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

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...

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Autores principales: Caparica, Rita, Júlio, Ana, Araújo, Maria Eduarda Machado, Baby, André Rolim, Fonte, Pedro, Costa, João Guilherme, Santos de Almeida, Tânia
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2020
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7072522/
https://www.ncbi.nlm.nih.gov/pubmed/32033222
http://dx.doi.org/10.3390/biom10020233
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author Caparica, Rita
Júlio, Ana
Araújo, Maria Eduarda Machado
Baby, André Rolim
Fonte, Pedro
Costa, João Guilherme
Santos de Almeida, Tânia
author_facet Caparica, Rita
Júlio, Ana
Araújo, Maria Eduarda Machado
Baby, André Rolim
Fonte, Pedro
Costa, João Guilherme
Santos de Almeida, Tânia
author_sort Caparica, Rita
collection PubMed
description 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.
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spelling pubmed-70725222020-03-19 Anticancer Activity of Rutin and Its Combination with Ionic Liquids on Renal Cells Caparica, Rita Júlio, Ana Araújo, Maria Eduarda Machado Baby, André Rolim Fonte, Pedro Costa, João Guilherme Santos de Almeida, Tânia Biomolecules Article 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. MDPI 2020-02-04 /pmc/articles/PMC7072522/ /pubmed/32033222 http://dx.doi.org/10.3390/biom10020233 Text en © 2020 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 (http://creativecommons.org/licenses/by/4.0/).
spellingShingle Article
Caparica, Rita
Júlio, Ana
Araújo, Maria Eduarda Machado
Baby, André Rolim
Fonte, Pedro
Costa, João Guilherme
Santos de Almeida, Tânia
Anticancer Activity of Rutin and Its Combination with Ionic Liquids on Renal Cells
title Anticancer Activity of Rutin and Its Combination with Ionic Liquids on Renal Cells
title_full Anticancer Activity of Rutin and Its Combination with Ionic Liquids on Renal Cells
title_fullStr Anticancer Activity of Rutin and Its Combination with Ionic Liquids on Renal Cells
title_full_unstemmed Anticancer Activity of Rutin and Its Combination with Ionic Liquids on Renal Cells
title_short Anticancer Activity of Rutin and Its Combination with Ionic Liquids on Renal Cells
title_sort anticancer activity of rutin and its combination with ionic liquids on renal cells
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7072522/
https://www.ncbi.nlm.nih.gov/pubmed/32033222
http://dx.doi.org/10.3390/biom10020233
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