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

• DOI: 10.1021/acs.molpharmaceut.6b00411
• Publication Date: 2016-05-31T18:49:16Z
• Authors: 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
• Keywords: Inflammation; Male; Oxalates; 3. Good health; Arthritis, Rheumatoid; Mice; 03 medical and health sciences; RAW 264.7 Cells; 0302 clinical medicine; Fluorodeoxyglucose F18; Cell Line, Tumor; Positron-Emission Tomography; Animals; Humans

To obtain an additional pharmacological agent for the diagnosis of inflammation, we investigated the medical use of (89)Zr-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-[(18)F]fluoro-d-glucose ([(18)F]FDG) and sodium [(18)F]fluoride. (89)Zr-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 (89)Zr-oxalate. Compared to [(18)F]FDG and sodium [(18)F]fluoride, (89)Zr-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 (89)Zr-oxalate uptake. In a rheumatoid arthritis (RA) mouse model, (89)Zr-oxalate demonstrated a high level of accumulation in inflammatory lesions. (89)Zr-oxalate is a new strategic tool for tumor imaging and inflammatory processes.