A Tumor-targeting and Mitochondria-anchorable Probe for NIR/MRI Imaging-guided Photodynamic Therapy of Colorectal Cancer

Abstract

Phototherapy is one of important therapeutic modalities for tumor treatment. However, traditional phototherapy still faces huge challenges in clinics. Herein, we rationally design and synthesize a tumor-targeting and mitochondria-anchorable theranostic probe dIR-Gd that consists of a NIR fluorophore IR780, a cyclic peptide cRGD, a sulfenic acid-reactive cyclohexanedione for covalent anchoring, and a MR imaging unit DOTA-Gd3+. Taking advantage of good tumor specificity and covalent immobilization within mitochondria, dIR-Gd is demonstrated to be used for sensitive NIR/MRI imaging and effective photodynamic therapy of αvβ3 integrin overexpressed colorectal tumors. We believe that this covalent mitochondria-targeted probe may provide a powerful and universal means for accurate diagnosis and treatment of tumor.