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

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...

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Veröffentlicht in:Molecular pharmaceutics 2016-07, Vol.13 (7), p.2571-2577
Hauptverfasser: Park, Ji-Ae, Lee, Yong Jin, Lee, Ji Woong, Yoo, Ran Ji, Shin, Un Chol, Lee, Kyo Chul, Kim, Byung il, Kim, Kyeong Min, Kim, Jung Young
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container_end_page 2577
container_issue 7
container_start_page 2571
container_title Molecular pharmaceutics
container_volume 13
creator Park, Ji-Ae
Lee, Yong Jin
Lee, Ji Woong
Yoo, Ran Ji
Shin, Un Chol
Lee, Kyo Chul
Kim, Byung il
Kim, Kyeong Min
Kim, Jung Young
description 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.
doi_str_mv 10.1021/acs.molpharmaceut.6b00411
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Pharmaceutics</addtitle><description>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. 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Pharmaceutics</addtitle><date>2016-07-05</date><risdate>2016</risdate><volume>13</volume><issue>7</issue><spage>2571</spage><epage>2577</epage><pages>2571-2577</pages><issn>1543-8384</issn><eissn>1543-8392</eissn><abstract>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.</abstract><cop>United States</cop><pub>American Chemical Society</pub><pmid>27243098</pmid><doi>10.1021/acs.molpharmaceut.6b00411</doi><tpages>7</tpages></addata></record>
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subjects Animals
Arthritis, Rheumatoid - diagnostic imaging
Cell Line, Tumor
Fluorodeoxyglucose F18 - analysis
Fluorodeoxyglucose F18 - chemistry
Humans
Inflammation - diagnostic imaging
Male
Mice
Oxalates - analysis
Oxalates - chemistry
Positron-Emission Tomography - methods
RAW 264.7 Cells
title Evaluation of [89Zr]-Oxalate as a PET Tracer in Inflammation, Tumor, and Rheumatoid Arthritis Models
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