4.8 Article

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

期刊

ANGEWANDTE CHEMIE-INTERNATIONAL EDITION
卷 58, 期 1, 页码 164-167

出版社

WILEY-V C H VERLAG GMBH
DOI: 10.1002/anie.201810361

关键词

cisplatin; fluorescent probes; glutathione; platinum; prodrugs

资金

  1. Ministry of Education
  2. National University of Singapore [R143-000-A53-114]

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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.

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