title: Synthesis and biologic evaluation of I-123-labeled porphyrin derivative as a potential tumor-imaging agent.
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.
authors.affiliation: Department of Chemistry, Inha University, Inchon, Korea.
authors.forename: Jae Hak
authors.initials: JH
authors.lastname: Lee
authors.forename: Byung Seok
authors.initials: BS
authors.lastname: Moon
authors.forename: Tae Sup
authors.initials: TS
authors.lastname: Lee
authors.forename: Dae Yoon
authors.initials: DY
authors.lastname: Chi
authors.forename: Kwon Soo
authors.initials: KS
authors.lastname: Chun
authors.forename: Gi Jeong
authors.initials: GJ
authors.lastname: Cheon
mesh_terms: D000818:Animals; D045744:Cell Line, Tumor; D005260:Female; D007457:Iodine Radioisotopes; D008546:Melanoma, Experimental / Q000000981:diagnostic imaging / Q000378:metabolism* / Q000473:pathology; D051379:Mice; D008810:Mice, Inbred C57BL; D015394:Molecular Structure; D011166:Porphyrins / Q000138:chemical synthesis / Q000737:chemistry / Q000493:pharmacokinetics*; D011877:Radionuclide Imaging; D019275:Radiopharmaceuticals / Q000138:chemical synthesis / Q000493:pharmacokinetics*; D014018:Tissue Distribution
chemical_list: D007457:Iodine Radioisotopes; D011166:Porphyrins; D019275:Radiopharmaceuticals; C051233:5,10,15,20-tetra(3-hydroxyphenyl)porphyrin