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1、肼基煙酰胺基酰肼基-葉酸的合成與動(dòng)物顯像中國醫(yī)學(xué)科學(xué)院ACrAACADEMIAEMEDICAESICAE葉酸受體腫瘤顯像劑mTc.肼基煙酰胺基酰肼基-葉酸的合成與動(dòng)物顯像劉麗琴#,王世真,李方,滕寶,王克棧,邱飛蟬(中國醫(yī)學(xué)科學(xué)院中國協(xié)和醫(yī)科大學(xué)北京協(xié)和醫(yī)院核醫(yī)學(xué)科,北京100730)?論著?摘要:目的研究葉酸受體腫瘤顯像劑∞Tc.肼基煙酰胺基酰肼基.葉酸(‰Tc.HYNIC.葉酸)的合成,生物分布及其動(dòng)物顯像.方法以葉酸為原料經(jīng)過多步反應(yīng)合成葉酸衍生物HYNIC.葉酸,以該衍生物為配體,并以三(羥甲基)甲基甘氨酸和三苯甲基膦三磺酸鈉為共配體進(jìn)行∞T
2、c標(biāo)記,對(duì)其放化純度,穩(wěn)定性進(jìn)行分析,對(duì)正常小鼠及荷瘤小鼠的體內(nèi)生物分布和荷瘤小鼠的相機(jī)顯像進(jìn)行研究.結(jié)果配體HYNIC.葉酸的結(jié)構(gòu)經(jīng)核磁共振氫譜和質(zhì)譜進(jìn)行確認(rèn),經(jīng)標(biāo)記后,放化純度為96%,體外穩(wěn)定性好.在荷瘤小鼠中的生物分布和顯像結(jié)果表明,∞Tc-HYNIC-葉酸在腫瘤中有較高的濃集,單位質(zhì)量攝取率為5.620±0.753.除在腎中攝取較高(單位質(zhì)量攝取率為41.959±6.759)外,其他非靶組織中攝取均較低.結(jié)論Tc-HYNIC-葉酸有望成為性能良好的葉酸受體腫瘤顯像劑.關(guān)鍵詞:葉酸受體;葉酸衍生物;同位素標(biāo)記;生物分布;顯像中圈分類號(hào):R81
3、7.9文獻(xiàn)標(biāo)識(shí)碼:A文章編號(hào):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鐘Tcusingtricineandtrisodiumphenylphosp
5、hine-3,3',3"-trisulfonate(ⅡrS)a8coligands.111eradiechemiealpurityandstabihtyof99Tc-HYNIC-Folatewasmeasured.rI'Ilebiodistributionsof鐘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鯽Tc-HYNIC-Folatehasthepotentialtobeusedasanoninvasiveradiodiagnosficimagingagen
8、tforthedetectionoffolatereceptor-positivehumancanCe1"8
