Quercetin mitigates valinomycin‐induced cellular stress via stress‐induced metabolism and cell uptake

Gonzales, Gerard Bryan; Smagghe, Guy; Grootaert, Charlotte; Rajković, Andreja; Wiele, Tom Van de; Camp, John Van

doi:10.1002/mnfr.201500999

Cited by 9 publications

(3 citation statements)

References 35 publications

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“…1B, cell viability above 100 % was observed for free quercetin in all concentrations tested. Works reported in literature shows that cytotoxicity is narrowly associated with the oxidative stress in cells (Wang et al, 2014a) and as quercetin and its cellular metabolites have antioxidant properties, this compound is able to promote ROS scavenging due to cellular stress (Gonzales et al, 2016). Similar behaviour for other hydrophobic bioactive compound were reported by Le Maux, Giblin, Croguennec, Bouhallab, and Brodkorb (2012).…”

Section: β-Lg Micro-and Nanostructures Effect On Cell Viabilitysupporting

confidence: 60%

β-lactoglobulin micro- and nanostructures as bioactive compounds vehicle: In vitro studies

Simões

Martins

Pinheiro

et al. 2020

Food Research International

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Lactoglobulin (β-Lg) is known to be capable to bind hydrophilic and hydrophobic bioactive compounds. This research aimed to assess the in vitro performance of β-Lg micro-(diameter ranging from 200 to 300 nm) and nano (diameter < 100 nm) structures associated to hydrophilic and hydrophobic model compounds on Caco-2 cells and under simulated gastrointestinal (GI) conditions. Riboflavin and quercetin were studied as hydrophilic and hydrophobic model compounds, respectively. Cytotoxicity experiment was conducted using in vitro cellular model based on human colon carcinoma Caco-2 cells. Moreover, the digestion process was simulated using the harmonized INFOGEST in vitro digestion model, where samples were taken at each phase of digestion processoral, gastric and intestinal-and characterized in terms of particle size, polydispersity index (PDI), surface charge by dynamic light scattering (DLS); protein hydrolysis degree by 2,4,6-trinitrobenzene sulfonic acid (TNBSA) assay and native polyacrylamide gel electrophoresis; and bioactive compound concentration. Caco-2 cell viability was not affected up to 21 × 10 −3 mg mL −1 of riboflavin and 16 × 10 −3 mg mL −1 quercetin on β-Lg micro-and nanostructures. In the oral phase, β-Lg structures' particle size, PDI and surface charge values were not changed comparing to the initial β-Lg structures (i.e., before being subjected to in vitro GI digestion). During gastric digestion, β-Lg structures were resistant to proteolytic enzymes and to acid environment of the stomachconfirmed by TNBSA and native gel electrophoresis. In vitro digestion results indicated that β-Lg micro-and nanostructures protected both hydrophilic and hydrophobic compounds from gastric conditions and deliver them to target site (i.e., intestinal phase). In addition, β-Lg structures were capable to enhance riboflavin and quercetin bioaccessibility and bioavailability potential compared to bioactive compounds in their free form. This study indicated that β-Lg micro-and nanostructures were capable to enhance hydrophilic and hydrophobic compounds bioavailability potential and they can be used as oral delivery systems.

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Section: β-Lg Micro-and Nanostructures Effect On Cell Viabilitysupporting

confidence: 60%

β-lactoglobulin micro- and nanostructures as bioactive compounds vehicle: In vitro studies

Simões

Martins

Pinheiro

et al. 2020

Food Research International

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“…In vitro, the dose of 50 µM quercetin was based on a previous report. [ 57 ] RAW264.7 macrophages were treated with 50 µM quercetin with or without other reagents, after 24 h, cells were collected for bioassays.…”

Section: Methodsmentioning

confidence: 99%

Quercetin Attenuates Atherosclerotic Inflammation by Inhibiting Galectin‐3‐NLRP3 Signaling Pathway

