Hyoun Kim Myoung, Kim Seul-Gi, Guhn Kim Chang, Kim Dae-Weung
Department of Nuclear Medicine and Institute of Wonkwang Medical Science, Wonkwang University School of Medicine, Iksan, Jeollabuk-do, Korea.
Research Unit of Molecular Imaging Agent (RUMIA), Wonkwang University School of Medicine, Iksan, Jeollabuk-do, Korea.
Appl Radiat Isot. 2017 Mar;121:22-27. doi: 10.1016/j.apradiso.2016.12.026. Epub 2016 Dec 21.
The serine-aspartic acid-valine (SDV) peptide binds specifically to integrin αvβ3. We developed a Tc-99m and TAMRA labeled peptide, Tc-99m SDV-ECG-K-TAMRA for multimodal imaging of angiogenesis. Tc-99m SDV-ECG-K-TAMRA was prepared in high yield (>96%) and showed low cytotoxicity. Tc-99m tetrofosmin images 1 week after operation, revealed significantly decreased perfusion of the ischemic hindlimb, and the perfusion recovered gradually for 4 weeks. In contrast, Tc-99m SDV-ECG-K-TAMRA uptake was maximal 1 week after the operation (ischemic-to-non-ischemic uptake ratio =5.03±1.01) and decreased gradually. The ischemic-to-non-ischemic ratio of Tc-99m SDV-ECG-K-TAMRA and Tc-99m tetrofosmin was strongly negatively correlated (r =-0.94). A postmortem analysis revealed increased angiogenesis markers and uptake of Tc-99m SDV-ECG-K-TAMRA by ischemic tissue. Our in vivo and in vitro studies revealed substantial uptake of Tc-99m SDV-ECG-K-TAMRA by ischemic tissue. Tc-99m SDV-ECG-K-TAMRA could be a good candidate dual-modality imaging agent to assess angiogenesis.
丝氨酸-天冬氨酸-缬氨酸（SDV）肽可特异性结合整合素αvβ3。我们研发了一种锝-99m和四甲基罗丹明标记的肽，即锝-99m SDV-ECG-K-四甲基罗丹明，用于血管生成的多模态成像。锝-99m SDV-ECG-K-四甲基罗丹明的制备产率很高（>96%），且细胞毒性较低。术后1周的锝-99m替曲膦图像显示，缺血后肢的灌注显著降低，且在4周内灌注逐渐恢复。相比之下，锝-99m SDV-ECG-K-四甲基罗丹明的摄取在术后1周达到最大值（缺血与非缺血摄取比=5.03±1.01），并逐渐降低。锝-99m SDV-ECG-K-四甲基罗丹明与锝-99m替曲膦的缺血与非缺血比值呈强烈负相关（r = -0.94）。尸检分析显示，缺血组织中的血管生成标志物增加，且有锝-99m SDV-ECG-K-四甲基罗丹明的摄取。我们的体内和体外研究显示，缺血组织对锝-99m SDV-ECG-K-四甲基罗丹明有大量摄取。锝-99m SDV-ECG-K-四甲基罗丹明可能是评估血管生成的一种良好的双模态成像剂候选物。
