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Open AccessArticle

Anticancer Activity of Rutin and Its Combination with Ionic Liquids on Renal Cells

1
CBIOS—Universidade Lusófona’s Research Center for Biosciences & Health Technologies, Campo Grande 376, 1749-024 Lisboa, Portugal
2
Department of Biomedical Sciences, University of Alcalá, Ctra. Madrid-Barcelona Km. 33.600, Alcalá de Henares, 28871 Madrid, Spain
3
CQE, and Department of Chemistry and Biochemistry, Faculty of Sciences, University of Lisbon, Campo Grande 1749-016 Lisboa, Portugal
4
Department of Pharmacy, School of Pharmaceutical Sciences, University of São Paulo, 580 Prof. Lineu Prestes Av., Bl. 15, São Paulo, SP 05508-900, Brazil
5
iBB-Institute for Bioengineering and Biosciences, Department of Bioengineering, Instituto Superior Técnico, Universidade de Lisboa, 1049-001 Lisboa, Portugal
6
Center for Marine Sciences (CCMar), University of Algarve and Department of Chemistry and Pharmacy, Faculty of Sciences and Technology, University of Algarve, Gambelas Campus, 8005-139 Faro, Portugal (currente adress)
*
Authors to whom correspondence should be addressed.
These authors contributed equally to the senior authorship.
Biomolecules 2020, 10(2), 233; https://doi.org/10.3390/biom10020233
Received: 30 December 2019 / Revised: 24 January 2020 / Accepted: 31 January 2020 / Published: 4 February 2020
(This article belongs to the Special Issue Selected Papers from Bio.Natural Meeting 2019)
The renal cell carcinoma (RCC) is the most common type of kidney cancer. Identifying novel and more effective therapies, while minimizing toxicity, continues to be fundamental in curtailing RCC. Rutin, a bioflavonoid widely found in nature, has shown promising anticancer properties, but with limited applicability due to its poor water solubility and pharmacokinetics. Thus, the potential anticancer effects of rutin toward a human renal cancer cell line (786-O), while considering its safety in Vero kidney cells, was assessed, as well as the applicability of ionic liquids (ILs) to improve drug delivery. Rutin (up to 50 µM) did not show relevant cytotoxic effects in Vero cells. However, in 786-O cells, a significant decrease in cell viability was already observed at 50 µM. Moreover, exposure to rutin caused a significant increase in the sub-G1 population of 786-O cells, reinforcing the possible anticancer activity of this biomolecule. Two choline-amino acid ILs, at non-toxic concentrations, enhanced rutin’s solubility/loading while allowing the maintenance of rutin’s anticancer effects. Globally, our findings suggest that rutin may have a beneficial impact against RCC and that its combination with ILs ensures that this poorly soluble drug is successfully incorporated into ILs–nanoparticles hybrid systems, allowing controlled drug delivery.
Keywords: rutin; renal cancer; 786-O cells; Vero cells; cytotoxicity; cell cycle; ionic liquids; Solubility; ILs–nanoparticles hybrid system rutin; renal cancer; 786-O cells; Vero cells; cytotoxicity; cell cycle; ionic liquids; Solubility; ILs–nanoparticles hybrid system
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MDPI and ACS Style

Caparica, R.; Júlio, A.; Araújo, M.E.M.; Baby, A.R.; Fonte, P.; Costa, J.G.; Santos de Almeida, T. Anticancer Activity of Rutin and Its Combination with Ionic Liquids on Renal Cells. Biomolecules 2020, 10, 233.

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