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1、肼基烟酰胺基酰肼基-叶酸的合成与动物显像中国医学科学院ACrAACADEMIAEMEDICAESICAE叶酸受体肿瘤显像剂mTc.肼基烟酰胺基酰肼基-叶酸的合成与动物显像刘丽琴#,王世真,李方,滕宝,王克栈,邱飞蝉(中国医学科学院中国协和医科大学北京协和医院核医学科,北京100730)?论着?摘要:目的研究叶酸受体肿瘤显像剂∞Tc.肼基烟酰胺基酰肼基.叶酸(‰Tc.HYNIC.叶酸)的合成,生物分布及其动物显像.方法以叶酸为原料经过多步反应合成叶酸衍生物HYNIC.叶酸,以该衍生物为配体,并以三(羟甲基)甲基甘氨酸和三苯甲基膦三磺酸钠为共配体进行∞T
2、c标记,对其放化纯度,稳定性进行分析,对正常小鼠及荷瘤小鼠的体内生物分布和荷瘤小鼠的相机显像进行研究.结果配体HYNIC.叶酸的结构经核磁共振氢谱和质谱进行确认,经标记后,放化纯度为96%,体外稳定性好.在荷瘤小鼠中的生物分布和显像结果表明,∞Tc-HYNIC-叶酸在肿瘤中有较高的浓集,单位质量摄取率为5.620±0.753.除在肾中摄取较高(单位质量摄取率为41.959±6.759)外,其他非靶组织中摄取均较低.结论Tc-HYNIC-叶酸有望成为性能良好的叶酸受体肿瘤显像剂.关键词:叶酸受体;叶酸衍生物;同位素标记;生物分布;显像中圈分类号:R81
3、7.9文献标识码:A文章编号:1000-503x(2o06)o6.0786.04SynthesisandAnimalImagingofTc-Hydrazinonicotinamide.Folate嬲aNewFolateReceptor-TargetedTumorImagingAgentLIULi?qin,WANGShi-zhen,LIFang,TENGBao,WANGKe-zhan,QIUFei.chan(DepartmentofNuclearMedicine,PUMCHospital,CAMSandPUMC,Beijing100730,China)
4、ABSTRACT:ObjectiveThesynthesis,biodistribution,andanimalimagingof99Tc-hydrazinonicoti-namide-fohte(咖Tc-HYNIC-Folate)werestudieda8afolmereceptor-targetedtumorimagingagenLMethodsHYNIC-Fohtewassynthesizedbyamuti-stepreactionandradiolabeledwith钟Tcusingtricineandtrisodiumphenylphosp
5、hine-3,3',3"-trisulfonate(ⅡrS)a8coligands.111eradiechemiealpurityandstabihtyof99Tc-HYNIC-Folatewasmeasured.rI'Ilebiodistributionsof钟Tc-HYNIC-Folateinnormalmiceandtumor-bearingmiceweredetected.Whole-bodygammaimagingWasperformedusinganathymicmousetumorxenograftmode1.ResultsrI'Ile
6、ligandHYNIC-FolateWassuccessfuHysynthesizedandcharacterizedbyhydrogennuclearmag-neticresonance(HNMR)andmassspectrometry(MS).rI'Ileradiechemicalpurityof‰Tc-HYNIC-FolateWas96%underoptimalconditions.Datafromscintigraphyandthebiodistributionintumor-bearingmiceshowedthatTc-HYNIC-Fol
7、atepredominantlyaccumulatedintumor,itsuptakeratepergramtissuemWas5.620±0.753.rI'IleuptakesofTc-HYNIC-Fol~eintheothernon-targettissueswereverylow.exceptitWashi曲inthekidneys(was41.959±6.759).Conclusion鲫Tc-HYNIC-Folatehasthepotentialtobeusedasanoninvasiveradiodiagnosficimagingagen
8、tforthedetectionoffolatereceptor-positivehumancanCe1"8
