Abstract
Quercetin is a member of the flavonoid group of compounds, which is abundantly present in various dietary sources. It has excellent antioxidant properties and anti-inflammatory activity and is very effective as an anti-cancer agent against various types of tumors, both in vivo and in vitro. Quercetin has been also reported to modulate the activity of some members of the multidrug-resistance transporters family, such as P-gp, ABCC1, ABCC2, and ABCG2, and the activity of ecto-5′-nucleotidase (NT5E/CD73), a key regulator in some tumor processes such as invasion, migration, and metastasis. In this study, we investigated the effect of Quercetin on ABCC6 expression in HepG2 cells. ABCC6 is a member of the superfamily of ATP-binding cassette (ABC) transporters, poorly involved in drug resistance, whose mutations cause pseudoxanthoma elasticum, an inherited disease characterized by ectopic calcification of soft connective tissues. Recently, it has been reported that ABCC6 contributes to cytoskeleton rearrangements and HepG2 cell motility through purinergic signaling. Gene and protein expression were evaluated by quantitative Reverse-Transcription PCR (RT-qPCR) and western blot, respectively. Actin cytoskeleton dynamics was evaluated by laser confocal microscopy using fluorophore-conjugated phalloidin. Cell motility was analyzed by an in vitro wound-healing migration assay. We propose that ABCC6 expression may be controlled by the AKT pathway as part of an adaptative response to oxidative stress, which can be mitigated by the use of Quercetin-like flavonoids.
Highlights
Quercetin is a member of the flavonoid group of compounds, which is abundantly present in various dietary sources like vegetables, fruits, spices, tea, and wine
In order to assess the effect of Quercetin on cells viability, an MTT assay was performed on HepG2 cells treated with different concentrations of Quercetin, ranging from 660 to 82.5 μM, for 24 and 48 h
Most studies have been focused on P-gp, BCRP, and MRP1, which have a major role in drug resistance, but very limited information is available on different transporters and, on ABCC6, to our knowledge [41]
Summary
Quercetin is a member of the flavonoid group of compounds, which is abundantly present in various dietary sources like vegetables, fruits, spices, tea, and wine. Quercetin is usually present as a glycoside, though the aglycone moiety is absorbed after deglycosylation in the gut. Thanks to its ability to bind transition metal ions [2] and to scavenge free radicals, Quercetin has excellent antioxidant properties attributed to the catechol group in the B ring and the OH group at position 3 of the A ring [3]. Quercetin is effective against O2− and ONOO− and can terminate lipid peroxidation, which has deleterious effects especially on the cardiovascular and nervous systems [4,5]. Quercetin shows good anti-inflammatory activity by reducing Lipopolysaccharide (LPS)-induced expression of Tumor Necrosis Factor (TNF) TNF-α and Interleukin (IL)-1α [6] and by preventing the production of the inflammatory enzymes lipoxygenases (LOX) and cyclooxygenases (COX) [7]
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