Abstract

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.

Highlights

  • Renal cell carcinoma (RCC) is the most common type of kidney malignancy in adults that is established in the renal proximal convoluted tubules [1,2]

  • The MTT assay was used to evaluate the impact of rutin (0–250 μM; 48 h) treatment on the cell viability of two renal cell lines, the Vero normal kidney cells, and the 786-O human renal cancer cells

  • Our results showed that rutin did not induce relevant cytotoxicity up to 50 μM, at concentrations higher than 50 μM the cell viability of Vero cells significantly decreased

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Summary

Introduction

Renal cell carcinoma (RCC) is the most common type of kidney malignancy in adults that is established in the renal proximal convoluted tubules [1,2]. RCC is highly vascularized and can metastasize to different body sites, including lungs, liver, and bones [2,3]. The clear cell RCC (ccRCC) is the most common type, comprising approximately 70%–80% of the RCC cases [3,4,5,6]. The effectiveness of the surgery highly depends on the grade and stage of the disease and the presence or absence of metastasis [4,5]. It becomes essential to find new, safe, and more effective treatments against RCC

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