A Ratiometric Fluorescent Probe for Cisplatin: Investigating the Intracellular Reduction of Platinum(IV) Prodrug Complexes. Issue 1 (4th December 2018)

• Record Type: Journal Article
• Authors: Ong, Jun Xiang; Lim, Carine Shu Qing; Le, Hai Van; Ang, Wee Han
• Is Part Of: Angewandte Chemie international edition. Volume 58:Issue 1(2018)
• Page Start: 164
• Page End: 167
• Publication Date: 2018-12-04
• Subjects: cisplatin -- fluorescent probes -- glutathione -- platinum -- prodrugs; Chemistry -- Periodicals; 540
• DOI: 10.1002/anie.201810361
• Languages: English
• ISSNs: 1433-7851

Abstract

Abstract: 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. Abstract : Watching closely : A ratiometric fluorescent probe was engineered to detect the clinically relevant platinum drug cisplatin. The ability to distinguish platinum(II) species from their parental platinum(IV) complexes allowed the application of the probe to the study of the activation of platinum(IV) carboxylate prodrug complexes within a complex intracellular environment.