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Issue 14, 2018
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A long-lived cuprous bis-phenanthroline complex for the photodynamic therapy of cancer

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Abstract

Copper is an earth-abundant and a biologically essential metal that offers a promising alternative to noble metals in photochemistry and photobiology. In this work, a series of sterically encumbered Cu(I) bis-phenanthroline complexes were investigated for their use in photochemotherapy (PCT). It was found that Cu(dsbtmp)2+ [dsbtmp = 2,9-disec-butyl-3,4,7,8-tetramethyl-1,10-phenanthroline] (compound 3), which possessed the longest excited state lifetime, exhibited significant in vitro photocytotoxicity on A375 (human malignant melanoma) and A549 (human lung carcinoma) cell lines. Fluorescence imaging demonstrated the significant uptake and localization of compound 3 in a perinuclear fashion. A comet assay indicated the induction of DNA damage in the dark. The DNA breaks were significantly amplified upon photoactivation. The light-induced enhancement of cytotoxicity was associated with the formation of reactive oxygen species (ROS), a known intermediate in photodynamic therapy (PDT). This successful demonstration of photocytotoxicity using long-lived cuprous phenanthroline paves the way to exploit this class of photosensitizers for PDT applications.

Graphical abstract: A long-lived cuprous bis-phenanthroline complex for the photodynamic therapy of cancer

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Publication details

The article was received on 11 Jan 2018, accepted on 27 Feb 2018 and first published on 27 Feb 2018


Article type: Paper
DOI: 10.1039/C8DT00140E
Citation: Dalton Trans., 2018,47, 4959-4967
  • Open access: Creative Commons BY-NC license
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    A long-lived cuprous bis-phenanthroline complex for the photodynamic therapy of cancer

    C. Al Hageh, M. Al Assaad, Z. El Masri, N. Samaan, M. El-Sibai, C. Khalil and R. S. Khnayzer, Dalton Trans., 2018, 47, 4959
    DOI: 10.1039/C8DT00140E

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