Abstract
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 β-cyclodextrin (BCD) and hydroxypropyl-β-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.
Keywords: Antioxidant, apoptosis, cyclodextrin, phytocompound, proliferation, rutin.
Current Pharmaceutical Biotechnology
Title:Rutin and Its Cyclodextrin Inclusion Complexes: Physico-chemical Evaluation and in vitro Activity on B164A5 Murine Melanoma Cell Line
Volume: 18 Issue: 13
Author(s): Danciu Corina, Bojin Florina, Pinzaru Iulia*, Dehelean Cristina, Ambrus Rita, Popescu Alexandra, Paunescu Virgil, Monica Hancianu, Minda Daliana and Soica Codruta
Affiliation:
- Department of Toxicology, Faculty of Pharmacy, “Victor Babes” University of Medicine and Pharmacy, Eftimie Murgu Square, No. 2, 300041 Timisoara,Romania
Keywords: Antioxidant, apoptosis, cyclodextrin, phytocompound, proliferation, rutin.
Abstract: 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 β-cyclodextrin (BCD) and hydroxypropyl-β-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.
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Corina Danciu, Florina Bojin, Iulia Pinzaru *, Cristina Dehelean , Rita Ambrus , Alexandra Popescu, Virgil Paunescu , Hancianu Monica, Daliana Minda and Codruta Soica, Rutin and Its Cyclodextrin Inclusion Complexes: Physico-chemical Evaluation and in vitro Activity on B164A5 Murine Melanoma Cell Line, Current Pharmaceutical Biotechnology 2017; 18 (13) . https://dx.doi.org/10.2174/1389201019666180209165523
DOI https://dx.doi.org/10.2174/1389201019666180209165523 |
Print ISSN 1389-2010 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4316 |
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