Chemiluminescent Self-Activating Photosensitizers for Selective Anticancer Therapy

first_page settings Order Article Reprints Font Type: Arial Georgia Verdana Font Size: Aa Aa Aa Line Spacing:    Column Width:    Background: Open AccessAbstract Chemiluminescent Self-Activating Photosensitizers for Selective Anticancer Therapy † by Carla M. Magalhães 1,*, Patricia González-Berdullas 1, Joaquim C. G. Esteves da Silva 1,2 and Luís Pinto da Silva 1,2 1 Chemistry Research Unit (CIQUP), Institute of Molecular Sciences (IMS), Department of Geosciences, Environment and Territorial Planning, Faculty of Sciences, University of Porto, Rua do Campo Alegre s/n, 4169-007 Porto, Portugal 2 LACOMEPHI, GreenUPorto, Department of Geosciences, Environment and Territorial Planning, Faculty of Sciences, University of Porto, Rua do Campo Alegre s/n, 4169-007 Porto, Portugal * Author to whom correspondence should be addressed. † Presented at the 8th International Electronic Conference on Medicinal Chemistry, 1–30 November 2022; Available online: https://ecmc2022.sciforum.net/. Med. Sci. Forum 2022, 14(1), 37; https://doi.org/10.3390/ECMC2022-13174 Published: 1 November 2022 Download Download PDF Download PDF with Cover Download XML Download Supplementary Material Versions Notes Keywords: chemiluminescence; self-illuminating; tumor-selective; anticancer Cancer is a challenging disease to treat, regarding treatment efficiency and side-effects. To overcome these problems, extensive studies are exploring therapies with reduced side-effects, such as photodynamic therapy (PDT). PDT has advantages over conventional therapies; however, its dependence on light limits it to treating tumors under the skin/on the outer lining of organs [1]. We developed new photosensitizers that can self-activate intracellularly with tumor selectivity based on chemiluminescent reactions involving a cancer marker. The photosensitizer is directly chemiexcited to a triplet excited state generating singlet oxygen, without an external light source. Thus, we aimed to develop self-activating photosensitizers which can be used for light-free photodynamic therapy, eliminating its light-related restrictions [2,3]. Cytotoxicity assays with breast and prostate cell lines showed that the novel photosensitizers possess significant toxicity toward tumor cells, while not affecting normal cells. Furthermore, we compared the activity of these compounds with reference chemotherapeutic drugs, finding higher cytotoxicity [3]. Supplementary MaterialsThe conference presented material is available at: https://www.mdpi.com/article/10.3390/ECMC2022-13174/s1.Author ContributionsConceptualization, L.P.d.S.; Funding acquisition, L.P.d.S.; Investigation, C.M.M. and P.G.-B.; Supervision, J.C.G.E.d.S. and L.P.d.S.; Visualization, C.M.M. and P.G.-B.; Writing—original draft, C.M.M.; Writing—review & editing, J.C.G.E.d.S. and L.P.d.S. All authors have read and agreed to the published version of the manuscript.FundingThe Portuguese “Fundação para a Ciência e Tecnologia” (FCT, Lisbon) is acknowledged for funding of project PTDC/QUI-QFI/2870/2020. Carla Magalhães acknowledges FCT for funding her PhD grant (SFRH/143211/2019). Luís Pinto da Silva also acknowledges funding from FCT (CEECINST/00069/2021).Institutional Review Board StatementNot applicable.Informed Consent StatementNot applicable.AcknowledgmentsThe Laboratory of Computational Modelling of Environmental Pollutant-Human Interactions (LACOMEPHI) and the Materials Center of the University of Porto (CEMUP) are acknowledged.Conflicts of InterestThe authors declare no conflict of interest.ReferencesMagalhães, M.; Esteves, C.G.; Pinto, L. Chemiluminescence and bioluminescence as an excitation source in the photodynamic therapy of cancer: A critical review. Chem. Phys. Chem. 2016, 17, 2286–2294. [Google Scholar] [CrossRef] [PubMed]da Silva, L.P.; Núnez-Montenegro, A.; Magalhães, C.M.; Ferreira, P.J.O.; Duarte, D.; Gonzalez-Berdullas, P.; Rodríguez-Borges, J.E.; Vale, N.; da Silva, J.C.G.E. Single-molecule chemiluminescent photosensitizer for a self-activating and tumor-selective photodynamic therapy of cancer. Eur. J. Med. Chem. 2019, 183, 111683. [Google Scholar] [CrossRef] [PubMed]da Silva, L.P.; Magalhães, C.M.; Núñez-Montenegro, A.; Ferreira, P.J.O.; Duarte, D.; Rodríguez-Borges, J.E.; Vale, N.; da Silva, J.C.G.E. Study of the combination of self-activating photodynamic therapy and chemotherapy for cancer treatment. Biomolecules 2019, 9, 384. [Google Scholar] [CrossRef] [PubMed]Publisher’s Note: MDPI stays neutral with regard to jurisdictional claims in published maps and institutional affiliations. © 2022 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (https://creativecommons.org/licenses/by/4.0/). Share and Cite MDPI and ACS Style Magalhães, C.M.; González-Berdullas, P.; Silva, J.C.G.E.d.; Silva, L.P.d. Chemiluminescent Self-Activating Photosensitizers for Selective Anticancer Therapy. Med. Sci. Forum 2022, 14, 37. https://doi.org/10.3390/ECMC2022-13174 AMA Style Magalhães CM, González-Berdullas P, Silva JCGEd, Silva LPd. Chemiluminescent Self-Activating Photosensitizers for Selective Anticancer Therapy. Medical Sciences Forum. 2022; 14(1):37. https://doi.org/10.3390/ECMC2022-13174 Chicago/Turabian Style Magalhães, Carla M., Patricia González-Berdullas, Joaquim C. G. Esteves da Silva, and Luís Pinto da Silva. 2022. 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