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1.
Curr Pharm Biotechnol ; 18(13): 1067-1077, 2017.
Artículo en Inglés | MEDLINE | ID: mdl-29437003

RESUMEN

BACKGROUND: Recent studies have shown that rutin presents a heightened interest due to the plethora of biological activities. The major drawback for this phytocompound is the poor water solubility, a parameter that limits its bioavailability. The study aimed to prepare and assess the inclusion complexes of rutin with ß-cyclodextrin (BCD) and hydroxypropyl-ß-cyclodextrin (HPBCD), followed by the evaluation of the antioxidant, antiproliferative and pro-apoptotic activity against B164A5 murine melanoma cell line. METHODS: Inclusion complexes were prepared by kneading method. Scanning electron microscopy, differential scanning calorimetry and X-ray powder diffraction were used in order to assess their formation. Antioxidant activity was determined by DPPH assay. Antiproliferative and pro-apoptotic effects where tested by MTT, respectively Annexin V-PI assays. Physico-chemical methods proved that incorporation took place. RESULTS: Results show that rutin presents antioxidant activity, and complexation increases this property. After 72 h of incubation at the concentration of 100 µM rutin proved to be an active antiproliferative and pro-apoptotic compound against B164A5 cells. CONCLUSION: Incorporation in BCD and HBCD maintained the activity, thus representing an important finding and open path for in vivo experiments.


Asunto(s)
2-Hidroxipropil-beta-Ciclodextrina , Antineoplásicos , Antioxidantes , Rutina , beta-Ciclodextrinas , 2-Hidroxipropil-beta-Ciclodextrina/química , 2-Hidroxipropil-beta-Ciclodextrina/farmacología , Animales , Antineoplásicos/química , Antineoplásicos/farmacología , Antioxidantes/química , Antioxidantes/farmacología , Apoptosis/efectos de los fármacos , Rastreo Diferencial de Calorimetría , Línea Celular Tumoral , Proliferación Celular/efectos de los fármacos , Ratones , Difracción de Polvo , Rutina/química , Rutina/farmacología , Difracción de Rayos X , beta-Ciclodextrinas/química , beta-Ciclodextrinas/farmacología
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