A naphthalimide-based peptide conjugate for concurrent imaging and apoptosis induction in cancer cells by utilizing endogenous hydrogen sulfide

Abstract

The excessive production of endogenous hydrogen sulfide (H2S) in cancer cells leads to enhanced tumor growth and metastasis. On the other hand, decreased endogenous H2S suppresses tumor growth. The reported approaches for inhibiting tumor growth are selective silencing of the tumor-promoting genes and pharmacological inhibition of these proteins. To enhance the antitumor efficacy of frontline chemotherapeutic agents, herein, we synthesized a highly sensitive endogenous H2S responsive fluorescent probe,i.e., a hydrogen sulfide-sensing naphthalimide-based peptide conjugate (HSNPc), which showed selective inhibition of proliferation of cancer cells due to apoptosis induction. Furthermore,HSNPcsuppressed the glycolytic reserve, a critical energy source for the proliferation of cancer cells.HSNPcalso decreased the Young's modulus of HeLa cells compared to the control cells, which demonstrated a direct relation between cell apoptosis and cell stiffness. Taken together, we demonstrated the dual function of detection and killing of cancer cells byHSNPcthat can be likened to a theranostic role.