A Ratiometric Fluorescent Probe for Cisplatin: Investigating the Intracellular Reduction of Platinum(IV) Prodrug Complexes

摘要

The Pt-IV prodrug strategy has emerged as an excellent alternative to tackle the problems associated with conventional Pt-II drug therapy. However, there is a lack of tools to study how this new class of Pt-IV drugs are processed at the cellular level. Herein, we report the first ratiometric probe for cisplatin detection and use it to investigate Pt-IV anticancer complexes in biological systems. The probe was able to distinguish between cisplatin and its Pt-IV derivatives, allowing us to probe the intracellular reduction of Pt-IV prodrug complexes. The correlation between the amount of active Pt-II species available after intracellular reduction of Pt-IV complexes and their cytotoxicity and the role glutathione plays in the reduction of Pt-IV complexes were investigated.