氨基酸类肿瘤显像剂氟-18标记方法

Review of the Labeling Methods of Fluorinated Amino Acid with ^(18)F for Tumor Imaging

阅读国内外相关文献并进行整理分析,对氨基酸类肿瘤显像剂的氟-18(^(18)F)标记方法进行系统综述。正电子发射断层(positron emission tomography,PET)显像是一种发展迅速的核医学诊断技术,是一种能定量确定人体器官或组织局部功能和生化过程的显像技术,在肿瘤及其他疾病的诊断中具有十分重要的作用。2-氟-2-脱氧-D-葡萄糖作为临床上使用最广泛的PET显像剂,已成功地用于临床各个方面,如分辨肿瘤的良恶性、评价肿瘤的恶性程度等,但临床使用中也发现2-氟-2-脱氧-D-葡萄糖特异性差,有时会出现假阳性、肿瘤和炎症不能区分等问题。这要求我们进一步研发新的PET显像剂来弥补。考虑到在肿瘤组织中,不仅糖代谢旺盛,氨基酸转运和蛋白质的合成代谢也会增加,因此用正电子核素标记氨基酸就成为另一类有潜力的肿瘤诊断显像剂。

Positron emission tomography（PET） is a nuclear imaging technology, which can accurately determine the local function and the biochemical course of organs or tissues of human body, so PET technology has an important role in the diagnosis of tumors and other diseases. 18 F-FDG has been used in oncology for differentiating of benign tumors from malignant tumors, detecting and staging of malignant tumors. However, 18F-FDG has low specificity, no uptake in some tumor cells but appreciable uptake in inflammation. Therefore designing and synthesizing tumor imaging agents with high specificity and sensitivity is necessary and exigent. In view of the fact that the metabolism of protein is also increased in tumor tissues in addition to the metabolism of glucose, developing new amino acid imaging agents labeled by positron emission nuclide may have quite large potential.