Xiao

et al. 2021

Molecular Nutrition Food Res

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Scope Atherosclerosis is the underlying pathogenesis of cardiovascular events caused by inflammation, and dietary intervention has been recommended as one fundamental prevention strategy. Herein, the anti‐arteriosclerotic properties of quercetin are investigated by modulating galectin‐3 (Gal‐3)‐NLR family, pyrin domain‐containing 3 (NLRP3) pathway. Methods and results Plaques from ApoE−/− mice fed by high‐fat diet (HFD) with or without quercetin (100 mg (kg·bw)−1) for 16 weeks, and carotid plaques from patients with carotid stenosis are collected for histopathological examinations and molecular mechanism assays. Quercetin significantly alleviates atherosclerotic lesions and reduces lipid retention caused by HFD. Proteomic technology identified Gal‐3 increased by HFD but lowered by quercetin. Furthermore, immunofluorescence and immunohistochemistry exhibit higher expressions of Gal‐3 and NLRP3 in carotid plaques and plaques from HFD‐fed mice, which are concurrently down‐regulated by quercetin. Similar to TD139, quercetin dramatically suppresses NLRP3 inflammasome activation in oxidized low‐density lipoprotein‐laden macrophages, and accordingly alleviates cellular steatosis and IL‐1β secretion, which is abolished by recombinant Gal‐3. Co‐immunoprecipitation shows Gal‐3 binding to NLRP3 promotes inflammasome activation. Conclusion Gal‐3 initiates inflammatory lesions by activating NLRP3 inflammasome which functions as a candidate target of quercetin exerting favorable anti‐atherogenic effects. The findings highlight a promising strategy for atherosclerosis prevention and treatment by naturally‐occurring quercetin.

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“…Methyl-quercetin was found to accumulate more in valinomycin-stressed cells than in unstressed undifferentiated Caco-2 cells treated with quercetin. More interestingly, quercetin and its methyl-ester derivative were found on the cell membrane of the unstressed cells, whereas they localised intracellularly upon exposure to valinomycin, which caused a recovery in cellular viability and reduction of intracellular reactive oxygen species ( 49 ) . These results are interesting as they point to the possibility that local/ in situ concentrations of flavonoids (in the affected cells) could be much higher than the concentration of the metabolites in the blood.…”

Section: Use Of Flavonoid Aglycones In In Vitro Bioactivity Assaysmentioning

confidence: 99%

In vitro bioavailability and cellular bioactivity studies of flavonoids and flavonoid-rich plant extracts: questions, considerations and future perspectives

Gonzales

2016

Proc. Nutr. Soc.

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In vitro techniques are essential in elucidating biochemical mechanisms and for screening a wide range of possible bioactive candidates. The number of papers published reporting in vitro bioavailability and bioactivity of flavonoids and flavonoid-rich plant extracts is numerous and still increasing. However, even with the present knowledge on the bioavailability and metabolism of flavonoids after oral ingestion, certain inaccuracies still persist in the literature, such as the use of plant extracts to study bioactivity towards vascular cells. There is therefore a need to revisit, even question, these approaches in terms of their biological relevance. In this review, the bioavailability of flavonoid glycosides, the use of cell models for intestinal absorption and the use of flavonoid aglycones and flavonoid-rich plant extracts in in vitro bioactivity studies will be discussed. Here, we focus on the limitations of current in vitro systems and revisit the validity of some in vitro approaches, and not on the detailed mechanism of flavonoid absorption and bioactivity. Based on the results in the review, there is an apparent need for stricter guidelines on publishing data on in vitro data relating to the bioavailability and bioactivity of flavonoids and flavonoid-rich plant extracts.

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Quercetin mitigates valinomycin‐induced cellular stress via stress‐induced metabolism and cell uptake

Cited by 9 publications

References 35 publications

β-lactoglobulin micro- and nanostructures as bioactive compounds vehicle: In vitro studies

β-lactoglobulin micro- and nanostructures as bioactive compounds vehicle: In vitro studies

Quercetin Attenuates Atherosclerotic Inflammation by Inhibiting Galectin‐3‐NLRP3 Signaling Pathway

In vitro bioavailability and cellular bioactivity studies of flavonoids and flavonoid-rich plant extracts: questions, considerations and future perspectives

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