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1、BiochemicalPharmacology82(2011)1832–1842ContentslistsavailableatSciVerseScienceDirectBiochemicalPharmacologyjournalhomepage:www.elsevier.com/locate/biochempharmEffectsofthenovelvasculartargetingagentMDS-11Pontumorvascularityanditsantitumoractivitya,1a,1aaaaaZhi-Ti
2、ngDeng,TengFeng,PengWang,XinQi,Xue-HongChen,Ying-XiaLi,Chun-LiSong,b,**,a,*Mei-YuGengJingLiaKeyLaboratoryofMarineDrugs,MinistryofEducation,SchoolofMedicineandPharmacy,OceanUniversityofChina,5Yu-ShanRoad,Qingdao266003,ChinabDivisionofAntitumorPharmacology,StateKeyL
3、aboratoryofDrugResearch,ShanghaiInstituteofMateriaMedica(SIMM),ChineseAcademyofSciences,Shanghai201203,ChinaARTICLEINFOABSTRACTArticlehistory:Vasculardisruptingagentsshowselectiveeffectsontumorestablishedvasculature,andachieveReceived9July2011encouragingresultsinb
4、othpre-clinicalandclinicalexperiments.Inthepresentstudy,weinvestigatedAccepted31August2011theAvailableeffectsofanewCA4derivativeMDS-11anditsprodrugMDS-11Ponvasculardisruptingactivityinonline6September2011vitroandinvivo.Surfaceplasmonresonance(SPR)andtubulinpolymer
5、izationassayshowedthatMDS-11interactedwithtubulindirectlyandinhibitedtubulinpolymerizationinacellfreesystem,andKeywords:westernVascularblotassayfurthercon?rmedtheactioninthecellularlevel.MDS-11wasfoundtosigni?cantlydisruptingagentsdisruptMDS-11Pthemicrotubulinskel
6、etoninproliferatingHUVECsthanquiescentonesdeterminedbyconfocalmicroscopy.Furthermore,MDS-11wasfoundtodamagetheHUVEC-formedtubequickly,butdidnotAntitumorin?uencestructuresofmicrovesselsfromaorticringpossessingpericytesandsmoothmusclecellsuntilCA4derivativeVasculari
7、ty3htreatment.InA549xenograftmice,immunohistochemistrystainingoftumorsectionsrevealedthatasingledoseofMDS-11Pledtolargeareasofnecrosiswithintumorandreducedthenumberoftumorvessels,whichwasconsolidatedbyperfusedvascularvolumeassay.PharmacokineticstudiesofMDS-11Pindi
8、catedthatMDS-11Prapidlyconvertedtotheactiveform,MDS-11,andexhibitedamuchfastereliminationinmice.TheantitumoranalysisusingH22andA549micexenograftmodelsre
