Live intraoperative diagnosis of hepatic metastasis via HDACs targeting molecular theranostic agent

[Display omitted] •Theranostic agent (CBHAc) was designed based on β-carboline derivative.•CBHAc possessed both HDACs targeting and pH-responsive fluorescence characteristics.•Preciously intraoperative real-time diagnosis for micrometastases was developed.•Significant suppression against colon cancer and hepatic matastasis was achieved. Precise diagnosis and effective treatment of cancer metastasis remain a great challenge in the clinic. Theranostic agents that consist of both diagnostic and therapeutic components have gained great interest in cancer therapy. Herein, we report an intraoperative theranostic strategy for the accurate live detection of micrometastases with selective chemotherapeutic activity using a small multifunctional agent (CBHAc). Combining histone deacetylase (HDACs) targeting and pH-responsive fluorescence characteristics, CBHAc provided highly sensitive and selective real-time fluorescence diagnosis for microtumors in zebrafish and hepatic micrometastases in mice. Furthermore, CBHAc demonstrated significant tumor inhibition against colon cancer and hepatic matastasis, prolonging the survival of tumor-bearing mice through attenuating epithelial-mesenchymal transition (EMT). Therefore, this cancer-targeting fluorescence agent delivers a new platform for both intraoperative diagnosis and suppression of cancer metastasis in surgery, broadening the impact of multifunctional agents for theranostic precision medicine.