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1.
Foods ; 10(1)2020 Dec 23.
Article in English | MEDLINE | ID: mdl-33374616

ABSTRACT

Antioxidants are powerful compounds that help the body to destroy the excess of endogenous radical species responsible for many severe conditions like neurodegenerative, inflammatory, and cardiovascular impairments, and even some forms of cancer [...].

2.
Biomolecules ; 10(2)2020 02 04.
Article in English | MEDLINE | ID: mdl-32033222

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.


Subject(s)
Antineoplastic Agents/administration & dosage , Carcinoma, Renal Cell/drug therapy , Drug Carriers/chemistry , Ionic Liquids/chemistry , Kidney Neoplasms/drug therapy , Rutin/administration & dosage , Animals , Antineoplastic Agents/chemistry , Antineoplastic Agents/pharmacology , Carcinoma, Renal Cell/pathology , Cell Cycle/drug effects , Cell Line, Tumor , Cell Survival/drug effects , Chlorocebus aethiops , Drug Liberation , Humans , Kidney Neoplasms/pathology , Nanoparticles/chemistry , Rutin/chemistry , Rutin/pharmacology , Solubility , Vero Cells
3.
Braz. J. Pharm. Sci. (Online) ; 55: e17695, 2019. tab, graf
Article in English | LILACS | ID: biblio-1039080

ABSTRACT

The influence of common tea preparation procedures (temperature, infusion time, consumption time interval and tea bag/loose-leaf) and the type of water used, on the total phenolic content (TPC), the radical scavenging activity and the α-glucosidase inhibitory activity were assessed. Higher TPC and antioxidant activity were obtained when using lower mineralized waters. Tea bags also evidenced higher antioxidant activity than loose-leaf samples. Under the same conditions (90 ºC and five minutes of infusion time) green tea contains almost twice the quantity of polyphenols and the free radical scavenging ability of black tea. In the α-glucosidase assay all infusions were active (97-100 %). Furthermore, HPLC allowed to identify some of the polyphenols present in both teas and to monitor their composition change with time. After twenty-four hours, the antioxidant activity was maintained without significant changes, but a small decrease in enzyme inhibition was observed, although this activity was still very high


Subject(s)
Tea/classification , alpha-Glucosidases/analysis , Antioxidants/analysis , Water/analysis , Chromatography, High Pressure Liquid/methods , Polyphenols
4.
Pharmaceutics ; 10(4)2018 Dec 19.
Article in English | MEDLINE | ID: mdl-30572636

ABSTRACT

The development of effective forms to incorporate poorly soluble drugs into delivery systems remains a problem. Thus, it is important to find alternatives such as finding excipients that increase drug solubility. Ionic liquids (ILs), particularly choline-based ILs, have been studied as solubility enhancers in drug delivery systems. Nonetheless, to acknowledge this property as a functionality, it needs to be proven at non-toxic concentrations. Hence, herein two choline-amino acid ILs were studied as functional excipients by evaluating their influence on the solubility of the poorly water-soluble ferulic acid and rutin, while considering their safety. The solubility of the drugs was always higher in the presence of the ILs than in water. Ionic liquids did not affect the radical scavenging activity of the drugs or the cell viability. Moreover, stable oil-in-water (O/W) emulsions were prepared containing each drug and the ILs, allowing a significantly higher drug loading. Globally, our results suggest that choline-based ILs may act as green functional excipients, since at non-toxic concentrations they considerably improve drug solubility/loading, without influencing the antioxidant activity of the drugs, the cell viability, or the stability of the formulations.

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