18F-FPA的合成及对荷前列腺癌裸鼠的显像研究

摘要

目的 探讨显像剂2-18 F-氟丙酸(18 F-FPA)的合成及对荷前列腺癌裸鼠的显像价值.方法 利用CFN-multi-200型多功能药物合成模块自动化合成18 F-FPA,进行质量控制.建立荷PC3前列腺癌裸鼠(16只)和荷22RV1前列腺癌裸鼠(4只)模型,分别进行18 F-FPA显像,并与18F-氟代脱氧葡萄糖(18F-FDG)和11 C-胆碱显像进行对比,评价18F-FPA对前列腺癌的显像价值.将荷PC3前列腺癌裸鼠分为4组进行生物分布测定,计算每克组织百分注射剂量率(％ID/g)和肿瘤与非肿瘤比值.结果 18F-FPA的合成过程约40 min,产率为(38±2)％(未经时间校正),放射化学纯度大于97％,体外稳定性良好.注射18F-FPA后显像,两种荷瘤裸鼠肿瘤均显影清晰,而18 F-FDG和11C-胆碱显像肿瘤仅轻微摄取.荷PC3前列腺癌裸鼠的肿瘤在注射18F-FPA后0.5、1.0、2.0和4.0h的生物分布分别为(6.91±0.72)、(6.99±0.55)、(7.17±0.25)和(6.49士0.74)％ID/g,差异无统计学意义(P＞0.05).结论 18 F-FPA合成简单,对荷前列腺癌裸鼠有较好的显像效果,有望用于临床前列腺癌的检测.%Objective To explore the synthesis of photographic developer 2-18 F-fluoropropionic acid(18 F-FPA) and its imaging value in prostate cancer-bearing nude mice.Methods 18F-FPA was automatically synthesized by using the CFN-multi-200 multifunctional drug synthesis module,then the quality control were performed.The PC3 prostate cancer-bearing nude mice models(16 cases) and 22RV1 prostate cancer-bearing nude mice models(4 cases) were constructed.Then 18F-FPA imaging was conducted in these models,which were compared with those by 2-deoxy-2-18 F fluoro-D-glueose(18 F-FDG) and 11C-choline for evaluating the imaging value of 18F-FPA in prostate cancer.The mice bearing PC3 prostate cancer were randomly divided into 4 group for conducting the biodistribution measurement.The percentage rate of injection dose per gram tissue(％ID/g) and tumor/non-tumor tissue ratio was calculated.Results The synthetic process of 18 F-FPA was about 40 min,the yield rate was (38 ± 2) ％ (without time correction),the radiochemical purity was more than 97 ％,with good in vitro stability.After 18F-FPA injection,the tumor image in two kinds of tumor-bearing nude micecould was developed clearly,while a slight uptake was detected in developed tumor with 18 F-FDG and n C-choline imaging.The biodistributions of tumor in PC3 prostate cancer bearing nude mice were (6.91 ± 0.72),(6.99 ±0.55),(7.17 ± 0.25),(6.49 ± 0.74) ％ ID/g at 0.5,1.0,2.0 and 4.0 h after 18 F-FPA injection,respectively,the difference was not statistically significant(P＞0.05).Conclusion 18 F-FPA is simply synthesized,has better imaging effect for the nude mice bearing prostate cancer and is expected to be used for clinical detection of prostate cancer.