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1、SynthesisandinVitroCytotoxicityofaNovelConjugateofPolyamideandPhospholipidChineseChemicalLettersVo1.17,No.5,PP599—602,2006http://www.imrn.ac.cn/joumal/cc1.htmlSynthesisandinVitroCytotoxicityofaNovelConjugateofPolyamideandPhospholipid599YiL1U,YuLinDENG,RongZHENG,PeiLong
2、ZHANG,HuiZHAI,KeZhongLIU,ChangJinZHU}DepartmentofAppliedChemistry,BeijingInstituteofTechnology,Beijing100081SchoolofLifeScienceandBiotechnology,BeijingInstituteofTechnology,Bering100081Abstract:Inordertoincreasethecellpenetrationanddecreasethecytotoxicityofthesynthetic
3、molecule,wedesignedandsynthesizedaDNA—bindingligand,whichWasaconjugateofpolyamideandphospholipid.WeexaminedthedifferencesintheeffectoncytotoxicitybetweentheCOniugateandthenativepolyamide.Asexpec~dthattheinvitrocytotoxicityoftheconjugateWasobviouslylowertllanthatofthena
4、tivepolyamideeitllerinHeLacellsorSH—SY5Yneuroblastomacells.Keywords:Polyamide,phospholipidconjugate,cytotoxicitySmallmoleculeswith也eabilitytotargetpredeterminedsequencesofDNAwouldbevaluabletoolsinmolecularbiologyandpotentiallyinhumanmedicine一.Syntheticpolyamidesconsist
5、ingofN—methylpyrrole(Py),N-methylimidazole(Im)havereceivedspecialattentionduetotheirhighDNAaffinity,sequencespecificity,andrelativelysmallsize..Forpolyamidestobeeffectiveingeneregulation,theymustreachtheirtargetDNAinsidethecell.Inthepresentstudies,wedesignedaconjugatei
6、nwhichaphosphafidyrlcholinewasattachedtothepolyamide.Thein~oduedonofmephOSpholipidwasexpectedtoimprovethepermeabilityofthesyntheticmoleculethroughthecellmembrane,guidethemovementtowardtonucleusincells,andtherebyreducethecytotoxicity.Thephospholipidisaprimarycomponentof
7、biologicallmembrane,andhasproventobenoncytotoxic.Inparticular,thehydrophobictailofthelipidispossibletogreatlybenefitthemovementoftheconjugatetowardtonucleusinceUs,andsubsequentlypromotetheinteractionwithnucleicDNA.ThetargetedCOnjugate13weresynthesizedasshowninScheme1.B
8、—Alanine2,3functionedasaspacerbothinpolyamide10andconjugate13.Primarily,DCCcouplingmethodwasusedinthesynthesis.Direct
