Dataset Information

Polyphenols from Citrus Tacle® Extract Endowed with HMGCR Inhibitory Activity: An Antihypercholesterolemia Natural Remedy.

ABSTRACT: Tacle® is a citrus fruit obtained from the crossbreeding of Clementine and Tarocco cultivars. This fruit retains a promising nutraceutical potential most likely due to a high content in polyphenols, among which the main constituents are the two glycosides naringin and hesperidin. Herein, we evaluated, through an in vitro assay, the capability of Tacle extracts to inhibit the hydroxymethylglutaryl-CoA reductase enzyme, which plays a key role in cholesterol biosynthesis. The results obtained spurred us to investigate whether the anti-enzymatic activity observed may be due to a direct interaction of aglycones naringenin and hesperetin with the enzyme catalytic site. Molecular docking simulations indicated that these two compounds are able to anchor to the protein with binding modes and affinities similar to those found for statins, which represent mainstream medications against hypercholesterolemia. The overall results showed an interesting nutraceutical potential of Tacle, suggesting that its extract could be used for dietary supplementation in the treatment of moderate hypercholesterolemia.

SUBMITTER: Grande F

PROVIDER: S-EPMC8470345 | biostudies-literature | 2021 Sep

REPOSITORIES: biostudies-literature

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Polyphenols from Citrus Tacle<sup>®</sup> Extract Endowed with HMGCR Inhibitory Activity: An Antihypercholesterolemia Natural Remedy.

Grande Fedora F Occhiuzzi Maria Antonietta MA Perri Maria Rosaria MR Ioele Giuseppina G Rizzuti Bruno B Statti Giancarlo G Garofalo Antonio A

Molecules (Basel, Switzerland) 20210921 18

Tacle<sup>®</sup> is a citrus fruit obtained from the crossbreeding of Clementine and Tarocco cultivars. This fruit retains a promising nutraceutical potential most likely due to a high content in polyphenols, among which the main constituents are the two glycosides naringin and hesperidin. Herein, we evaluated, through an in vitro assay, the capability of Tacle extracts to inhibit the hydroxymethylglutaryl-CoA reductase enzyme, which plays a key role in cholesterol biosynthesis. The results obt ...[more]

PMID: 34577189

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Project description:BackgroundThe COVID-19 pandemic will continue to threaten our health care systems in the next years. In addition to vaccination there is a need for effective tools for prevention and treatment. Products from natural sources, like standardized plant extracts offer a wide range of antiviral effects and possible applications.PurposeThe aim of this study was to investigate, whether a sorbitol/lecithin-based throat spray containing concentrated green tea extract (sGTE) interacts with SARS-CoV-2 viral particles and additionally is capable to block the virus replication.Study design and methodsThe antiviral effect was studied in a VeroE6 cell culture model, including concentration/effect correlations and the biological mechanism of virus blockade, using the Wuhan type of SARS CoV-2 as well as its beta- and delta-mutations. In addition, the qualitative and quantitative tannin profile present on the oral mucosa after spray application has been investigated by LC-MS/MS and HPLC-DAD analyses of (-)-epigallocatechin-3-O-gallate (EGCG) and related catechin derivatives.ResultsThe findings of this study demonstrate, that sGTE has strong neutralizing activity on SARS-CoV-2 resulting in an up to 6,3E+04-fold reduction of infectivity independent from the strain. The type of interaction of sGTE with surface proteins seems to be direct and non-specific concerning the viral surface protein structures and resembles the general non-specific activity of polyphenols. By HPLC-DAD analysis, eight catechins were identified in sGTE, with EGCG and (-)-epicatechin-3-O-gallate as the most abundant ones. The total content of catechin derivatives, calculated as catechin, was 76 g/100 g. LC-MS/MS and HPLC-DAD analyses of throat swabs after application of a sGTE spray have shown that the concentrations of green tea tannins in the pharyngeal mucosa are higher than the effective dose found in the in vitro studies with SARS-CoV-2, even 1 h after the last application.ConclusionThe findings of this study suggest that sGTE has strong neutralizing activity on SARS-CoV-2 independent from the strain (Wuhan strain, beta- or delta-variants). sGTE might be relevant for reduction of corresponding viral infections when periodically applied to mouth and throat.

Dataset Information

Polyphenols from Citrus Tacle® Extract Endowed with HMGCR Inhibitory Activity: An Antihypercholesterolemia Natural Remedy.

Publications

Polyphenols from Citrus Tacle<sup>®</sup> Extract Endowed with HMGCR Inhibitory Activity: An Antihypercholesterolemia Natural Remedy.

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