天然产物研究与开发NatProdResDev2013,25:662-666文章编号:1001-6880(2013)5-0662-05苦瓜籽蛋白MAP30的聚乙二醇化学修饰及抗肿瘤活性研究何义国+,赵兴秀,邓静,吴华昌‘四川理工学院,自贡643000摘要:采用硫酸铵分级沉淀、SP.SepharoseFF离子交换层析和BlueSepharoseCL-6B亲和层析获得苦瓜蛋白MAP30;采用(mPEG)2-Lys-NHS修饰MAP30;对修饰后的MAP30.PEG结合物与MAP30的抗肿瘤活性进行了比较分析。结果发现:MAP30对多数肿瘤细胞株具有明显的抑制作用,而且抑制效果在一定范围内具有剂量和时效依赖关系。但是在相同条件下,MAF30对人正常胚肺二倍体细胞株WI-38的毒性极小。MAP30和MAP30.PEG结合物对小鼠黑色素瘤(B16)、人宫颈癌细胞(Hela)和人表皮癌细胞(A431)细胞均表现出抑制作用,且这种作用在一定范围内呈时效和量效依耐性。但在相同浓度下PEG-MAP30对小鼠黑色素瘤(B16)、人官颈癌细胞(Hela)和人表皮癌细胞(A431)的抑制作用低于MAP30,约占65%一70%左右。关键词:苦瓜籽;核糖体失活蛋白(MAP30);MAP30.PEG结合物;抗肿瘤中图分类号:R73文献标识码:AStudyontheAntitumorActivityofMAP30andPEG.Ⅳ丛P30fromBitterMelonSeedsHEYi-guo+,ZHAOXing-xiu,DENGJing,WUHua—changSichuanUn&emiffofScience&Engineering,Zigong,Sichuan643000,ChinaAbstract:Aprotein,namelyMAP30,wasiselatedandpurifiedfromtheseedsofbittermelonbyacetonefractionafionandchmmatographiesonSuperdex75andBlueSepharoseCL-6B.Theanti—tumoractivityofMAP30WaSstudiedonsey.eraltumorcelllines.ThestructureofMAP30wasmodifiedwith(mPEG),.Lys.NHS.andtheanti.tumoractivityofPEG.MAP30WasthencomparedtOthatofMAP30.TheresultsrevealedthattheMAP30WasactivetOmanytumorcelllines.anditexhibitedinthedose—dependentandtime.dependentmanner8.LittlecytotoxieeffectonWI.38WasfoundunderthessJrleassaycondition.Theanti.tumoractivityassayshowedthatbothMAP30andPEG.MAP30exhibiteddose.dependentandtime.dependentinhibitionagainstB16ceHs,HelaceUsandA431ceUs,andtheinhibitionratesofPEG.MAP30againstB16ceHs.HelacellsandA431eeHs流vitrowerearound60%-70%.Keywords:seedsofbittermelon;MAP30;MAP30.PEG;anti.tumor1990年,美国科学家首次发现MAP30(Me—mordicaanti—HIVproteinof30kD,I型核糖体失...