Porphyrin-Based Tumor-Targeting Theranostic Agent: Gd-TDAP

Soyeon Kim; Ji-Ung Yang; Jae Hun Ahn; In Ok Ko; Jung Young Kim; Yong Jin Lee; Ji-Ae Park

doi:10.1021/acsmedchemlett.1c00283

Porphyrin-Based Tumor-Targeting Theranostic Agent: Gd-TDAP

ACS Med Chem Lett. 2021 Aug 13;12(9):1459-1463. doi: 10.1021/acsmedchemlett.1c00283. eCollection 2021 Sep 9.

Authors

Soyeon Kim^{1

2}, Ji-Ung Yang^{1

2}, Jae Hun Ahn^{1

3}, In Ok Ko¹, Jung Young Kim¹, Yong Jin Lee¹, Ji-Ae Park¹

Affiliations

¹ Division of Applied RI, Korea Institute of Radiological & Medical Sciences (KIRAMS), Seoul 01812, Korea.
² Department of Medical & Biological Engineering, Kyungpook National University, Daegu 41566, Korea.
³ Graduate School of Translational Medicine, Seoul National University College of Medicine, Seoul 03080, Korea.

Abstract

The aim of this work was to evaluate a tumor-targeting porphyrin-based gadolinium complex (Gd-TDAP) for use as an MR/optical imaging agent and potential therapeutic agent. Gd-TDAP had higher longitudinal relaxivity (11.8 mM^-1 s^-1) than a commercial MRI contrast agent (Omniscan; 3.7 mM^-1 s^-1) in HSA solution (0.67 mM) at 3 T. The tumor-targeting characteristics were confirmed by T₁-weighted MR imaging and optical imaging using an orthotopic brain tumor mouse model, which showed 1.3-fold higher uptake in tumor compared to normal brain tissues. The cell fraction data using U87MG glioblastoma cells indicated the potential for gadolinium neutron capture therapy (Gd-NCT), which requires gadolinium to be inside the cell nucleus. In addition, porphyrin derivatives can be used for photodynamic therapy (PDT), and the results demonstrated that Gd-TDAP has great potential not only as a bimodal imaging agent but also for treatment.