A zinc(II) phthalocyanine conjugated with an oxaliplatin derivative for dual chemo- and photodynamic therapy

Research output: Journal Publications and Reviews (RGC: 21, 22, 62)21_Publication in refereed journal

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Author(s)

  • Janet T. F. Lau
  • Pui-Chi Lo
  • Wing-Ping Fong
  • Dennis K. P. Ng

Detail(s)

Original languageEnglish
Pages (from-to)5446-5454
Journal / PublicationJournal of Medicinal Chemistry
Volume55
Issue number11
Publication statusPublished - 14 Jun 2012
Externally publishedYes

Abstract

A novel zinc(II) phthalocyanine substituted with an oxaliplatin derivative via a triethylene glycol linker has been synthesized. The two components work in a cooperative manner in the antitumor action. The conjugate shows a cytotoxic effect in the dark due to the cytostatic oxaliplatin moiety and an enhanced cytotoxicity upon illumination due to the photosensitizing phthalocyanine unit against the HT29 human colon adenocarcinoma cells. The IC 50 value of the conjugate is as low as 0.11 μM, which is 5-fold lower than that of the reference compound without the platinum complex. The high photodynamic activity of the conjugate can be attributed to its high cellular uptake and efficiency in generating intracellular reactive oxygen species. The conjugate also shows preferential localization in the lysosomes of the cells and induces cell death mainly through apoptosis. © 2012 American Chemical Society.