中华核医学与分子影像杂志
中華覈醫學與分子影像雜誌
중화핵의학여분자영상잡지
Chinese Journal of Nuclear Medicine and Molecular Imaging
2015年
5期
351-354
,共4页
李业森%张德良%张现忠%彭添兴%范文博%颜和平%吴华
李業森%張德良%張現忠%彭添興%範文博%顏和平%吳華
리업삼%장덕량%장현충%팽첨흥%범문박%안화평%오화
肝肿瘤%AlF-NOTA-G-TMTP1%氟放射性同位素%化学合成%体层摄影术,发射型计算机%小鼠,裸
肝腫瘤%AlF-NOTA-G-TMTP1%氟放射性同位素%化學閤成%體層攝影術,髮射型計算機%小鼠,裸
간종류%AlF-NOTA-G-TMTP1%불방사성동위소%화학합성%체층섭영술,발사형계산궤%소서,라
Liver neoplasms%AlF-NOTA-G-TMTP1%Fluorine radioisotopes%Chemical synthesis%Tomography,emission-computed%Mice,nude
目的 合成18F-AlF-NOTA-G-TMTP1,并在高转移潜能肝癌细胞荷瘤裸鼠体内评价其生物学性质.方法 通过固相法合成NOTA-G-TMTP1,利用18F标记制得PET探针18F-AlF-NOTA-G-TMTP1.分别用低转移潜能肝癌细胞株HCC97L和高转移潜能肝癌细胞株HCCLM3建立荷瘤裸鼠模型,并进行microPET/CT显像及生物分布研究.结果 18F-AlF-NOTA-G-TMTP1标记产率为(25±6)％(n=5),放化纯大于95％,比活度大于11.1 GBq/μmol,脂水分配系数为-3.166±0.022.注射后35 min的microPET/CT显像结果显示,18F-AlF-NOTA-G-TMTP1在HCC97L和HCCLM3荷瘤裸鼠模型中的肿瘤/肌肉比值分别为1.8±0.4和4.7±0.2.竞争性抑制实验结果显示,共注射G-TMTP1可将HCCLM3肿瘤对18F-AlF-NOTA-G-TMTP1的摄取降低61.4％.结论 成功合成的18F-AlF-NOTA-G-TMTP1可特异性靶向由高转移潜能肝癌细胞构建的瘤体.
目的 閤成18F-AlF-NOTA-G-TMTP1,併在高轉移潛能肝癌細胞荷瘤裸鼠體內評價其生物學性質.方法 通過固相法閤成NOTA-G-TMTP1,利用18F標記製得PET探針18F-AlF-NOTA-G-TMTP1.分彆用低轉移潛能肝癌細胞株HCC97L和高轉移潛能肝癌細胞株HCCLM3建立荷瘤裸鼠模型,併進行microPET/CT顯像及生物分佈研究.結果 18F-AlF-NOTA-G-TMTP1標記產率為(25±6)％(n=5),放化純大于95％,比活度大于11.1 GBq/μmol,脂水分配繫數為-3.166±0.022.註射後35 min的microPET/CT顯像結果顯示,18F-AlF-NOTA-G-TMTP1在HCC97L和HCCLM3荷瘤裸鼠模型中的腫瘤/肌肉比值分彆為1.8±0.4和4.7±0.2.競爭性抑製實驗結果顯示,共註射G-TMTP1可將HCCLM3腫瘤對18F-AlF-NOTA-G-TMTP1的攝取降低61.4％.結論 成功閤成的18F-AlF-NOTA-G-TMTP1可特異性靶嚮由高轉移潛能肝癌細胞構建的瘤體.
목적 합성18F-AlF-NOTA-G-TMTP1,병재고전이잠능간암세포하류라서체내평개기생물학성질.방법 통과고상법합성NOTA-G-TMTP1,이용18F표기제득PET탐침18F-AlF-NOTA-G-TMTP1.분별용저전이잠능간암세포주HCC97L화고전이잠능간암세포주HCCLM3건립하류라서모형,병진행microPET/CT현상급생물분포연구.결과 18F-AlF-NOTA-G-TMTP1표기산솔위(25±6)％(n=5),방화순대우95％,비활도대우11.1 GBq/μmol,지수분배계수위-3.166±0.022.주사후35 min적microPET/CT현상결과현시,18F-AlF-NOTA-G-TMTP1재HCC97L화HCCLM3하류라서모형중적종류/기육비치분별위1.8±0.4화4.7±0.2.경쟁성억제실험결과현시,공주사G-TMTP1가장HCCLM3종류대18F-AlF-NOTA-G-TMTP1적섭취강저61.4％.결론 성공합성적18F-AlF-NOTA-G-TMTP1가특이성파향유고전이잠능간암세포구건적류체.
Objective To synthesize 18F-AlF-NOTA-G-TMTP1 and evaluate its potential for PET imaging on nude mice bearing high-metastatic potential hepatoma cells.Methods NOTA-G-TMTP1 was synthesized by the standard Fmoc-solid phase synthetic protocols and radiolabeled with 18F using NOTA-AlF chelation method.The nude mice models bearing low-metastatic potential HCC97L and high-metastatic potential HCCLM3 xenografts were established separately.The tumor-targeting characteristics of 18F-AlF-NOTA-G-TMTP1 were assessed by microPET/CT and biodistribution assay.Results NOTA-G-TMTP1 was labeled with 18F in one step with (25±6)％ labeling yield (n=5).The radiochemical purity of 18F-AlF-NOTA-G-TMTP1 was more than 95％ with a specific activity more than 11.1 GBq/μmol.The octanol/water partition coefficient (logP) for 18F-AlF-NOTA-G-TMTP1 was-3.166±0.022.The tumor to muscle ratios were 1.8± 0.4 and 4.7±0.2 at 35 min post injection for HCC97L and HCCLM3,respectively.The uptake of 18F-AlF-NOTA-G-TMTP1 in HCCLM3 tumor was inhibited (61.4％) by unlabeled G-TMTP1.Conclusion 18F-AlF-NOTA-G-TMTP1 has been successfully synthesized.It shows specific uptake by tumor induced by the high-metastatic potential hepatoma cells.
