摘要
目的 制备2－^18F－氟丙酸，并在荷Lewis肺癌小鼠模型中进行显像和体内分布研究。方法 经亲核取代反应制备2－^18F－氟丙酸，测定其亲水性。制备荷Lewis肺癌小鼠模型，经其尾静脉注射2－^18F－氟丙酸7.4～11.1 MBq，分别在注射后20、80 min行microPET显像。同时设丙酸钠和二氯乙酸钠阻断组。分析荷Lewis肺癌小鼠体内2－^18F－氟丙酸的分布情况。各组间比较采用两样本t检验。结果 2－^18F－氟丙酸的合成时间约40 min，放化纯〉99%；该化合物具有很强的亲水性。注射2－^18F－氟丙酸后，放射性主要聚集于肿瘤、膀胱和盲肠，肌肉、背部的棕色脂肪、骨骼的放射性摄取不明显。定量分析表明，注射后80 min和20 min相比，Lewis肺癌病灶对2－^18F－氟丙酸的摄取略有上升，但差异无统计学意义[（19.33±2.45） %ID/g与（17.03±2.87） %ID/g；t＝1.100，P〉0.05]；丙酸钠和二氯乙酸钠均不能阻断Lewis肺癌对2－^18F－氟丙酸的摄取（t＝1.544和0.894，均P〉0.05）。结论 2－^18F－氟丙酸的合成快捷、物化性质好，能清晰显示小鼠Lewis肺癌，且不会被丙酸钠和二氯乙酸钠阻断，有望用于临床肺癌的全身无创性检测。
Objective To prepare 2-[^18F]fluoropropionic acid （^18F-FPA） and evaluate its biodistribution and imaging capacity in Lewis lung carcinoma-bearing mice.Methods ^18F-FPA was prepared by nucleophilic substitution reaction, and its hydrophilicity was analyzed. ^18F-FPA （7.4-11.1 MBq） was injected into Lewis lung carcinoma-bearing mice via tail vein. MicroPET imaging was performed at 20, 80 min after the injection. The biodistribution of ^18F-FPA in organs was analyzed. The blocking effects of sodium propionate and dichloroacetate to ^18F-FPA were tested in vivo. Data were analyzed by two-sample t test using GraphPad Prism software.Results The synthesis of ^18F-FPA took 40 min. ^18F-FPA had high radiochemical purity （〉99%） and hydrophilicity. 18F-FPA was mainly distributed in the carcinoma, the urinary bladder and the caecum. The radioactive uptakes in muscles, brown fat and bones were relatively low. Quantitative analysis showed that the uptake of ^18F-FPA in Lewis lung carcinoma from 20 min to 80 min was slightly increased （（17.03±2.87） %ID/g vs （19.33±2.45） %ID/g） without significant difference （t=1.100, P〉0.05）. Neither sodium propionate nor dichloroacetate could block the uptake of ^18F-FPA in Lewis lung carcinoma （t=1.544, 0.894; both P〉0.05）.Conclusions ^18F-FPA can be quickly synthesized and has good physicochemical properties. It can be used as a tracer to visualize Lewis lung carcinoma in mice, and its tumor uptaking can not be blocked by propionate and dichloacetate. ^18F-FPA PET has the potential to detect lung cancer noninvasively in clinic.
出处
《中华核医学与分子影像杂志》
CAS
北大核心
2016年第2期180-183,共4页
Chinese Journal of Nuclear Medicine and Molecular Imaging
