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首页> 外文期刊>RSC Advances >Arginine-glycine-aspartate (RGD)-targeted positron-labeled dendritic polylysine nanoprobe for tumor PET imaging
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Arginine-glycine-aspartate (RGD)-targeted positron-labeled dendritic polylysine nanoprobe for tumor PET imaging

机译：用于肿瘤宠物成像的精氨酸 - 甘氨酸 - 天冬氨酸（RGD）标记的正电子标记的树突式聚乙烯纳米孔

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摘要

This work investigated the optimization of the(68)Ga radiolabeling of the dendritic polylysine-1,4,7-triazacyclononane-1,4,7-triacetic acid conjugate (DGL-NOTA). Under pH = 4.0, reaction temperature of 70 degrees C, and incubation time of 10.0 min, the conjugate (DGL-NOTA) radiochemical yield was between 50% and 70%. After separation and purification, the radiochemical purity was greater than 98%. The radiolabeled formulation (Ga-68-NOTA-DGL-PEG-RGDyC) remained stable in both phosphate buffer and serum (all radiochemically greater than 95%) for up to 2 hours with a specific activity of 30 GBq/mu mol. Cellular experimental studies have shown that radiolabeled preparations can rapidly enter U87MG cells, and after 2 hours, there was still retention of imaging agents in the cells.In vivodistribution studies had shown that the tracer is excreted by the kidneys. Two hours after injecting the imaging agent, the U87MG tumor tissue uptake value was (4.67 +/- 0.09)% ID/g. Positron emission tomography (PET) imaging in animals showed that(68)Ga-NOTA-DGL-PEG-RGDyC had good targeting and can be enriched in tumor sites. Through hemolysis testing and morphological changes of red blood cells, it was proved that NOTA-DGL-PEG-RGDyC has good blood compatibility.
机译：该作品研究了树枝状多晶-1,4,7-三氮杂氨基甲烷-1,4,7-三芳基酸缀合物（DGL-NOTA）的（68）GA放射性标记的优化。在pH = 4.0下，反应温度为70℃，孵育时间为10.0分钟，缀合物（DGL-NOTA）放射化学产率在50％至70％之间。分离和纯化后，放射化学纯度大于98％。放射性标记的制剂（GA-68-NOTA-DGL-PEG-RGDYC）在磷酸盐缓冲液和血清（所有放射化学上大于95％）中保持稳定，最多2小时，特异性活性为30GBq / mumol。细胞实验研究表明，放射性标记的制剂可以快速进入U87mg细胞，并且在2小时后，仍然存在细胞中的成像剂。在体内分析研究表明，示踪剂被肾脏排出。注射成像剂后两小时，U87MG肿瘤组织吸收值是（4.67 +/- 0.09）％ID / g。在动物中成像的正电子发射断层扫描（PET）显影显示（68）GA-NOTA-DGL-PEG-RGDYC具有良好的靶向，可以富含肿瘤位点。通过红细胞的溶血测试和形态变化，证明NOTA-DGL-PEG-RGDYC具有良好的血液相容性。

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  • 来源
    《RSC Advances》 |2020年第39期|共10页
  • 作者

    Fang Qi; Xiao Yongcheng; Zhang Rongqin; Yin Jilin; Xie Deming; Wang Xinlu;

  • 作者单位

    Guangzhou Med Univ Dept Nucl Med Clin Hosp 1 Guangzhou 510120 Peoples R China;

    Jinan Univ Guangdong Prov Engn &

    Technol Res Ctr Drug Carrie Guangdong Higher Educ Inst Dept Biomed Engn Key Lab Biomat Guangzhou 510632 Peoples R China;

    PLA Dept Nucl Med Gen Hosp Southern Theater Command Guangzhou 510010 Peoples R China;

    PLA Dept Nucl Med Gen Hosp Southern Theater Command Guangzhou 510010 Peoples R China;

    Jinan Univ Guangdong Prov Engn &

    Technol Res Ctr Drug Carrie Guangdong Higher Educ Inst Dept Biomed Engn Key Lab Biomat Guangzhou 510632 Peoples R China;

    Guangzhou Med Univ Dept Nucl Med Clin Hosp 1 Guangzhou 510120 Peoples R China;

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  • 中图分类 化学;
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