1. Academic Validation
  2. Discovery and Feasibility Study of Medical Fluorophore 33 as a Novel Theranostic Agent

Discovery and Feasibility Study of Medical Fluorophore 33 as a Novel Theranostic Agent

  • ACS Appl Mater Interfaces. 2023 Oct 4;15(39):45539-45548. doi: 10.1021/acsami.3c05971.
Kwang Hee Son 1 Da Sol Lee 1 Geumi Park 1 So Yeon Jeon 1 Jae-Eon Lee 1 Hui-Jeon Jeon 2 Sijoon Lee 1 Woo-Jin Park 3 Yeonju Shin 4 Seong Gon Kim 4 Dong-Seok Lee 5 6 Ye Ri Han 2 Dong-Su Kim 4 Yong Hyun Jeon 1
Affiliations

Affiliations

  • 1 Preclinical Research Center, Daegu-Gyeongbuk Medical Innovation Foundation (K-MEDIhub), 80 Cheombok-ro, Dong-gu, Daegu 41061, Republic of Korea.
  • 2 New Drug Development Center, Daegu-Gyeongbuk Medical Innovation Foundation (K-MEDIhub), 80 Cheombok-ro, Dong-gu, Daegu 41061, Republic of Korea.
  • 3 Department of Chemistry, Center for NanoMedicine, Institute for Basic Science (IBS), Seoul 03722, Republic of Korea.
  • 4 Therapeutics and Biotechnology Division, Korea Research, Institute of Chemical Technology, 141 Gajeongro, Yuseong, Daejeon 31414, South Korea.
  • 5 School of Life Sciences, BK21 FOUR KNU Creative BioResearch Group, Kyungpook National University, Daegu 41566, Republic of Korea.
  • 6 School of Life Sciences & Biotechnology, College of Natural Sciences, Kyungpook National University, Daegu 41566, Republic of Korea.
Abstract

Fluorescent dyes have garnered significant attention as theranostic platforms owing to their inherent characteristics. In this study, we present the discovery of Medical Fluorophore 33 (MF33), a novel and potent theranostic agent with a phenaleno-isoquinolinium salt structure that can serve as a Cancer therapeutic strategy. The synthesis of MF33 is readily achievable through a simple Rh(III)-catalyzed reaction. Moreover, MF33 displayed strong fluorescence signals, excellent microsomal stability, and high biocompatibility in vivo. It induces significant Apoptosis in Cancer cells via the p53/p21/Caspase-3 signaling pathway, leading to selective cytotoxicity in various Cancer cells. In vivo fluorescence imaging with MF33 enabled the visualization of sentinel lymph nodes in living mice. Notably, repeated intraperitoneal administration of MF33 resulted in antitumor activity in mice with colorectal Cancer. Collectively, our findings suggest that phenaleno-isoquinolinium salt-based MF33 is a viable theranostic agent for biomedical imaging and Cancer treatment.

Keywords

cancer therapy; fluorescent dye; medical fluorophore; phenaleno-isoquinolinium; sentinel lymph nodes; theranostic.

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