一种低分子量叶酸受体靶向对比剂，用于磁共振肿瘤成像。
A low molecular weight folate receptor targeted contrast agent for magnetic resonance tumor imaging.
机构信息
MRC Clinical Sciences Centre, Imperial College London, Hammersmith Hospital, London, UK.
出版信息
Mol Imaging Biol. 2011 Aug;13(4):653-62. doi: 10.1007/s11307-010-0400-3.
PURPOSE
This study aims to develop a low molecular weight folate receptor (FR) contrast agent for MR tumor imaging.
PROCEDURES
Gadolinium-tetraazacyclododecane tetraacetic acid (Gd.DOTA) was conjugated to folic acid to create Gd.DOTA.Folate. The efficacy of Gd.DOTA.Folate to bind FR was evaluated in vitro by inductively coupled mass spectrometry (ICP-MS) and in vivo by magnetic resonance imaging (MRI) tumor enhancement over 14 h, utilizing an overexpressing α-FR cell line (IGROV-1), compared to an α-FR-negative cell line (OVCAR-3). Gd.DOTA.Folate localization ex vivo was verified by laser ablation ICP-MS.
RESULTS
ICP-MS confirmed Gd.DOTA.Folate uptake by IGROV-1 cells and competitive binding with free folic acid inhibited binding. IGROV-1 tumors showed an increase in R (1) at 2 h, which increased significantly over 14 h post-Gd.DOTA.Folate with clear enhancement on MR images. This was not observed in controls.
CONCLUSION
These data support the use of FR-targeted small molecular weight MRI contrast agents for tumor imaging in vivo.
目的
本研究旨在开发一种用于磁共振成像的低分子量叶酸受体（FR）对比剂。
方法
将钆-四氮杂环十二烷四乙酸（Gd.DOTA）与叶酸连接，制成 Gd.DOTA.叶酸。通过电感耦合质谱（ICP-MS）体外评估 Gd.DOTA.叶酸与 FR 的结合效力，并通过磁共振成像（MRI）在 14 小时内评估肿瘤增强情况，使用过表达α-FR 的细胞系（IGROV-1）进行比较，与α-FR 阴性细胞系（OVCAR-3）进行比较。通过激光烧蚀 ICP-MS 验证 Gd.DOTA.叶酸的体外定位。
结果
ICP-MS 证实 Gd.DOTA.叶酸被 IGROV-1 细胞摄取，游离叶酸的竞争性结合抑制了结合。IGROV-1 肿瘤在 2 小时时 R（1）增加，在 Gd.DOTA.叶酸后 14 小时内显著增加，MR 图像上有明显增强。在对照组中未观察到这种情况。
结论
这些数据支持使用 FR 靶向的小分子 MRI 对比剂进行体内肿瘤成像。
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