In Vivo Evaluation of a Bombesin Analogue Labeled with Ga-68 and Co-55/57
In Vivo Evaluation of a Bombesin Analogue Labeled with Ga-68 and Co-55/57
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DOI：
10.1007/s11307-015-0911-z
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发表时间：
2016-06-01
影响因子：
3.1
通讯作者：
Thisgaard, Helge
中科院分区：
文献类型：
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作者：
Dam, Johan Hygum;Olsen, Birgitte Brinkmann;Thisgaard, Helge
本研究的目的是将Co-55或Ga-68标记的蛙黄素类似物NOTA-AMBA应用于前列腺癌的临床前显像。在异种移植小鼠(PC3)中使用固定数量的多肽在1、4和24小时(仅24小时只含钴)进行生物分布。接种后4周，尾静脉注射[Ga-68]NOTA-AMBA或[Co-55]NOTA-AMBA后，对移植小鼠进行正电子发射断层扫描/X射线计算机断层扫描，获得了大于90%的产率。Ga-68和Co-55的放化纯度(RCP)分别为95%和90%。[Ga-68]NOTA-AMBA 1 h摄取10.3%ID/g，4 h摄取6.4%ID/g；[Co-57]NOTA-AMBA 1 h摄取8.2%ID/g，24 h摄取5.3%ID/g。随着时间的推移，正常组织被清除，提高了肿瘤与本底的比率。NOTA-AMBA高产率标记，RCP用Ga-68和Co-55/57标记。在小鼠前列腺癌皮下模型中观察到高肿瘤摄取率。在注射后24 h，[Co-55/57]NOTA-AMBA的肿瘤脏器比在注射后1 h和4 h均优于[Ga-68]NOTA-AMBA。因此，在成像方面，[Co-55]NOTA-AMBA被发现优于[Ga-68]NOTA-AMBA。
The purpose of this study was to apply an analogue of bombesin, NOTA-AMBA, labeled with Co-55 or Ga-68, for preclinical imaging of prostate cancer.The peptide NOTA-AMBA was labeled with Ga-68 or Co-55 by microwave irradiation. Biodistribution in xenograft mice (PC3) was performed at 1, 4, and 24 h (only cobalt at 24 h) using a fixed amount of peptide. Four weeks post-inoculation, xenograft mice were positron emission tomography/X-ray computed tomography scanned after tail vein injection of [Ga-68]NOTA-AMBA or [Co-55]NOTA-AMBA.Labeling with Ga-68 and Co-55/57 was achieved in yields greater than 90 %. A radiochemical purity (RCP) of 95 and 90 % were obtained for Ga-68 and Co-55, respectively. Both radiopeptides showed high uptake in the intestines, stomach, pancreas, and in the tumor ([Ga-68]NOTA-AMBA, 10.3 %ID/g at 1 h to 6.4 %ID/g at 4 h; [Co-57]NOTA-AMBA, 8.2 %ID/g at 1 h to 5.3%ID/g at 24 h). Normal tissue cleared over time improving tumor-to-background ratios.NOTA-AMBA was labeled in high yields and RCP with Ga-68 and Co-55/57. High tumor uptake in a subcutaneous mouse prostate cancer model was observed. At 24 h, [Co-55/57]NOTA-AMBA showed better tumor-to-organ ratios than [Ga-68]NOTA-AMBA at both 1 and 4 h post-injection. Hence, for imaging, [Co-55]NOTA-AMBA was found to be superior compared to [Ga-68]NOTA-AMBA.