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

Bibliographic Details
Title: Polyphenols from Citrus Tacle® Extract Endowed with HMGCR Inhibitory Activity: An Antihypercholesterolemia Natural Remedy
Authors: Fedora Grande, Maria Antonietta Occhiuzzi, Maria Rosaria Perri, Giuseppina Ioele, Bruno Rizzuti, Giancarlo Statti, Antonio Garofalo
Source: Molecules, Vol 26, Iss 18, p 5718 (2021)
Publisher Information: MDPI AG, 2021.
Publication Year: 2021
Collection: LCC:Organic chemistry
Subject Terms: flavanones, anti-enzymatic assays, molecular docking, Organic chemistry, QD241-441
More Details: 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.
Document Type: article
File Description: electronic resource
Language: English
ISSN: 1420-3049
Relation: https://www.mdpi.com/1420-3049/26/18/5718; https://doaj.org/toc/1420-3049
DOI: 10.3390/molecules26185718
Access URL: https://doaj.org/article/580c2a413c124249b79437e778255d25
Accession Number: edsdoj.580c2a413c124249b79437e778255d25
Database: Directory of Open Access Journals
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More Details
ISSN:14203049
DOI:10.3390/molecules26185718
Published in:Molecules
Language:English