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中药化学成分肠吸收研究中Caco-2细胞模型和标准操作规程的建立作者：杨秀伟，杨晓达，王莹，马莲，张悦，杨晓改，王夔，Xiu-weiYANG，Xiao-daYANG，YingWANG，LianMA，YueZHANG，Xiao-gaiYANG，KuiWANG作者单位：北京大学药学院天然药物及仿生药物国家重点实验室,北京,100083刊名：中西医结合学报英文刊名：JOURNALOFCHINESEINTEGRATIVEMEDICINE年，卷(期)：2007，5(6)被引用次数：11次参考文献(33条)1.杨秀伟基于体内过程的中药有效成分和有效效应物质的发现策略[期刊论文]-中国中药杂志2007(05)2.杨秀伟基于体内过程的中药毒性成分和毒性效应物质的发现策略[期刊论文]-中华中医药杂志2007(02)3.杨秀伟中药实验医学研究中的关键基础科学问题[期刊论文]-中西医结合学报2005(02)4.杨秀伟中药成分的肠内和肝内行为与中药有效成分的确定2004(zk)5.杨秀伟.郝美荣.服部征雄中药成分代谢分析20036.周昕药物吸收体外研究方法的概述[期刊论文]-中国临床药理学与治疗学杂志2006(04)7.TurowskiGA.RashidZ.HongFGlutaminemodulatesphenotypeandstimulatesproliferationinhumancoloncancercelllines1994(22)8.RashidZ.BassonMDTopoisomeraseⅡinhibitiondifferentiallymodulatesCaco-2intestinalepithelialcellphenotype1996(01)9.YeeSYInvitropermeabilityacrossCaco-2cells(colonic)canpredictinvivo(smallintestinal)absorptioninman-factormyth1997(06)10.ChongS.DandoSA.MorrisonRAEvaluationofbiocoatintestinalepitheliumdifferentiationenvironment(3-dayculturedCaco-2cells)asanabsorptionscreeningmodelwithimprovedproductivity1997(12)11.GaoJN.HuggerED.Beck-WestermeyerMSEstimatingintestinalmucosalpermeationofcompoundsusingCaeo-2cellmonolayer200012.WalleUK.FrenchKL.WalgrenRATransportofgenistein-7-glucosidebyhumanintestinalCaco-2cells:PotentialroleforMRP21999(01)13.TianXJ.YangXD.WangKTheeffluxofflavonoidsmorin,isorhamnetin-3-O-rutinosideanddiosmetin-7-O-beta-D-xylopyranosyl-(1-6)-beta-D-glucopyranosideinthehumanintestinalcelllineCaeo-22006(08)14.YangXW.GuoQM.WangYIntestinalpermeabilityofantivirusconstituentsfromthefruitsofEucalyptusglobulusLabill.inCaco-2cellmodel2007(04)15.田莉.杨秀伟.王莹顺式-和反式-阿霍烯在Caco2细胞模型中的体外摄取、转运和外排特性[期刊论文]-药学学报2007(01)16.YangXG.YuanLan.WangKComparisonofintestinalabsorptionoftwoinsulinmimicvanadylcomplexesusingCaco-2monolayersasmodelsystem[期刊论文]-ChineseScienceBulletin2003(09)17.ZhangY.YangXD.WangKThepermeabilityandcytotoxicityofinsulin-mimeticvanadium(Ⅲ,Ⅳ,Ⅴ)-dipicolinatecomplexes2006(01)18.BohetsH.AnnaertP.MannensGStrategiesforabsorptionscreeningindrugdiscoveryanddevelopment2001(05)19.张正全.陆彬口服结肠定位给药系统新进展2000(01)20.KomuraH.ShigemotoY.KawaharaIHighthroughputscreeningofpharmacokinetiesandmetabolismindrugdiscovery(Ⅲ)-investigationonin-silicomodelformembranepermeabilityandCYPIA2inhibition2005(01)21.牟永平.吴刚.