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Evaluation of the In Vitro and In Vivo Efficacy of Ruthenium Polypyridyl Compounds against Breast Cancer

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Instituto de Tecnologia Química e Biológica António Xavier, ITQB, Av. da República, EAN, 2780-157 Oeiras, Portugal
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UCIBIO, Departamento Ciências da Vida, NOVA School of Science and Technology, Universidade Nova de Lisboa, Campus Caparica, 2829-516 Caparica, Portugal
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Associate Laboratory i4HB—Institute for Health and Bioeconomy, NOVA School of Science and Technology, NOVA University Lisbon, 2819-516 Caparica, Portugal
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Departamento de Zoología, Genética y Antropología Física. Facultad de Veterinaria, Universidade de Santiago de Compostela, 27002 Lugo, Spain
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Preclinical Animal Models Group, Health Research Institute of Santiago de Compostela (IDIS), 15706 Santiago de Compostela, Spain
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Departamento de Química, Centro de Investigaciones Científicas Avanzadas (CICA), Universidade da Coruña, 15008 A Coruña, Spain
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Authors to whom correspondence should be addressed.
Academic Editor: Giovanni Natile
Int. J. Mol. Sci. 2021, 22(16), 8916; https://doi.org/10.3390/ijms22168916
Received: 9 July 2021 / Revised: 31 July 2021 / Accepted: 10 August 2021 / Published: 18 August 2021
(This article belongs to the Section Molecular Genetics and Genomics)
The clinical success of cisplatin, carboplatin, and oxaliplatin has sparked the interest of medicinal inorganic chemistry to synthesize and study compounds with non-platinum metal centers. Despite Ru(II)–polypyridyl complexes being widely studied and well established for their antitumor properties, there are not enough in vivo studies to establish the potentiality of this type of compound. Therefore, we report to the best of our knowledge the first in vivo study of Ru(II)–polypyridyl complexes against breast cancer with promising results. In order to conduct our study, we used MCF7 zebrafish xenografts and ruthenium complexes [Ru(bipy)2(C12H8N6-N,N)][CF3SO3]2Ru1 and [{Ru(bipy)2}2(μ-C12H8N6-N,N)][CF3SO3]4Ru2, which were recently developed by our group. Ru1 and Ru2 reduced the tumor size by an average of 30% without causing significant signs of lethality when administered at low doses of 1.25 mg·L−1. Moreover, the in vitro selectivity results were confirmed in vivo against MCF7 breast cancer cells. Surprisingly, this work suggests that both the mono- and the dinuclear Ru(II)–polypyridyl compounds have in vivo potential against breast cancer, since there were no significant differences between both treatments, highlighting Ru1 and Ru2 as promising chemotherapy agents in breast cancer therapy. View Full-Text
Keywords: ruthenium; polypyridyl compounds; cytotoxicity; cell death; cell cycle; in vivo toxicity; MCF7 zebrafish xenograft ruthenium; polypyridyl compounds; cytotoxicity; cell death; cell cycle; in vivo toxicity; MCF7 zebrafish xenograft
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MDPI and ACS Style

Lenis-Rojas, O.A.; Roma-Rodrigues, C.; Fernandes, A.R.; Carvalho, A.; Cordeiro, S.; Guerra-Varela, J.; Sánchez, L.; Vázquez-García, D.; López-Torres, M.; Fernández, A.; Fernández, J.J. Evaluation of the In Vitro and In Vivo Efficacy of Ruthenium Polypyridyl Compounds against Breast Cancer. Int. J. Mol. Sci. 2021, 22, 8916. https://doi.org/10.3390/ijms22168916

AMA Style

Lenis-Rojas OA, Roma-Rodrigues C, Fernandes AR, Carvalho A, Cordeiro S, Guerra-Varela J, Sánchez L, Vázquez-García D, López-Torres M, Fernández A, Fernández JJ. Evaluation of the In Vitro and In Vivo Efficacy of Ruthenium Polypyridyl Compounds against Breast Cancer. International Journal of Molecular Sciences. 2021; 22(16):8916. https://doi.org/10.3390/ijms22168916

Chicago/Turabian Style

Lenis-Rojas, Oscar A., Catarina Roma-Rodrigues, Alexandra R. Fernandes, Andreia Carvalho, Sandra Cordeiro, Jorge Guerra-Varela, Laura Sánchez, Digna Vázquez-García, Margarita López-Torres, Alberto Fernández, and Jesús J. Fernández 2021. "Evaluation of the In Vitro and In Vivo Efficacy of Ruthenium Polypyridyl Compounds against Breast Cancer" International Journal of Molecular Sciences 22, no. 16: 8916. https://doi.org/10.3390/ijms22168916

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