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Synthesis and in Vitro Biological Evaluation of a Second-Generation Multimodal Water-Soluble Porphyrin-RAPTA Conjugate for the Dual-Therapy of Cancers

Sandland, Jordon; Savoie, Huguette; Boyle, Ross W.; Murray, Benjamin S.

Authors

Jordon Sandland

Huguette Savoie



Abstract

In this study, we report the synthesis and biological evaluation of a novel cationic porphyrin-[Ru(η6-arene)(C2O4)PTA] (RAPTA) conjugate with potential as a multimodal dual-therapeutic agent. In the absence of high intensity light, relative to untreated cells our conjugate resulted in a 83% decrease in viable human adenocarcinoma cells at a concentration of 10 μM, which is significantly more active than the 57% decrease achieved with the same concentration of the unconjugated RAPTA complex alone. With a light dose of 20 J cm–2 (400–1200 nm) a reduction of 98% of viable cells was observed for the same concentration of conjugate. The conjugate is internalized by HT-29 cancer cells as proven by ICP-MS analysis and fluorescence microscopy; the latter result suggests that the conjugate has applications as a multimodal agent by acting as a fluorophore to obtain in vivo biodistribution data. Furthermore, the conjugate has an excellent relative singlet oxygen quantum yield, and the tetrapyrollic unit was found to be photostable under irradiation by either white light or red light.

Citation

Sandland, J., Savoie, H., Boyle, R. W., & Murray, B. S. (2020). Synthesis and in Vitro Biological Evaluation of a Second-Generation Multimodal Water-Soluble Porphyrin-RAPTA Conjugate for the Dual-Therapy of Cancers. Inorganic chemistry, 59(11), 7884-7893. https://doi.org/10.1021/acs.inorgchem.0c01044

Journal Article Type Article
Acceptance Date May 1, 2020
Online Publication Date May 14, 2020
Publication Date Jun 1, 2020
Deposit Date May 16, 2020
Publicly Available Date May 15, 2021
Journal Inorganic Chemistry
Print ISSN 0020-1669
Electronic ISSN 1520-510X
Publisher American Chemical Society
Peer Reviewed Peer Reviewed
Volume 59
Issue 11
Pages 7884-7893
DOI https://doi.org/10.1021/acs.inorgchem.0c01044
Keywords Porphyrin; RAPTA; Dual-therapy; Photosensitiser; Theranostic
Public URL https://hull-repository.worktribe.com/output/3509270
Publisher URL https://pubs.acs.org/doi/10.1021/acs.inorgchem.0c01044