乔秀文手性金属配合物d,l-[Ni(phen)3]2+经Caco-2细胞单层模型的吸收转运[期刊论文]-包头医学院学报2006(04)22.Schmiedlin-RenP.T'hummelKE.FisherJMExpressionofenzymatieallyactiveCYP3A4byCaco-2cellsgrownonextracellularmatrix-coatedpermeablesupportsisinthepresenceoflalpha,25-dihydroxyvitaminD31997(05)23.AnnaertP.KingetR.NaesensLTransport,uptake,andmetabolismofthebis(pivaloyloxymethyl)esterprodrugof9-(2-phosphonylmethoxyethyl)adenineinaninvitrocellculturesystemoftheintestinalmucosa(Caco-2)1997(04)24.VanGelderJ.AnnaertP.NaesensLInhibitionofintestinalmetabolismoftheantiviralesterprodrughis(POC)-PMPAbynature-identicalfruitextractsasastrategytoenhanceitsoralabsorption:aninvitrostudy1999(07)25.BartelsH.KorsiakE.DanielHTransportactivityoftheMDR1-geneproductinmonolayersofCaeo-2cells199426.DibasA.WoodJ.MiaAJTheATP-depletingreagentiodoacetamideinducesthedegradationofproteinkinaseCalpha(PKCalpha)inLLC-PK1pigkidneycells1997(17)27.TsuruoT.IidaH.TsukagoshiSOvercomingofvincristineresistanceinP388leukemiainvivoandinvitrothroughenhancedcytotoxicityofvincristineandvinblastinebyverapamil1981(05)28.RoepePDTheP-glycoproteineffluxpump:howdoesittransportdrugs?1997(03)29.LeierI.JedlitschkyG.BuchholzUTheMRPgeneencodesanATP-dependentexportpumpforleukotrieneC4andstructurallyrelatedconjugates1994(45)30.JedlitschkyG.LeierI.BuchholzUATP-dependenttransportofglutathioneS-conjugatesbythemultidrugresistance-associatedprotein1994(18)31.BarrandMA.BargrijT.NeoSYMultidrugresistanceassociatedprotein:AproteindistinctfromP-glycoproteininvolvedincytotoxicdrugexpulsion1997(05)32.ChenJ.LinH.HuMAbsorptionandmetabolismofgenisteinanditsfiveisoflavoneanalogsinthehumanintestinalCaco-2model2005(02)33.NikolicD.LiY.ChadwickLRInvitrostudiesofintestinalpermeabilityandhepaticandintestinalmetabolismof8-prenylnaringenin,apotentphytoestrogenfromhops(HumuluslupulusL.)2006(05)相似文献(10条)1.期刊论文郑艳.杨秀伟茯苓三萜类化合物在人源Caco-2细胞单层模型中的吸收研究-中国中药杂志2008,33(13)目的:研究中药茯苓中3-表去氢土莫酸(3-epidehydrotumulosicacid,EDHTA)、猪苓酸C(polyporenicacidC,PPAC)和6α-羟基猪苓酸C(6α-hydroxypolyporenicacidC,HPPA)在人肠的吸收.方法:采用人源结肠腺癌细胞系Caco-2细胞单层模型研究EDHTA,PPAC和HPPA由绒毛面(AP侧)到基底面(BL侧)、BL侧到AP侧2个方向的转运过程.应用高效液相色谱法分离、紫外检测法对上述3个化合物进行定量分析,计算转运参数和表观渗透系数,并与阳性对照药普萘洛尔和阿替洛尔进行比较.结果:EDHTA,PPAC和HPPA由AP侧到BL侧的表观渗透系数(Papp)值分别为(9.99±1.08)×10-6、(10.06±0.53)×10-6和(3.32±0.66)×10-6cm·s-1;由BL侧到AP侧的Papp值分别为(17.76±0.91)×10-6、(19.23±1.16)×10-6和(8.19±0.57)×10-6cm·s-1.与本实验中在Caco-2细胞单层模型上呈良好吸收的阳性对照药普萘洛尔的Papp值(1.45×10-5cm·s-1)和呈难于吸收的阳性对照药阿替洛尔的Papp值(4.22×10-7cm·8-1)比较,EDHTA和PPAC与普萘洛尔在同一数量级;HPPA介于普萘洛尔和阿替洛尔之间.EDHTA、PPAC和HPPA的PappA→B/PappB→A比值分别为0.56,0.52和0.41;EDHTA,PPAC和HPPA外流分别是摄取的1.78,1.91,2.47倍.结论:EDHTA,PPAC和HPPA可以通过小肠上皮细胞被动吸收进入体内,EDHTA和PPAC属于良好吸收的化合物;HPPA属于中等吸收的化合物.EDHTA、PPAC和HPPA在Caco-2细胞单层模型中的转运可能存在外流机制.2.学位论文邓长凤葛根素口服微乳生物利用度及其吸收机制初步研究2009目的:通过葛根素口服微乳在大鼠体内的生物利用度以及在Caco-2细胞模型中摄取特性的研究，初步探讨其吸收机制。方法:1葛根素口服微乳