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Photodynamic antitumor activity of Ru(II) complexes of imidazo-phenanthroline conjugated hydroxybenzoic acid as the tumour targeting photosensitizers

Abstract

Two novel Ru(II) polypyridyl complexes bearing imidazo-phenanthroline conjugated hydroxybenzoic acid were designed to enhance tumor targeting as the photosenistizers for photodynamic therapy. [Ru(bpy)2(phcpip)] (ClO4)2 (Ru-1) and [Ru(bpy)2(ohcpip)] (ClO4)2 (Ru-2) (bpy = 2,2'-Bipyridine; phcpip = 2-(3-carboxyl-4-hydroxyphenyl) imidazo [4,5-f]phenanthroline; ohcpip = 2-(2-hydroxyl-3-carboxyphenyl) imidazo [4,5-f] [1,10] phenanthroline) were synthesized and their photodynamic antitumor activity were investigated. Both complexes displayed high photocytotoxicity toward cancerous cell lines HepG2, A549, MCF-7, and MDA-MB-231, but low photocytotoxicity toward normal cell lines GES-1 and Huvec. They were mainly localized at the nucleus of HepG2 cells after 24 h incubation, arrested the cell cycle at the G2/M phase and induced cancer cell apoptosis through reactive oxygen species (ROS) mediated pathways. Tumor targeting of the complexes is attributed to stronger molecular binding to DNA.

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Publication details

The article was received on 26 Sep 2019, accepted on 29 Nov 2019 and first published on 02 Dec 2019


Article type: Paper
DOI: 10.1039/C9TB02103E
J. Mater. Chem. B, 2019, Accepted Manuscript

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    Photodynamic antitumor activity of Ru(II) complexes of imidazo-phenanthroline conjugated hydroxybenzoic acid as the tumour targeting photosensitizers

    Z. Liu, J. Zhang, Y. Sun, C. Zhu, Y. Lu, J. Wu, J. Li, H. Liu and Y. Ye, J. Mater. Chem. B, 2019, Accepted Manuscript , DOI: 10.1039/C9TB02103E

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