Discovery and Feasibility Study of Medical Fluorophore 33 as a Novel Theranostic Agent,ACS Applied Materials & Interfaces

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Discovery and Feasibility Study of Medical Fluorophore 33 as a Novel Theranostic Agent
ACS Applied Materials & Interfaces ( IF 8.3 ) Pub Date : 2023-09-15 , 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

Affiliation

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.

中文翻译：

医用荧光团 33 作为新型治疗诊断剂的发现和可行性研究

荧光染料由于其固有的特性而作为治疗诊断平台而受到广泛关注。在这项研究中，我们发现了医用荧光团 33 ( MF33 )，这是一种新型有效的治疗诊断剂，具有苯酚异喹啉盐结构，可作为癌症治疗策略。 MF33的合成可以通过简单的 Rh(III) 催化反应轻松实现。此外， MF33表现出强烈的荧光信号、优异的微粒体稳定性和高体内生物相容性。它通过 p53/p21/caspase-3 信号通路诱导癌细胞显着凋亡，从而对多种癌细胞产生选择性细胞毒性。使用MF33进行体内荧光成像可以实现活体小鼠前哨淋巴结的可视化。值得注意的是，重复腹腔注射MF33可在患有结直肠癌的小鼠中产生抗肿瘤活性。总的来说，我们的研究结果表明，基于苯酚异喹啉盐的MF33是一种用于生物医学成像和癌症治疗的可行的治疗诊断剂。

更新日期：2023-09-15

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