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1、內(nèi)皮抑素的多硫酸化肝素修飾及修飾物的二級(jí)結(jié)構(gòu)和抗新生血管生成活性研究譚海寧+川，王鳳山怡*(十山東大學(xué)藥學(xué)院，*山東大學(xué)國(guó)家糖工程技術(shù)研究中心，山東濟(jì)南250012fax:0086-531-88382548;E-mail:fswang@sdu.edu.cn)CovalentModificationofEndostatinwithPolysulfatedHeparinandTheirSecondaryStructureandAnti-angiogenesisActivityStudyHainingT
2、an%，YuhongLiu'''andFengshanWang*(InstituteofBiochemicalandBiotechnologicalDrug,SchoolofPharmaceuticalScience,ShandongUniversity,Jinan,250012,China,andNationalGlycoengineeringResearchCenter,ShandongUniversity,Jinan,250012,China.)Correspondingauthor.(Dr
3、FengshanWang)Tel:1-86-531-8838028&Fax:86-531-8838254&E-mail:fswang@sdu.edu.cn.'SchoolofPharmaceuticalScience,ShandongUniversity?'NationalGlycocnginccringResearchCenter,ShandongUniversity.ABSTRACTEndostatin(ES)isa20kDC-terminalfragmentofcollagenXVIIIth
4、atinhibitsendothelialcellproliferation,angiogenesisandthegrowthofseveralprimarytumors.However,someobstacleslimititsclinicaluse,suchasneedofhighdosetomaintainitsefficacy,expensive,andpoorstability,etc.Inordertoovercometheseshortcomings,wechemicallymodi
5、fiedESbypoly-sulfatedheparin(PSH).WestudiedtheinhibitionsonendothelialcellproliferationandangiogenesisofESanditsmodifiedproduct,respectively.ThechangesofthesecondarystructurewerealsostudiedbyCirculardichroism(CD)spectratoobtainbetterESderivatives.Ours
6、tudydemonstratedthatthemodifiedproducthasabetterheattolerancethanESandtheinhibitionsonendothelialcellproliferationandangiogenesisisbetterthanES.Theresultofsecondary-structureanalysissuggestedthatthepercentageofP-turninthemodifiedproduct,animportantfac
7、torontheactivityandstability,hadlittlechangecomparedwiththatofES.Collectively,thesefindingsdemonstratedthatthemodifiedproductofES(PSH-ES),withlittlesecondarystructurechange,hasabetterheatstabilityandanti-angiogenesisactivitythanES.INTRODUCTIONNewblood
8、vesselsnourishingtumorgrowthformbyangiogenesis,whichmakeinhibitionofvesselformationanexcellenttargetforcancertherapy.Endostatin(ESAbbreviations:BCS,bovinecalfserum;CAM,chorioallantoicmembraneassay;CD,Circulardichroism;CM-ILCarboxymethylcellulo
