A rhodamine-based single-molecular theranostic agent for multiple-functionality tumor therapy

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.