Synthesis and biological studies of new multifunctional curcumin platforms for anticancer drug delivery

Andrii Bazylevich, Helena Tuchinsky, Eti Zigman-Hoffman, Ran Weissman, Ofer Shpilberg, Oshrat Hershkovitz-Rokah, Leonid Patsenker, Gary Gellerman

Research output: Contribution to journalArticlepeer-review

Abstract

Background: Scientists have extensively investigated curcumin, yielding many publications on treatments of cancer. Numerous derivatives of curcumin were synthesized, evaluated for their anti-oxidant and free-radical scavenging, SAR, ADME properties and tested in anticancer applications. Objective: We decided to exploit curcumin as a bioactive core platform for carrying anticancer drugs, which likely possesses a carboxyl moiety for potential linkage to the carrier for drug delivery. Methods: The goal of this work is to develop biolabile multifunctional curcumin platforms towards anticancer drug delivery, including determination of drug release profiling in hydrolytic media, in vitro cytotoxicity, antioxidant properties and blockage of relevant cell survival pathways. Results: We report on a facile synthesis of the bioactive multifunctional curcumin-based platforms linked to a variety of anticancer drugs like amonafide and chlorambucil, and release of the drugs in a hydrolytic environment. The leading curcumin-based platform has presented antioxidant activity similar to curcumin, but with much more potent cytotoxicity in vitro in agreement with the augmented blockage of the NF-κB cell survival pathway. Conclusion: The approach presented here may prove beneficial for bioactive curcumin-based delivery applications where multiple drug delivery is required in a consecutive and controlled mode.

Original languageEnglish
Pages (from-to)537-549
Number of pages13
JournalMedicinal Chemistry
Volume15
Issue number5
DOIs
StatePublished - 1 Jan 2019
Externally publishedYes

Keywords

  • Anticancer
  • Antioxidant
  • Bifunctional
  • Curcumin
  • Platform
  • Stability

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