Synthesis and biologic evaluation of I-123-labeled porphyrin derivative as a potential tumor-imaging agent.
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.
Lee
Jae Hak
JH
Department of Chemistry, Inha University, Inchon, Korea.
Moon
Byung Seok
BS
Lee
Tae Sup
TS
Chi
Dae Yoon
DY
Chun
Kwon Soo
KS
Cheon
Gi Jeong
GJ
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
D007457:Iodine Radioisotopes; D011166:Porphyrins; D019275:Radiopharmaceuticals; C051233:5,10,15,20-tetra(3-hydroxyphenyl)porphyrin