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F-18标记的血管活性肠肽类似物在裸鼠结肠癌正电子发射断层显像中的应用

F-18 labeled vasoactive intestinal peptide analogue in the PET imaging of colon carcinoma in nude mice.

作者信息

Cheng Dengfeng, Liu Yuxia, Shen Hua, Pang Lifang, Yin Duanzhi, Wang Yongxian, Li Shanqun, Shi Hongcheng

机构信息

Department of Nuclear Medicine, Zhongshan Hospital, Fudan University, Shanghai 200032, China ; Shanghai Institute of Medical Imaging, Shanghai 200032, China.

Shanghai Institute of Applied Physics, Chinese Academy of Sciences, Shanghai 201800, China.

出版信息

Biomed Res Int. 2013;2013:420480. doi: 10.1155/2013/420480. Epub 2013 Dec 26.

DOI:10.1155/2013/420480
PMID:24459669
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC3888718/
Abstract

As large amount of vasoactive intestinal peptide (VIP) receptors are expressed in various tumors and VIP-related diseases, radiolabeled VIP provides a potential PET imaging agent for VIP receptor. However, structural modification of VIP is required before being radiolabeled and used for VIP receptor imaging due to its poor in vivo stability. As a VIP analogue, [R(8, 15, 21), L(17)]-VIP exhibited improved stability and receptor specificity in preliminary studies. In this study, F-18 labeled [R(8,15,21), L(17)]-VIP was produced with the radiochemical yield being as high as 33.6% ± 3% (decay-for-corrected, n = 5) achieved within 100 min, a specific activity of 255 GBq/ μmol, and a radiochemical purity as high as 99% as characterized by radioactive HPLC, TLC, and SDS-Page radioautography. A biodistribution study in normal mice also demonstrated fast elimination of F-18 labeled [R(8,15,21), L(17)]-VIP in the blood, liver, and gastrointestinal tracts. A further micro-PET imaging study in C26 colon carcinoma bearing mice confirmed the high tumor specificity, with the tumor/muscle radioactivity uptake ratio being as high as 3.03 at 60 min following injection, and no apparent radioactivity concentration in the intestinal tracts. In addition, blocking experiment and Western Blot test further confirmed its potential in PET imaging of VIP receptor-positive tumor.

摘要

由于大量血管活性肠肽（VIP）受体在各种肿瘤和VIP相关疾病中表达，放射性标记的VIP为VIP受体提供了一种潜在的PET成像剂。然而，由于其体内稳定性差，在进行放射性标记并用于VIP受体成像之前，需要对VIP进行结构修饰。作为一种VIP类似物，[R(8, 15, 21), L(17)]-VIP在初步研究中表现出了更好的稳定性和受体特异性。在本研究中，制备了F-18标记的[R(8,15,21), L(17)]-VIP，在100分钟内放射化学产率高达33.6%±3%（校正衰变，n = 5），比活度为255 GBq/μmol，经放射性HPLC、TLC和SDS-聚丙烯酰胺凝胶电泳放射自显影表征，放射化学纯度高达99%。正常小鼠的生物分布研究也表明，F-18标记的[R(8,15,21), L(17)]-VIP在血液、肝脏和胃肠道中快速清除。对荷C26结肠癌小鼠进行的进一步微型PET成像研究证实了其高肿瘤特异性，注射后60分钟时肿瘤/肌肉放射性摄取比高达3.03，且肠道内无明显放射性浓聚。此外，阻断实验和蛋白质免疫印迹试验进一步证实了其在VIP受体阳性肿瘤PET成像中的潜力。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/aa96/3888718/f83d30fa72e4/BMRI2013-420480.004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/aa96/3888718/184e156a2b7b/BMRI2013-420480.001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/aa96/3888718/6310f1a5f028/BMRI2013-420480.002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/aa96/3888718/9f69a257246a/BMRI2013-420480.003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/aa96/3888718/f83d30fa72e4/BMRI2013-420480.004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/aa96/3888718/184e156a2b7b/BMRI2013-420480.001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/aa96/3888718/6310f1a5f028/BMRI2013-420480.002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/aa96/3888718/9f69a257246a/BMRI2013-420480.003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/aa96/3888718/f83d30fa72e4/BMRI2013-420480.004.jpg

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