A rhodamine-based single-molecular theranostic agent for multiple-functionality tumor therapy. (July 2019) - Qu, Xiaofang
Abstract: In the fight against cancer, it is urgently necessary to design a single-molecular theranostic agent (SMTA) for simultaneous diagnosis and therapy. However, this goal has not been accomplished. Here, to achieve this ambition, a chemotherapy drug of the aromatic nitrogen mustard class is covalently conjugated onto a small molecule, rhodamine, as an SMTA for the first time. The SMTA can perform multiple functionalities, including mitochondrial-targeted delivery, near-infrared (NIR) fluorescence imaging, NIR photodynamic therapy, and chemotherapy. We verified the synergetic anti-cancer effect through both in vitro and in vivo experiments. Our SMTA may provide a new avenue to explore multiple-functionality anti-cancer agents in theranostics. Graphical abstract: A novel single-molecular theranostic agent (RAC ) has been designed for explore multiple-functionality anticancer prodrug in theranostics. It provides a platform for simultaneous mitochondrial-targeted delivery, NIR fluorescence imaging and high-efficiency synergetic NIR photodynamic-chemo cancer therapy.Image 1 Highlights: A SMAT is designed for explore multiple-functionality anticancer agents in theranostics. The introduction of aromatic nitrogen mustard to rhodamine generated the PDT-chemo synergistic effect. The SMAT is able to image and mitochondrial-targeted delivery cancer cells as well as tumors. The first example of a SMAT based on rhodamine has been found and applied in biological systems.