2. Academic Validation
  3. Synthesis and evaluation of radiolabeled porphyrin derivatives for cancer diagnoses and their nonradioactive counterparts for photodynamic therapy

Synthesis and evaluation of radiolabeled porphyrin derivatives for cancer diagnoses and their nonradioactive counterparts for photodynamic therapy

  • RSC Med Chem. 2022 Sep 22;13(12):1565-1574. doi: 10.1039/d2md00234e.
Nur Izni Ramzi 1,  Kenji Mishiro 2,  Masayuki Munekane 1,  Takeshi Fuchigami 1,  Xiaojun Hu 3,  Renata Jastrząb 4,  Yoji Kitamura 5,  Seigo Kinuya 6,  Kazuma Ogawa 1 2
Affiliations

Affiliations

  • 1 Graduate School of Pharmaceutical Sciences, Kanazawa University Kakuma-machi Kanazawa Ishikawa 920-1192 Japan kogawa@p.kanazawa-u.ac.jp.
  • 2 Institute for Frontier Science Initiative, Kanazawa University Kakuma-machi Kanazawa Ishikawa 920-1192 Japan.
  • 3 Center for Molecular Recognition and Biosensing, School of Life Sciences, Shanghai University Shanghai 200444 China.
  • 4 Faculty of Chemistry, Adam Mickiewicz University of Poznan Uniwersytetu Poznanskiego 8 Poznan 61-614 Poland.
  • 5 Research Center for Experimental Modeling of Human Disease, Kanazawa University Takara-machi 13-1 Kanazawa Ishikawa 920-8640 Japan.
  • 6 Department of Nuclear Medicine, Kanazawa University Hospital, Kanazawa University Takara-machi 13-1 Kanazawa Ishikawa 920-8641 Japan.
PMID: 36561065 DOI: 10.1039/d2md00234e
Abstract

Radioiodinated porphyrin derivatives and the corresponding nonradioactive iodine introduced compounds, [125I]I-TPPOH ([125I]3), [125I]I-l-tyrosine-TPP ([125I]9), I-TPPOH (3), and I-l-tyrosine-TPP (9) were designed, synthesized, and evaluated by in vitro and in vivo experiments. In cytotoxicity assays, 3 and 9 exhibited significant cytotoxicity under light conditions but did not show significant cytotoxicity without light irradiation. Biodistribution experiments with [125I]3 and [125I]9 showed similar distribution patterns with high retention in tumors. In photodynamic therapeutic (PDT) experiments, 3 and 9 at a dose of 13.6 μmol kg-1 weight with 50 W single light irradiation onto the tumor area significantly inhibited tumor growth. These results indicate that the iodinated porphyrin derivatives [123/natI]3 and [123/natI]9 are promising Cancer theranostic agents.

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