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

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 evaluate...

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Published inMolecules (Basel, Switzerland) Vol. 26; no. 18; p. 5718
Main Authors Grande, Fedora, Occhiuzzi, Maria Antonietta, Perri, Maria Rosaria, Ioele, Giuseppina, Rizzuti, Bruno, Statti, Giancarlo, Garofalo, Antonio
Format Journal Article
LanguageEnglish
Published Basel MDPI AG 21.09.2021
MDPI
Subjects
Aglycones
anti-enzymatic assays
Binding sites
Biosynthesis
Cholesterol
Citrus fruits
Communication
Cross-breeding
Cultivars
Dietary supplements
Enzymatic activity
Enzymes
flavanones
Flavonoids
Fruits
Functional foods & nutraceuticals
Glycosides
Hesperidin
Hydroxymethylglutaryl-CoA reductase
Hypercholesterolemia
Investigations
Molecular docking
Naringenin
Polyphenols
Prescription drugs
Proteins
Reductases
Statins
Sterols
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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.
AbstractList 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.
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.
Author Garofalo, Antonio
Ioele, Giuseppina
Perri, Maria Rosaria
Statti, Giancarlo
Occhiuzzi, Maria Antonietta
Grande, Fedora
Rizzuti, Bruno
AuthorAffiliation 3 Institute of Biocomputation and Physics of Complex Systems (BIFI), Joint Units IQFR-CSIC-BIFI, and GBsC-CSIC-BIFI, University of Zaragoza, 50018 Zaragoza, Spain
2 CNR-NANOTEC, SS Rende (CS), Department of Physics, University of Calabria, Via P. Bucci, 87036 Rende, Italy; bruno.rizzuti@cnr.it
1 Department of Pharmacy, Health and Nutritional Sciences, University of Calabria, Ampl. Polifunzionale, Via P. Bucci, 87036 Rende, Italy; mariaantonietta.occhiuzzi@unical.it (M.A.O.); mariarosaria.perri@unical.it (M.R.P.); giuseppina.ioele@unical.it (G.I.); giancarlo.statti@unical.it (G.S.); antonio.garofalo@unical.it (A.G.)
AuthorAffiliation_xml – name: 2 CNR-NANOTEC, SS Rende (CS), Department of Physics, University of Calabria, Via P. Bucci, 87036 Rende, Italy; bruno.rizzuti@cnr.it
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– name: 1 Department of Pharmacy, Health and Nutritional Sciences, University of Calabria, Ampl. Polifunzionale, