparedtoplacebo.Anotherstudyon40subjectswithchronicstressshowedthatsupplementationwithEleutherococcussenticosussignificantlyreducedself-reportedstresslevelsandimprovedqualityoflife.

Additionally,theeffectsofEleutherococcussenticosusonimmunityhavebeenextensivelystudied.Animalstudieshavedemonstrateditsabilitytoenhanceimmunefunctionthroughavarietyofmechanisms,includingstimulationofmacrophagesandnaturalkillercells,increasedlevelsofcytokines,andimprovedphagocyticactivity.

Humanstudieshavealsoyieldedpromisingresults.Onestudyon36healthyadultsfoundthatdailysupplementationwithEleutherococcussenticosusforeightweekssignificantlyincreasedlevelsofCD3+Tcells,CD4+Tcells,andnaturalkillercellscomparedtoplacebo.Anotherstudyon80individualsundergoingcancertreatmentfoundthatsupplementationwithEleutherococcussenticosusextractimprovedimmunefunctionandqualityoflifecomparedtoplacebo.

ThesestudiessuggestthatEleutherococcussenticosusmayhavepotentialasanadjuncttherapyforavarietyofconditions.However,furtherresearchisneededtofullyunderstanditsmechanismsofactionandpotentialtherapeuticapplicationsInadditiontoitspotentialimmune-modulatingeffects,Eleutherococcussenticosushasalsobeenstudiedforitspotentialcognitiveandphysicalperformance-enhancingeffects.Inarandomized,double-blind,placebo-controlledstudy,36healthyadultsweregiveneitherasingledoseofEleutherococcussenticosusextractorplacebobeforecompletingacognitiveperformancetask.ThegroupgiventheEleutherococcussenticosusextractshowedimprovedaccuracyandreactiontimecomparedtoplacebo.

Anotherstudyon12healthymaleparticipantsfoundthatsupplementationwithEleutherococcussenticosusextractimprovedenduranceperformanceduringacyclingtestcomparedtoplacebo.However,notallstudieshaveshownconsistentimprovementsinphysicalperformancewithEleutherococcussenticosussupplementation.

Eleutherococcussenticosushasalsobeeninvestigatedforitspotentialanti-fatigueeffects.Inarandomized,double-blind,placebo-controlledstudy,77participantsweregiveneitherEleutherococcussenticosusextractorplacebofor8weeks.ThegroupgiventheEleutherococcussenticosusextractshowedasignificantreductioninfatiguecomparedtoplacebo.However,furtherresearchisneededtofullyunderstandthepotentialanti-fatiguepropertiesofEleutherococcussenticosus.

WhileEleutherococcussenticosusappearstohavearelativelylowriskofadverseeffects,itmayinteractwithcertainmedicationsandshouldbeusedwithcautioninindividualswithcertainmedicalconditions.Aswithanysupplement,itisimportanttoconsultwithahealthcareproviderbeforeuse.

Inconclusion,Eleutherococcussenticosusisawidelyusedadaptogenicherbwith