新型fap靶向配体68Ga-DOTA-FL在结肠癌小动物PET/CT成像中的初步研究

IF 2.3 4区 医学 Q2 RADIOLOGY, NUCLEAR MEDICINE & MEDICAL IMAGING
Zhan Xu, Yimeng Shi, Hongyan Yin, Jing Lv
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引用次数: 0

摘要

目的探讨68镓(Ga)标记的新型成纤维细胞激活蛋白(FAP)靶向配体用于小动物PET/CT(正电子发射计算机断层扫描/计算机断层扫描)肿瘤成像的可行性。方法采用添加螯合基团十二烷四乙酸(DOTA),并用68Ga标记法制备fap配体(FL)。采用MC38细胞系建立C57BL/6小鼠结肠癌模型。体外检测标记68Ga-DOTA-FL在小鼠模型各脏器的放射性分布。此外,采用小动物PET/CT对68Ga-DOTA-FL进行体内肿瘤靶向显像。最后对MC38细胞和异种移植肿瘤组织进行免疫印迹和免疫荧光成像。结果68Ga-DOTA-FL的放射性标记率和放射化学纯度均在95%以上。western blotting和免疫荧光成像显示FAP在肿瘤组织中表达,而在MC38细胞中不表达。小动物PET/CT成像显示,68Ga-DOTA-FL治疗后30min肿瘤影像最清晰。体外放射性分布检测显示,68Ga-DOTA-FL治疗30 min后,肿瘤和肌肉组织的靶/非靶比为4.0±0.3 (n = 3)。结论68ga - dota - fl可用于小鼠模型的特异性肿瘤成像,为fap靶向肿瘤成像提供了一种新的选择。
本文章由计算机程序翻译,如有差异,请以英文原文为准。

Preliminary study of a novel FAP-targeted ligand 68Ga-DOTA-FL in colon cancer imaging using small-animal PET/CT

Preliminary study of a novel FAP-targeted ligand 68Ga-DOTA-FL in colon cancer imaging using small-animal PET/CT

Purpose

This study explored the feasibility of 68gallium (Ga)-labeled novel fibroblast activation protein (FAP)-targeted ligand for tumor imaging through small-animal PET/CT (positron emission computed tomography/computed tomography).

Methods

The FAP-ligand (FL) was created by adding the chelating group dodecane tetraacetic acid (DOTA) and labeling with 68Ga. The MC38 cell line was used to establish a C57BL/6 mice colon cancer model. The radioactivity distribution of labeled 68Ga-DOTA-FL across various organs of the mouse model was examined ex-vivo. In addition, 68Ga-DOTA-FL tumor-targeted imaging in vivo was performed using small-animal PET/CT. Finally, western blotting and immunofluorescence imaging of MC38 cells and xenotransplant tumor tissues were conducted.

Results

The radiolabeling rate and radiochemical purity of 68Ga-DOTA-FL were above 95%. Both western blotting and immunofluorescence imaging revealed FAP expression in the tumor tissues, but not in the MC38 cells. Small-animal PET/CT imaging indicated that the tumor imaging was clearest at 30 min after 68Ga-DOTA-FL treatment. Examination of the radioactivity distribution in vitro revealed that at 30 min after the 68Ga-DOTA-FL treatment, the target/non-target ratio for tumor and muscle tissue was 4.0 ± 0.3 (n = 3).

Conclusions

68Ga-DOTA-FL can be used for the specific tumor imaging in mouse models, which might provide a novel alternative for FAP-targeted tumor imaging.

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来源期刊
Clinical and Translational Imaging
Clinical and Translational Imaging Medicine-Radiology, Nuclear Medicine and Imaging
CiteScore
3.60
自引率
4.80%
发文量
55
期刊介绍: Clinical and Translational Imaging is an international journal that publishes timely, up-to-date summaries on clinical practice and translational research and clinical applications of approved and experimental radiopharmaceuticals for diagnostic and therapeutic purposes. Coverage includes such topics as advanced preclinical evidence in the fields of physics, dosimetry, radiation biology and radiopharmacy with relevance to applications in human subjects. The journal benefits a readership of nuclear medicine practitioners and allied professionals involved in molecular imaging and therapy.
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