Issue 24, 2017

Synthesis, photophysical properties and in vitro evaluation of a chlorambucil conjugated ruthenium(ii) complex for combined chemo-photodynamic therapy against HeLa cells

Abstract

The combination of chemotherapy with photodynamic therapy can lead to improved therapeutic efficiencies and reduced side effects compared to conventional chemotherapy. Chlorambucil (CHL) is a DNA alkylating agent, but problems like drug instability, “off-target” binding and in situ monitoring after administration often limit its clinical application. In this regard, we designed a new heteroleptic Ru(II) complex CHL-RuL, bearing a CHL conjugated pendant, which is desired to serve as an image-guided chemo-photodynamic combined theranostic agent. CHL-RuL shows considerable promise as a photosensitizer for two-photon excitation photodynamic therapy: strong and wide UV-Vis absorption bands centered around 400 nm, strong red emission (∼702 nm) with a long lifetime at the microsecond level, moderate singlet oxygen quantum yield, and significant two-photon absorption cross-section (118 GM). More interestingly, this chemical modification affords CHL-RuL greater cellular uptake and remarkable mitochondria accumulation in HeLa cells. Furthermore, CHL-RuL shows a slight selective cytotoxicity toward carcinoma HeLa cells over normal MRC-5 cells. MTT assay results and two-photon scanning cell imaging demonstrate that CHL-RuL exhibits obvious chemo-photodynamic dual action against HeLa cells.

Graphical abstract: Synthesis, photophysical properties and in vitro evaluation of a chlorambucil conjugated ruthenium(ii) complex for combined chemo-photodynamic therapy against HeLa cells

Supplementary files

Article information

Article type
Paper
Submitted
14 Mar 2017
Accepted
08 May 2017
First published
08 May 2017

J. Mater. Chem. B, 2017,5, 4623-4632

Synthesis, photophysical properties and in vitro evaluation of a chlorambucil conjugated ruthenium(II) complex for combined chemo-photodynamic therapy against HeLa cells

J. Zhang, M. Pan and C. Su, J. Mater. Chem. B, 2017, 5, 4623 DOI: 10.1039/C7TB00702G

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