Short Commmunication: Synthesis and Biologic Evaluation of I-123-Labeled Porphyrin Derivative as a Potential Tumor-Imaging Agent
Jae Hak Lee, Byung Seok Moon, Tae Sup Lee, Dae Yoon, Kwon Soo Chun, Gi Jeong Cheon
Abstract
Jae Hak Lee, Byung Seok Moon, Tae Sup Lee, Dae Yoon, Kwon Soo Chun, Gi Jeong Cheon
Abstract
5-(3-(3-[(123)I]iodoallyloxy)phenyl)-10,15,20-tris-(3-carboxymethoxyphenyl)porphyrin ([ (123)I]2) was prepared for biologic evaluation in a B16-F10 tumor model to examine its potential as an imaging agent. The I-123-labeled porphyrin [(123)I]2 was purified by reverse-phase high-performance liquid chromatography (HPLC) to give a decay-corrected radiochemical yield of 8%-13% (n=9) and the radiochemical purity after HPLC purification was >95% and the overall radiolabeling time was 160 minutes. The in vitro cell uptake of [ (123)I]2 increased with time. Biodistribution in mice bearing the B16-F10 tumor, after an intravenous injection of [(123)I]2, also showed a time-dependent accumulation of the porphyrin in tumor tissue (10.35 %ID/g at 6 hours). The tumor-to-muscle ratio was 3.49, 3.38, 3.07, and 3.13 at 1, 2, 6, and 24 hours, respectively. The gamma-camera images of (123)I-porphyrin demonstrated a high focal accumulation of radioactivity in the B16-F10 melanoma tumor.
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5-(3-(3-[(123)I]iodoallyloxy)phenyl)-10,15,20-tris-(3-carboxymethoxyphenyl)porphyrin ([ (123)I]2) was prepared for biologic evaluation in a B16-F10 tumor model to examine its potential as an imaging agent. The I-123-labeled porphyrin [(123)I]2 was purified by reverse-phase high-performance liquid chromatography (HPLC) to give a decay-corrected radiochemical yield of 8%-13% (n=9) and the radiochemical purity after HPLC purification was >95% and the overall radiolabeling time was 160 minutes. The in vitro cell uptake of [ (123)I]2 increased with time. Biodistribution in mice bearing the B16-F10 tumor, after an intravenous injection of [(123)I]2, also showed a time-dependent accumulation of the porphyrin in tumor tissue (10.35 %ID/g at 6 hours). The tumor-to-muscle ratio was 3.49, 3.38, 3.07, and 3.13 at 1, 2, 6, and 24 hours, respectively. The gamma-camera images of (123)I-porphyrin demonstrated a high focal accumulation of radioactivity in the B16-F10 melanoma tumor.
Key concepts: Porphyrin, Biodistribution, High-performance liquid chromatography, Chemistry, Imaging agent, In vitro, Melanoma, Technetium