Cisplatin-eugenol Pt(IV) prodrugs target colon cancer stem cells: A novel strategy for enhanced anticancer efficacy

Vojtech Novohradsky, Tomer Babu, Hana Kostrhunova, Menucha Plaskow, Lenka Markova, Sourav Acharya, Dan Gibson*, Viktor Brabec*

*Corresponding author for this work

Research output: Contribution to journalArticlepeer-review

Abstract

Platinum(IV) compounds possess distinct properties that set them apart from platinum(II) compounds. Often designed as prodrugs, they are reduced within cancer cells to their active platinum(II) form, enabling their cytotoxic effects. Their versatility also lies in their ability to be functionalized and conjugated with bioactive molecules to enhance cancer cell targeting. This report introduces new prodrugs that combine antitumor cisplatin with axially coordinated eugenol, leveraging their synergistic action to target cancer stem cells. A third bioactive ligand, 4-phenylbutyrate or octanoate, was added to further enhance biological activity, creating 'triple action' prodrugs. These new platinum(IV) prodrugs offer a novel approach to cancer therapy by improving targeting, increasing efficacy, overcoming drug resistance, and reducing tumor invasiveness while sparing healthy tissue.

Original languageEnglish
Article number117854
JournalBiomedicine and Pharmacotherapy
Volume183
DOIs
StatePublished - Feb 2025

Bibliographical note

Publisher Copyright:
© 2025

Keywords

  • Cancer stem cells
  • Cisplatin
  • Eugenol
  • Platinum(IV)
  • Spheroids

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