Carbonic Anhydrase IX Targeted Polyaspartamide fluorescent Probes for Tumor imaging

Precise intraoperative tumor delineation is essential for successful surgical outcomes. However, conventional methods are often incompetent to provide intraoperative guidance due to lack specificity and sensitivity. Recently fluorescence-guided surgery for tumors to delineate between cancerous and healthy tissues has attracted widespread attention. The contrast-enhanced fluorescent imaging has been applied for non-invasive diagnosis of cancers using tumor-targeting fluorescent probes.

The carbonic anhydrase IX targeted polyaspartamide fluorescent compounds (SD-PHEA-NI) were synthesized by incorporating a tumor-targeting group of sulfadiazine (SD) and N-butyl-4-ethyldiamino-1,8-naphthalimide (NI) into water-soluble carriersof poly-α,β-[N-(2-hydroxyethyl)-L-aspartamide] (PHEA). These derivatives were also characterized by Fourier transform infrared spectroscopy, gel permeation chromatography, ultraviolet-visible spectroscopy, nuclear magnetic resonance spectroscopy and fluorescence assays. The cellular uptake, cytotoxicity, and fluorescence imaging ability were evaluated.

Experiment results indicated that SD-PHEA-NI has low cytotoxic to Henrietta Lacks (HeLa) cells. Moreover, B16F10 melanoma cells can take up SD-PHEA-NI and show good green fluorescent images. However, SD-PHEA-NI displayed a low-intensity green fluorescence signal in healthy human embryonic kidney (293T) cells.

SD-PHEA-NI can be considered a potential fluorescent probe for the detection of tumors. This study has the potential to enhance tumor diagnosis and image-guided surgical interventions by providing real-time information and robust decision support, thereby reducing recurrence and complication rates and ultimately improving patient outcomes.