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同位素  2011 

NGR短肽的188Re标记及其在荷瘤裸鼠体内的生物分布和SPECT显像

, PP. 77-82

Keywords: NGR,188Re,标记,SPECT

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Abstract:

采用188Re标记含有天冬酰胺、甘氨酸、精氨酸(Asn-Gly-Arg,NGR)序列的肿瘤血管靶向性短肽,得到188Re-NGR,观察了188Re-NGR在荷HepG2肝癌细胞严重联合免疫缺陷(SevereCombinedImmunodeficiency,SCID)裸鼠肿瘤模型中的生物分布,并对其进行了SPECT显像。结果显示,188Re-NGR的标记率>85%,放化纯度>90%。188Re-NGR在肿瘤模型鼠体内的生物分布显示,注射188Re-NGR后12h,肿瘤放射性摄取达最高,为(4.62±0.71)%ID/g,24h时仍有(2.01±0.38)%ID/g,说明标记物在肿瘤内停留时间较长;竞争性抑制组中,12h肿瘤放射性摄取为(1.43±0.61)%ID/g,明显低于实验组。肿瘤与肌肉组织的放射性摄取比(T/NT)12h为4.76。注射后1h肿瘤可显像,4~8h显像逐渐清晰,12h时更为清晰。以上结果提示,188Re-NGR具有良好的肿瘤血管靶向性。

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