Evaluation of [89Zr]-Oxalate as a PET Tracer in Inflammation, Tumor, and Rheumatoid Arthritis Models

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• 作者：Ji-Ae Park ; Yong Jin Lee ; Ji Woong Lee ; Ran Ji Yoo ; Un Chol Shin ; Kyo Chul Lee ; Byung il Kim ; Kyeong Min Kim ; Jung Young Kim
• 刊名：Molecular Pharmaceutics
• 出版年：2016
• 出版时间：July 5, 2016
• 年：2016
• 卷：13
• 期：7
• 页码：2571-2577
• 全文大小：387K
• 年卷期：0
• ISSN：1543-8392

文摘

To obtain an additional pharmacological agent for the diagnosis of inflammation, we investigated the medical use of ⁸⁹Zr-oxalate as a positron emission tomography (PET) probe for the in vivo imaging of inflammation and compared its efficacy to that of 2-deoxy-2-[¹⁸F]fluoro-d-glucose ([¹⁸F]FDG) and sodium [¹⁸F]fluoride. ⁸⁹Zr-oxalate exhibited observable higher uptake in a macrophage cell line than in tumor cells. The inflammatory lesions and tumors were clearly visualized by PET imaging and autoradiography using ⁸⁹Zr-oxalate. Compared to [¹⁸F]FDG and sodium [¹⁸F]fluoride, ⁸⁹Zr-oxalate demonstrated a high selectivity index to the tumor at an early time point after injection and to inflammation at a delayed time point after injection (24 h). Through histological examination, large numbers of macrophages and neutrophils were observed in the tumor lesions with the highest ⁸⁹Zr-oxalate uptake. In a rheumatoid arthritis (RA) mouse model, ⁸⁹Zr-oxalate demonstrated a high level of accumulation in inflammatory lesions. ⁸⁹Zr-oxalate is a new strategic tool for tumor imaging and inflammatory processes.