Bioavailability of the dietary antioxidant flavonol quercetin in man

doi:10.1016/S0304-3835(97)04644-2

Cancer Letters

Volume 114, Issues 1–2, 19 March 1997, Pages 139-140

https://doi.org/10.1016/S0304-3835(97)04644-2 Get rights and content

Abstract

Quercetin, a dietary antioxidant flavonoid, has anticarcinogenic properties. We quantified the absorption of quercetin in ileostomists. Absorption was 52 ± 5% for quercetin glucosides from onions, 17 ± 15% for quercetin rutinoside, and 24 ± 9% for quercetin aglycone. The plasma quercetin concentration in subjects with an intact colon, after ingestion of fried onions, apples and pure quercetin rutinoside, decreased slowly with elimination half-lives of about 25 h. Thus, repeated dietary intake of quercetin will lead to accumulation in plasma. The relative bioavailability of quercetin from apples and rutinoside was onethird of that from onions. Absorption kinetics and bioavailibility might be determined by the type of glycoside. Dietary quercetin could increase the antioxidant capacity of blood plasma.

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This study investigated the possibility of improving the antioxidant activities and solubilities of quercetin (QUE) and isoquercetin (IQUE) through a combination of nanoencapsulation with gel incorporation. QUE- and IQUE-loaded nanoparticles (QUE and IQUE NPs, respectively) were prepared through ionic gelation between chitooligosaccharide and poly-γ-glutamic acid. The antioxidant activities of QUE and IQUE increased by 2.5 and 3.5 times, respectively, after nanoencapsulation. Furthermore, QUE and IQUE NP-filled gelatin gels (G-QUE and G-IQUE NPs, respectively) showed higher antioxidant stabilities than QUE and IQUE NPs, respectively. G-QUE and G-IQUE NPs exhibited significantly (p < 0.05) higher G’ values than free QUE and IQUE in gels, respectively. Moreover, the hardness of G-QUE NPs was significantly (p < 0.05) higher than that of free QUE in gel. In conclusion, combining nanoencapsulation and gel incorporation can improve the antioxidant activities, stabilities, and physical properties of QUE and IQUE.
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The aim of the study was to investigate the effects of cross-linkers on quercetin (QUE) absorption characteristics of QUE-loaded chitosan nanoparticles (CS-NPs). CS-NPs (461.2–482.7 nm) were prepared by ionic gelation at pH 3.5 using tripolyphosphate (367.9 Da), dextran sulfate (>15 kDa), arabic gum (AG, >250 kDa), or hyaluronic acid (HA, >1000 kDa). Mucoadhesion and cell permeation of QUE were significantly increased by positive charged CS-NPs due to interactions with negatively charged mucosal layer. Moreover, CS-AG and CS-HA NPs prepared with relatively higher MW cross-linkers exhibited significantly higher adhesion and permeation than the others. These results were verified by a cellular antioxidant activity assay; CS-AG (137.5 unit) and CS-HA NPs (126.5 unit) showed significantly higher activities after internalization into Caco-2 cells. Therefore, encapsulation within CS-NPs prepared using high MW cross-linkers such as AG and HA is found to be potentially valuable techniques for improving the QUE absorption.
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Quercetin is an antioxidant flavonol very sensible to light and oxidants that can benefit from stabilisation by encapsulation into cyclodextrins. In this work we study the solid inclusion compounds of quercetin with β- and γ-cyclodextrins (β-CD and γ-CD) obtained by freeze-drying. Combined results from microanalysis, FT-IR, powder X-ray diffraction, ¹³C{¹H} CP/MAS NMR spectroscopy and thermogravimetry demonstrating that γ-CD, having a larger cavity, is the most adequate host to form a stable inclusion complex with quercetin. The anti-peroxidation capacity of the compounds was determined and followed the order β-CD·quercetin ≫ quercetin > γ-CD·quercetin. Both γ-CD·quercetin and β-CD·quercetin are able to inhibit DPPH radicals at a rate three times faster than pure quercetin, but their EC₅₀ is higher (50 μM vs 17 μM for quercetin). The practical applicability of the two CD·quercetin adducts as nutraceutical additives in fresh cheese was established. Fortified fresh cheese had a firmer texture and yellowish colour, but no significant changes in the overall sensorial qualities were found by a panel of non-trained tasters when compared with the control (non-treated fresh cheese).
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Hepatocellular carcinoma (HCC) pathogenesis involves the interplay of multiple signalling pathways. Notch and Hedgehog (Hh) are two major developmental pathways that act in concert to regulate adult cell repair. CK2α -serine-threonine kinase-down-regulation enhanced apoptotic activity and was proven beneficial for HCC patients. Quercetin is a bioactive flavonoid and has been shown to protect against HCC through its antioxidant activity. This study was carried out to elucidate the antineoplastic effect of quercetin through regulating both Notch and Hh pathways, apoptosis, cell proliferation and CK2α activity.
Hepatocellular carcinoma was induced in male Sprague Dawley rats by thioacetamide. Quercetin was administered in both protective and curative doses. Parameters of liver function and oxidative stress were assessed. CK2α, Notch and Hh pathways were evaluated using RT-PCR and ELISA. Apoptosis was investigated by detecting caspase-3, caspase-8 and p53. Proliferative and cell cycle markers as cyclin D1 and Ki-67 were detected immunohistochemically.
Quercetin inhibited CK2α and downregulated mRNA and protein expression of Notch1 and Gli2. Quercetin also suppressed caspase-3 expression but not caspase-8. Quercetin elevated p53 expression whereas proliferative and cell cycle markers cyclin D1 and Ki-67 were downregulated. Markers of hepatic cellular integrity such as AST, ALT, ALP, GGT, albumin and bilirubin were significantly ameliorated. This was confirmed by histological examination. Quercetin also alleviated oxidative stress as shown by SOD, GSH, MDA and NO levels.
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Bioavailability of the dietary antioxidant flavonol quercetin in man

Abstract

Am. J. Clin. Nutr.

Mammalian metabolism of flavonoids

Intake of potentially anticarcinogenic flavonoids and their determinants in adults in the Netherlands

Nutr. Cancer