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作为一种用于正电子发射断层显像肿瘤成像的新型放射性示踪剂的（6 8）镓- Lissamine罗丹明B（LRB）的合成与评估

The Synthesis and Evaluations of the (6 8) Ga-Lissamine Rhodamine B (LRB) as a New Radiotracer for Imaging Tumors by Positron Emission Tomography.

作者信息

Li Xuena, Yin Yafu, Du Bulin, Li Na, Li Yaming

机构信息

Department of Nuclear Medicine, The First Hospital of China Medical University, Shenyang 110001, China.

出版信息

Biomed Res Int. 2016;2016:8549635. doi: 10.1155/2016/8549635. Epub 2016 Feb 2.

DOI:10.1155/2016/8549635
PMID:26949707
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC4754471/
Abstract

PURPOSE

The aim of this study is to synthesize and evaluate (68)Ga-labeled Lissamine Rhodamine B (LRB) as a new radiotracer for imaging MDA-MB-231 and MCF-7 cells induced tumor mice by positron emission tomography (PET).

METHODS

Firstly, we performed the radio synthesis and microPET imaging of (68)Ga(DOTA-LRB) in athymic nude mice bearing MDA-MB-231 and MCF-7 human breast cancer xenografts. Additionally, the evaluations of (18)F-fluorodeoxyglucose (FDG), as a glucose metabolism radiotracer for imaging tumors in the same xenografts, have been conducted as a comparison.

RESULTS

The radiochemical purity of (68)Ga(DOTA-LRB) was >95%. MicroPET dynamic imaging revealed that the uptake of (68)Ga(DOTA-LRB) was mainly in normal organs, such as kidney, heart, liver, and brain and mainly excreted from kidney. The MDA-MB-231 and MCF-7 tumors were not clearly visible in PET images at 5, 15, 30, 40, 50, and 60 min after injection of (68)Ga(DOTA-LRB). The tumor uptake values of (18)F-FDG were 3.79 ± 0.57 and 1.93 ± 0.48%ID/g in MDA-MB-231 and MCF-7 tumor xenografts, respectively.

CONCLUSIONS

(68)Ga(DOTA-LRB) can be easily synthesized with high radiochemical purity and stability; however, it may be not an ideal PET radiotracer for imaging of MDR-positive tumors.

摘要

目的

本研究旨在合成并评估（68）镓标记的丽丝胺罗丹明B（LRB）作为一种新型放射性示踪剂，用于通过正电子发射断层扫描（PET）对MDA - MB - 231和MCF - 7细胞诱导的肿瘤小鼠进行成像。

方法

首先，我们在携带MDA - MB - 231和MCF - 7人乳腺癌异种移植瘤的无胸腺裸鼠中进行了（68）镓（DOTA - LRB）的放射性合成和微型PET成像。此外，作为比较，还对（18）氟 - 脱氧葡萄糖（FDG）进行了评估，它是用于对相同异种移植瘤中的肿瘤进行成像的葡萄糖代谢放射性示踪剂。

结果

（68）镓（DOTA - LRB）的放射化学纯度>95%。微型PET动态成像显示，（68）镓（DOTA - LRB）的摄取主要发生在正常器官，如肾脏、心脏、肝脏和大脑，并且主要通过肾脏排泄。在注射（68）镓（DOTA - LRB）后5、15、30、40、50和60分钟时，PET图像中MDA - MB - 231和MCF - 7肿瘤并不清晰可见。在MDA - MB - 231和MCF - 7肿瘤异种移植瘤中，（18）F - FDG的肿瘤摄取值分别为3.79±0.57和1.93±0.48%ID/g。

结论

（68）镓（DOTA - LRB）能够容易地合成，具有高放射化学纯度和稳定性；然而，它可能不是用于多药耐药（MDR）阳性肿瘤成像的理想PET放射性示踪剂。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f477/4754471/4fdc2db4ea6d/BMRI2016-8549635.006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f477/4754471/74f3abc239bd/BMRI2016-8549635.001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f477/4754471/9e914ea26bb9/BMRI2016-8549635.002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f477/4754471/06b6d215489b/BMRI2016-8549635.003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f477/4754471/10ce00a881e6/BMRI2016-8549635.004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f477/4754471/30bdfb4e8cf1/BMRI2016-8549635.005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f477/4754471/4fdc2db4ea6d/BMRI2016-8549635.006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f477/4754471/74f3abc239bd/BMRI2016-8549635.001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f477/4754471/9e914ea26bb9/BMRI2016-8549635.002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f477/4754471/06b6d215489b/BMRI2016-8549635.003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f477/4754471/10ce00a881e6/BMRI2016-8549635.004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f477/4754471/30bdfb4e8cf1/BMRI2016-8549635.005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f477/4754471/4fdc2db4ea6d/BMRI2016-8549635.006.jpg

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