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Article

Interaction with Blood Proteins of a Ruthenium(II) Nitrofuryl Semicarbazone Complex: Effect on the Antitumoral Activity

by
Bruno Demoro
1,
Andreia Bento-Oliveira
2,3,
Fernanda Marques
4,
João Costa Pessoa
5,
Lucía Otero
1,
Dinorah Gambino
1,*,
Rodrigo F. M. de Almeida
2,3 and
Ana Isabel Tomaz
2,*
1
Cátedra de Química Inorgánica, Facultad de Química, Universidad de la República—UDELAR, 11800 Montevideo, Uruguay
2
Centro de Química Estrutural, Faculdade de Ciências—CQE-FCUL, Universidade de Lisboa, 1749-016 Lisbon, Portugal
3
Centro de Química e Bioquímica, Faculdade de Ciências da Universidade de Lisboa, 1749-016 Lisbon, Portugal
4
Centro de Ciências Tecnológicas e Nucleares, Instituto Superior Técnico—C2TN-Técnico, Universidade de Lisboa, Campus Tecnológico e Nuclear, 2686-953 Sacavém, Portugal
5
Centro de Química Estrutural, Departamento de Engenharia Química, Instituto Superior Técnico, Universidade de Lisboa, 1049-001 Lisbon, Portugal
*
Authors to whom correspondence should be addressed.
Molecules 2019, 24(16), 2861; https://doi.org/10.3390/molecules24162861
Submission received: 10 July 2019 / Revised: 2 August 2019 / Accepted: 5 August 2019 / Published: 7 August 2019
(This article belongs to the Special Issue Medicinal Importance of Ruthenium Compounds)
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Abstract

The steady rise in the cancer burden and grim statistics set a vital need for new therapeutic solutions. Given their high efficiency, metallodrugs are quite appealing in cancer chemotherapy. This work examined the anticancer activity of an anti-trypanosomal ruthenium-based compound bearing the 5-nitrofuryl pharmacophore, [RuII(dmso)2(5-nitro-2-furaldehyde semicarbazone)] (abbreviated as RuNTF; dmso is the dimethyl sulfoxide ligand). The cytotoxicity of RuNTF was evaluated in vitro against ovarian adenocarcinoma, hormone-dependent breast adenocarcinoma, prostate carcinoma (grade IV) and V79 lung fibroblasts human cells. The activity of RuNTF was similar to the benchmark metallodrug cisplatin for the breast line and inactive against the prostate line and lung fibroblasts. Given the known role of serum protein binding in drug bioavailability and the distribution via blood plasma, this study assessed the interaction of RuNTF with human serum albumin (HSA) by circular dichroism (CD) and fluorescence spectroscopy. The fluorescence emission quenching from the HSA-Trp214 residue and the lifetime data upon RuNTF binding evidenced the formation of a 1:1 {RuNTF-albumin} adduct with log Ksv = (4.58 ± 0.01) and log KB = (4.55 ± 0.01). This is supported by CD data with an induced CD broad band observed at ~450 nm even after short incubation times. Importantly, the binding to either HSA or human apo-transferrin is beneficial to the cytotoxicity of the complex towards human cancer cells by enhancing the cytotoxic activity of RuNTF.
Keywords: ruthenium(II); 5-nitrofurylsemicarbazone; cancer; cytotoxicity; plasma protein binding; fluorescence; circular dichroism; conditional binding constants; human serum albumin; human serum apo-transferrin. ruthenium(II); 5-nitrofurylsemicarbazone; cancer; cytotoxicity; plasma protein binding; fluorescence; circular dichroism; conditional binding constants; human serum albumin; human serum apo-transferrin.
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MDPI and ACS Style

Demoro, B.; Bento-Oliveira, A.; Marques, F.; Costa Pessoa, J.; Otero, L.; Gambino, D.; F. M. de Almeida, R.; Tomaz, A.I. Interaction with Blood Proteins of a Ruthenium(II) Nitrofuryl Semicarbazone Complex: Effect on the Antitumoral Activity. Molecules 2019, 24, 2861. https://doi.org/10.3390/molecules24162861

AMA Style

Demoro B, Bento-Oliveira A, Marques F, Costa Pessoa J, Otero L, Gambino D, F. M. de Almeida R, Tomaz AI. Interaction with Blood Proteins of a Ruthenium(II) Nitrofuryl Semicarbazone Complex: Effect on the Antitumoral Activity. Molecules. 2019; 24(16):2861. https://doi.org/10.3390/molecules24162861

Chicago/Turabian Style

Demoro, Bruno, Andreia Bento-Oliveira, Fernanda Marques, João Costa Pessoa, Lucía Otero, Dinorah Gambino, Rodrigo F. M. de Almeida, and Ana Isabel Tomaz. 2019. "Interaction with Blood Proteins of a Ruthenium(II) Nitrofuryl Semicarbazone Complex: Effect on the Antitumoral Activity" Molecules 24, no. 16: 2861. https://doi.org/10.3390/molecules24162861

APA Style

Demoro, B., Bento-Oliveira, A., Marques, F., Costa Pessoa, J., Otero, L., Gambino, D., F. M. de Almeida, R., & Tomaz, A. I. (2019). Interaction with Blood Proteins of a Ruthenium(II) Nitrofuryl Semicarbazone Complex: Effect on the Antitumoral Activity. Molecules, 24(16), 2861. https://doi.org/10.3390/molecules24162861

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