Department of Nuclear Medicine, University of Marburg, Marburg, Germany.
Eur J Nucl Med Mol Imaging. 2009 Nov;36(11):1767-73. doi: 10.1007/s00259-009-1153-6. Epub 2009 May 16.
ReO(4)(-) has similar kinetics regarding the sodium iodide symporter (NIS) to I(-) and TcO(4)(-) in NIS-expressing tissue. We investigated the therapeutic potential of (186)ReO(4)(-) in NIS-transfected neuroendocrine tumour tissue.
For experiments, the stably NIS-transfected pancreatic neuroendocrine cancer cell line Bon1C was used. NIS-mediated internalization and externalization experiments in vitro and a biodistribution study in nude mice bearing Bon1C xenografts were performed. A therapy study was also conducted consecutively in nude mice xenografted with Bon1C in which the mice were injected intravenously with Na(186)ReO(4).
In vitro studies showed exponential internalization and efflux kinetics of (186)ReO(4)(-) in the cell line. The biodistribution study showed high uptake of (186)ReO(4)(-) in NIS-expressing tumours. Tumour growth inhibition was significant after injection of (186)ReO(4) in two groups of animals treated with activity levels below the determined maximum tolerable activity as compared to controls.
These results indicate that the use of (186)ReO(4)(-) in the treatment of NIS-expressing neuroendocrine tumours is feasible and support the concept of using NIS as a therapeutic target for (186)ReO(4)(-).
ReO(4)(-)在表达钠碘同向转运体（NIS）的组织中与 I(-)和 TcO(4)(-)具有相似的动力学特性。我们研究了（186）ReO(4)(-)在 NIS 转染的神经内分泌肿瘤组织中的治疗潜力。
实验中使用了稳定转染 NIS 的胰腺神经内分泌癌细胞系 Bon1C。进行了体外 NIS 介导的内化和外排实验以及裸鼠携带 Bon1C 异种移植瘤的生物分布研究。还在裸鼠中进行了连续的治疗研究，这些裸鼠用 Bon1C 异种移植，然后静脉注射 Na(186)ReO(4)。
体外研究表明（186）ReO(4)(-)在细胞系中具有指数内化和外排动力学。生物分布研究显示，（186）ReO(4)(-)在表达 NIS 的肿瘤中有高摄取。与对照组相比，在两个接受低于确定最大耐受活性的放射性活度水平治疗的动物组中，注射（186）ReO(4)后肿瘤生长抑制显著。
这些结果表明，（186）ReO(4)(-)在治疗表达 NIS 的神经内分泌肿瘤中的应用是可行的，并支持将 NIS 作为（186）ReO(4)(-)治疗靶点的概念。
