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Rutin and Its Cyclodextrin Inclusion Complexes: Physico-chemical Evaluation and in vitro Activity on B164A5 Murine Melanoma Cell Line

[ Vol. 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   Pages 1067 - 1077 ( 11 )

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.

Affiliation:

Department of Pharmacognosy, Faculty of Pharmacy, “Victor Babes” University of Medicine and Pharmacy, Eftimie Murgu Square, No. 2, 300041 Timisoara, Department of Functional Sciences, Faculty of Medicine, “Victor Babes” University of Medicine and Pharmacy, Eftimie Murgu Square, No. 2, 300041 Timisoara, Department of Toxicology, Faculty of Pharmacy, “Victor Babes” University of Medicine and Pharmacy, Eftimie Murgu Square, No. 2, 300041 Timisoara, Department of Toxicology, Faculty of Pharmacy, “Victor Babes” University of Medicine and Pharmacy, Eftimie Murgu Square, No. 2, 300041 Timisoara, Department of Pharmaceutical Technology, Faculty of Pharmacy, University of Szeged, Dom ter 8., Szeged H-6720, Department of Physical Chemistry, Faculty of Pharmacy, “Victor Babes” University of Medicine and Pharmacy, Eftimie Murgu Square, No. 2, 300041 Timisoara, Department of Functional Sciences, Faculty of Medicine, “Victor Babes” University of Medicine and Pharmacy, Eftimie Murgu Square, No. 2, 300041 Timisoara, Department of Pharmacognosy, Faculty of Pharmacy, “Gr.T.Popa” University of Medicine and Pharmacy, Universitatii Street, No., 16, 700115, Iasi, Department of Pharmacognosy, Faculty of Pharmacy, “Victor Babes” University of Medicine and Pharmacy, Eftimie Murgu Square, No. 2, 300041 Timisoara, Department of Pharmaceutical Chemistry, Faculty of Pharmacy, “Victor Babes” University of Medicine and Pharmacy, Eftimie Murgu Square, No. 2, 300041 Timisoara

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