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氟丙酰基氯代束丝氨酸放射性合成及其初步生物学评价作为胶质瘤成像的潜在 PET 示踪剂。

Radiosynthesis and Preliminary Biological Evaluation of F-Fluoropropionyl-Chlorotoxin as a Potential PET Tracer for Glioma Imaging.

机构信息

Department of Radiology, The First Affiliated Hospital, Sun Yat-Sen University, Guangzhou 510080, China.

Department of Radiology, Shenzhen City Nanshan District People's Hospital, Shenzhen 518000, China.

出版信息

Contrast Media Mol Imaging. 2018 Dec 20;2018:8439162. doi: 10.1155/2018/8439162. eCollection 2018.

DOI:10.1155/2018/8439162
PMID:30670934
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC6317094/
Abstract

PURPOSES

Chlorotoxin can specifically bind to matrix metalloproteinase 2 (MMP-2), which are overexpressed in the glioma. In this work, radiosynthesis of [F]-fluoropropionyl-chlorotoxin ([F]-FP-chlorotoxin) as a novel PET tracer was investigated, and biodistribution in vivo and PET imaging were performed in the C6 glioma model.

PROCEDURES

[F]-FP-chlorotoxin was prepared from the reaction of chlorotoxin with [F]-NFB (4-nitrophenyl 2-[F]-fluoropropionate), which was synthesized from multistep reactions. Biodistribution was determined in 20 normal Kunming mice. Small-animal PET imaging with [F]-FP-chlorotoxin was performed on the same rats bearing orthotopic C6 glioma at different time points (60 min, 90 min, and 120 min) after injection and compared with 2-deoxy-2-[F] fluoro-D-glucose ([F]-FDG).

RESULTS

[F]-FP-Chlorotoxin was successfully synthesized in the radiochemical yield of 41% and the radiochemical purity of more than 98%. Among all the organs, the brain had the lowest and stable uptake of [F]-FP-chlorotoxin, while the kidney showed the highest uptake. Compared with [F]-FDG, a low uptake of [F]-FP-chlorotoxin was detected in normal brain parenchyma and a high accumulation of [F]-FP-chlorotoxin was found in the gliomas tissue. The glioma to normal brain uptake ratio of [F]-FP-chlorotoxin was higher than that of [F]-FDG. Furthermore, the uptake of [F]-FP-chlorotoxin at 90 min after injection was better than that at 60 min after injection.

CONCLUSIONS

Compared with [F]-FDG, [F]-FP-chlorotoxin has a low and stable uptake in normal brain parenchyma. [F]-FP-Chlorotoxin seems to be a potential PET tracer with a good performance in diagnosis of the glioma.

摘要

目的

氯毒素可以特异性结合基质金属蛋白酶 2（MMP-2），后者在神经胶质瘤中过度表达。本研究旨在合成[F]-氟丙酰氯毒素（[F]-FP-氯毒素）作为一种新型 PET 示踪剂，并在 C6 神经胶质瘤模型中进行体内分布和 PET 成像。

方法

[F]-FP-氯毒素由氯毒素与[F]-NFB（4-硝基苯基 2-[F]-氟丙酸盐）反应制备，后者由多步反应合成。在 20 只正常昆明小鼠中进行了分布测定。在注射后不同时间点（60min、90min 和 120min），对荷原位 C6 神经胶质瘤的同窝大鼠进行小动物[F]-FP-氯毒素 PET 成像，并与 2-脱氧-2-[F]氟-D-葡萄糖（[F]-FDG）进行比较。

结果

[F]-FP-氯毒素的放射化学产率为 41%，放射化学纯度大于 98%。在所有器官中，脑的摄取率最低且稳定，而肾脏的摄取率最高。与[F]-FDG 相比，正常脑组织中[F]-FP-氯毒素的摄取较低，而胶质瘤组织中[F]-FP-氯毒素的积聚较高。[F]-FP-氯毒素的胶质瘤与正常脑摄取比值高于[F]-FDG。此外，注射后 90min 的摄取率优于注射后 60min。

结论

与[F]-FDG 相比，[F]-FP-氯毒素在正常脑实质中的摄取率较低且稳定。[F]-FP-氯毒素似乎是一种具有良好胶质瘤诊断性能的潜在 PET 示踪剂。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0204/6317094/c33dd9c73b71/CMMI2018-8439162.006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0204/6317094/26b2a026ab42/CMMI2018-8439162.001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0204/6317094/9e95bea0aa5c/CMMI2018-8439162.002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0204/6317094/42b08b051ac2/CMMI2018-8439162.003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0204/6317094/fb23d45374d0/CMMI2018-8439162.004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0204/6317094/bae3c2918006/CMMI2018-8439162.005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0204/6317094/c33dd9c73b71/CMMI2018-8439162.006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0204/6317094/26b2a026ab42/CMMI2018-8439162.001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0204/6317094/9e95bea0aa5c/CMMI2018-8439162.002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0204/6317094/42b08b051ac2/CMMI2018-8439162.003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0204/6317094/fb23d45374d0/CMMI2018-8439162.004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0204/6317094/bae3c2918006/CMMI2018-8439162.005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0204/6317094/c33dd9c73b71/CMMI2018-8439162.006.jpg

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