Anti-MDR Effects of Quercetin and its Nanoemulsion in Multidrug-Resistant Human Leukemia Cells

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Author(s): Maiara Bernardes Marques, Ayane Pontes Machado, Priscila Antiqueira Santos, Michele Carrett-Dias, Gabriela Soares Araújo, Barbara da Silva Alves, Bárbara Santos de Oliveira, Flavio M. R. da Silva Júnior, Cristiana Lima Dora, Andrés Delgado Cañedo, Daza M. V. B. Filgueira, Estela Fernandes e Silva*, Ana Paula de Souza Votto

Journal Name: Anti-Cancer Agents in Medicinal Chemistry
(Formerly Current Medicinal Chemistry - Anti-Cancer Agents)

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Background: The quercetin has potential against the multidrug resistance (MDR) phenotype, but with low bioavailability. The increase in the bioavailability can be obtained with nanostructures.

Objective: To analyze the effects of quercetin and its nanoemulsion on MDR and non-MDR cells.

Method: We used: high pressure homogenization for nanoemulsion production; Trypan Blue for cytostatic/cytotoxicity assays; Epifluorescence microscope (with specific probes) for apoptosis and DNA damage; Real Time PCR for gene expression; AutoDock Vina for docking and Flow Cytometry for efflux analysis. The quercetin exerted antiproliferative impact, induced apoptosis, necrosis and DNA damage on cells.

Results: Quercetin combined with vincristine showed an effect similar to verapamil (an ABCB1 inhibitor), and the docking showed that bind to ABCB1 in a similar region. The quercetin also was capable of to alter ABCB1 gene expression. The quercetin in nanoemulsion maintained the cytotoxic and cytostatic effects of quercetin which may increase bioavailability. Besides, the unloaded nanoemulsion was able to inhibit per se the efflux activity of ABCB1, demonstrating the pharmacological action of this structure.

Conclusion: The quercetin may be considered as a prospective drug to overcome resistance in cancer cells and its nanoemulsion can be an alternative for in vivo application.

Keywords: Docking, ABCB1, proliferation inhibition, apoptosis, nanoemulsion, DNA damage.

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(E-pub Ahead of Print)
DOI: 10.2174/1871520621999210104200722
Price: $95

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