방사선의학 웹진

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Abstract
Radiometal-labeled porphyrin derivatives have emerged candidates for targeted brain tumor imaging and therapy. In this study, we synthesized a boronic-acid-conjugated porphyrin and radiolabeled it with 64Cu to evaluate its dual-function potential for PET imaging and boron neutron capture therapy (BNCT). The 64Cu-labeled 5,10,15,20-(tetra-4-dihydroxyborylphenyl)-porphyrin ([64Cu]-Cu-TDBP) exhibited excellent serum stability and significant uptake in U87MG cells. PET imaging in both xenograft and orthotopic models demonstrated time-dependent tumor accumulation, with selective localization in the brain tumor at 18 h post-injection (p.i.). The tumor-to-brain ratio increased from 7.2 at 4 h p.i. to 26.3 at 18 h p.i., alongside a rise in tumor boron concentration from 0.79 to 1.83 ppm over the same period. These results highlight the potential of [64Cu]-Cu-TDBP as a promising theranostic agent for precise brain tumor imaging and effective BNCT.

Affiliations

Jae Hun Ahn 1 2, Changkeun Im 1, Soyeon Kim 3, Iqra Bibi 1 4, In Ok Ko 1, Yong Jin Lee 1, Ji-Ae Park 1 4, Choong Mo Kang 1 4
1Division of Applied RI, Korea Institute of Radiological & Medical Sciences (KIRAMS), Seoul 01812, Korea.
2Graduate School of Translational Medicine, Seoul National University College of Medicine, Seoul 03080, Korea.
3Leading Research Center of Total Solution for Osteoporosis Treatment, Chonnam National University, Yeosu 59626, Korea.
4Radiological and Medico-Oncological Sciences, University of Science and Technology (UST), Daejeon 34113, Korea.