β-Galactosidase-activated theranostic for hepatic carcinoma therapy and imaging.

A β-galactosidase activatable fluorescent turn-on theranostic Gal-CGem exhibits gemcitabine release specifically in β-galactosidase overexpressing hepatic carcinoma cells. The cytotoxicity of Gal-CGem in cancer cells is achieved through the apoptotic cell death pathway. Overall, Gal-CGem is a new frontline prodrug in cancer therapy that has provided antineoplastic information through fluorescence imaging.

Cell-specific activation of gemcitabine by endogenous HS stimulation and tracking through simultaneous fluorescence turn-on.

The endogenous HS-driven theranostic H2S-Gem has been invented. The theranostic prodrug H2S-Gem is selectively activated in cancer cells, releasing active gemcitabine with a simultaneous fluorescence turn-on. H2S-Gem selectively inhibited cancer cell growth compared to the mother chemotherapeutic gemcitabine.