同位素2024,Vol.37Issue(5) :407-412.DOI:10.7538/tws.2024.youxian.060

68Ga标记GIPR靶向探针的合成及其初步生物学评价

Synthesis and Preliminary Biological Evaluation of 68Ga-labeled GIPR Targeting Probe

张朋俊 吴江 罗波 吴文雨 王峰
同位素2024,Vol.37Issue(5) :407-412.DOI:10.7538/tws.2024.youxian.060

68Ga标记GIPR靶向探针的合成及其初步生物学评价

Synthesis and Preliminary Biological Evaluation of 68Ga-labeled GIPR Targeting Probe

张朋俊 1吴江 1罗波 1吴文雨 1王峰1
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作者信息

  • 1. 南京医科大学附属南京医院,南京市第一医院核医学科,南京 210006
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摘要

葡萄糖依赖性胰岛素释放肽受体(GIPR)是神经内分泌肿瘤(NETs)的重要靶标之一.本研究构建了新型的GIPR靶向探针68Ga-DOTA-GIP(1-30)-F-02,通过模块进行自动化标记,考察该方法制备的68Ga-DOTA-GIP(1-30)-F-02的标记率、放化纯度及体外稳定性.用正常ICR小鼠进行生物分布研究,并建立PC12-hGIP细胞荷瘤鼠模型进行Micro-PET/CT显像研究.结果表明,68Ga-DOTA-GIP(1-30)-F-02自动化标记简易方便,标记率为(65.32±1.57)%,放化纯度>99%,体外稳定性良好.生物分布显示,68Ga-DOTA-GIP(1-30)-F-02在正常组织摄取较低,主要通过肾脏代谢,Micro-PET/CT显像该探针在给药后 60 min肿瘤部位放射性摄取值可达(6.51±1.03)%ID/g,具有较好的肿瘤显像效果,初步表明,该探针具有用于神经内分泌肿瘤靶向显像的可行性和特异性.

Abstract

Glucose-dependent insulinotropic polypeptide receptor(GIPR)is one of the important targets of neuroendocrine tumors(NETs).In this study,a novel GIPR targeting probe 68Ga-DOTA-GIP(1-30)-F-02 was constructed through the module for automatic labeling.The labeling yield,radiochemical purity,and in vitro stability of this probe were investigated.The biodistribution in normal ICR mice and Micro-PET/CT imaging of PC12-hGIP tumor-bearing mouse models were studied.The results showed that the automatic method for 68Ga-DOTA-GIP(1-30)-F-02 preparation was simple and convenient with a good radiochemical yield of(65.32±1.57)%,high radiochemical purity(>99%),and good in vitro stability.The results of biodistribution showed low uptakes of 68Ga-DOTA-GIP(1-30)-F-02 in normal tissues,mainly excreted through the renal urinary system.Micro-PET/CT imaging showed the uptake at the tumor site reached(6.51±1.03)%ID/g at 60 min post-injection which indicates good tumor imaging potentiality.The feasibility and specificity of the probe for GIPR-targeted imaging of neuroendocrine tumors were preliminarily demonstrated.

关键词

葡萄糖依赖性胰岛素释放肽受体/自动化标记/质量控制/Micro-PET/CT显像

Key words

glucose dependent insulin releasing peptide receptor/automated labeling/quality control/Micro-PET/CT imaging

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基金项目

国家自然科学基金资助项目(82272038)

出版年

2024
同位素
中国核学会同位素分会

同位素

CSTPCD
影响因子:0.405
ISSN:1000-7512
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