Anticancer activity of rutin and its combination with ionic liquids in renal cancer

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Anticancer activity of rutin and its combination with ionic liquids in renal cancer

Friday, 24.04.2020

Rutin is a bioflavonoid widely found in nature that has shown several promising pharmacological properties, including antitumor activity. However, the low solubility of this compound remains one of the limiting factors of its applicability. In the published article “Anticancer Activity of Rutin and Its Combination with Ionic Liquids on Renal Cells”, the antitumor activity of rutin was demonstrated in 786-O cells, an in vitro model of human renal carcinoma, in which this activity had not yet been studied. Additionally, it was observed that the combination of rutin with ionic liquids (IL) significantly increased its solubility and incorporation in hybrid systems of IL-Nanoparticles, while maintaining the antitumor activity.


Authors and Affiliations:

Rita Caparica 1,2, Ana Júlio 1,2, Maria Eduarda Machado Araújo 3, André Rolim Baby 4, Pedro Fonte 1,5,6,7, João Guilherme Costa 1,† and Tânia Santos de Almeida 1,3,†

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  Center for Marine Sciences (CCMar), University of Algarve, Gambelas Campus, 8005-139 Faro, Portugal

6  Department of Chemistry and Pharmacy, Faculty of Sciences and Technology, University of Algarve, Gambelas Campus, 8005-139 Faro, Portugal

7  iBB - Institute for Bioengineering and Biosciences, Department of Bioengineering, Instituto Superior Técnico, Universidade de Lisboa, 1049-001 Lisboa, Portugal


† These authors contributed equally to this work



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.


Journal: Biomolecules (ISSN 2218-273X; CODEN: BIOMHC)