目的采用[18F]FDG直接一步法标记合成[18F]FDG-RGD,探讨其在肝纤维化动物模型中潜在的诊断价值。方法采用TRACERlab FX18F N平台,在酸性条件下将酸化的[F]FDG与RGD加热直接反应,然后采用固相柱进行分离目的示踪剂[18F]FDG-RGD。应用硫代乙酰胺(thioacetamide,TAA)构建大鼠肝纤维化模型,对照组(n=4)和肝纤维化组大鼠(n=4)经尾静脉注射[18F]FDG-RGD,采用Discovery Elite PET/CT的VIP模型进行动态扫描,用Sharp IR+VUE Point HD及OSEM迭代重建法对采集图像进行重建,通过勾画感兴趣方法(region of interest,ROI)处理图像,获取大鼠肝脏与心脏的放射性计数比值(liver/heart,L/H),比较对照组与肝纤维化动物模型肝脏摄取[18F]FDG-RGD的差异。结果 10次连续合成效率达到20%、放射化学纯度98%,整个合成过程大约30min。注射[18F]FDG-RGD后30min,对照组与肝纤维化组L/H分别为0.73±0.15、1.35±0.08,肝纤维化组明显高于对照组(P=0.018)。结论 [18F]FDG直接标记RGD多肽方法简单、方便可行,[18F]FDG-RGD有助于肝纤维化的诊断。
Objective To study the feasibility of labelling the PET tracer [18F]FDG –RGD directly, and to evaluate its value in diagnosis of liver fibrosis. Methods TRACERlab FX18 FN platform was used to heat the mixture of [ F] FDG and RGD peptide under the condition of acidification, and then the solid-phase column was used to separate the tracer [1 8 F]FDG –RGD. The thioacetamide(TAA) was applied to establish rat liver fibrosis models. [18F]FDG-RGD was injected through tail vein in control rats(n=4)and liver fibrotic rats(n=4). We used VIP model of Discovery Elite PET/CT to perform dynamic scanning,and Sharp IR+VUE Point HD and OSEM technique to construct the images,and got the ratio of liver and heart radioactivity(L/H) by region of interest(ROI). Results The yields of [18F]FDG–RGD reached to 20% after 10 successive synthetic cycles, and the radiochemical purity reached to 98%, about 30 minutes for the whole synthesis process. The L/H ratios were 0.73±0.15 in control rats and 1.35±0.08 in liver fibrosis rats, with much higher in fibrotic group than in control group( P =0.018). Conclusion This method is simple and feasible to prepare [18F] FDG-RGD,which would be helpful in diagnosis of liver fibrosis.