欢迎来到天天文库
浏览记录
ID:55404767
大小:395.67 KB
页数:5页
时间:2020-05-15
《芍药苷对乌头碱在Caco-2细胞模型上转运行为的影响研究.pdf》由会员上传分享,免费在线阅读,更多相关内容在行业资料-天天文库。
1、-322·WORLDCHINESEMEDICINEMar.2015,Vo1.10,No.3芍药苷对乌头碱在Caco一2细胞模型上转运行为的影响研究郑琴周欢熊文海王佳胡鹏翼杨明(江西中医药大学现代中药制剂教育部重点实验室,南昌,330004)摘要目的:研究芍药苷对乌头碱在Caco一2细胞模型转运行为的影响。方法:以鸟头碱累积转运量及表观渗透系数Papp值为指标,采用高效液相色谱法对乌头碱含量进行检测,考察不同浓度、不同孵育时间、不同方向乌头碱在Caco-2细胞上的转运行为,以及与芍药苷不同配伍后转运行为的变化,并考察P—gP
2、抑制剂存在与否对鸟头碱转运行为的影响。结果:鸟头碱累积转运量与给药浓度、孵育时间呈正相关,不同浓度乌头碱Papp值均大于1×10I¨am·s~,且保持恒定,无统计学意义,但外排作用明显强于吸收,外排比接近1.5。在P—gP抑制剂维拉帕米存在条件下乌头碱转运量显著增加。当乌头碱与芍药苷配伍比例为1:60时,乌头碱转运量显著减小。结论:乌头碱为吸收良好的一类药物,以被动转运为主,但仍存在外排蛋白P—gP的参与。"-3芍药苷配伍乌头碱达到一定比例时,对乌头碱的肠吸收具有显著的抑制作用。关键词乌头碱;Caco一2细胞;芍药苷;转运
3、;配伍;P—gp抑制剂EfectsofPaeoniflorinOilAconitineTransportBehaviorinCaco-2CellModelZhengQin,ZhouHuan,XiongWenhai,WangJia,HuPengyi,YangMing(KeyLabofModernPreparationofTraditionalChineseMedicine,MinistryofEducation,JiangxiUniversityofTraditionalChineseMedicine.Nanchang33O
4、004.China)AbstractObjective:ToexploreeffectsofPaeoniflorinonAconitinetransportbehaviorinCacCo一2cellmonolayermode1.Meth—ods:Bi-directiontransportbehaviorsofAconitineandeffectsofconcentrations,incubationtimeonAconitinetransportbehaviorwerestudiedonCaco-2celI.Theconc
5、entrationofAconitinewasanalyzedonareverse.phaseHPLCcolumn.Pappvalueandtotaltransportamountwerecalculated.TheeffectofP,gPinhibitoronAconitinetransportbehaviorwasinvestigatedaswel1.Results:ThetransportvolumeofAconitinewascorrelatedpositivelywiththeincubationtimeandd
6、rugconcentration.Therewerenosignifi—cantdifferencesinthePappvalueattheselectedconcentrations.Bi—directionaltransportstudiesonAconitineshowedthattheratioofpermeabilitvintheBasolateraltoApicaldirectionisabout1.5timesthatoftheApicaltoBasolateraldirection.ThePappvalue
7、ofAconitinewasabove1×10~cm·s~.ThetransportamountofAconitinewassignificantlyincreasedinthepresenceofVera—pamil.ThetransportamountofAconitinewassignificantlyreduced,whentheratioofAconitineandPaeoniflorincompatibilitywas1:60.Conclusion:TheresultssuggestedthatAconitin
8、ecouldbeeasilyabsorbedontheCaco-2monolayermodelbyapassivetransportation.However,eff[uxproteinmayalsoplayalimportantroleinthetransportprocess.Whenthecomp
此文档下载收益归作者所有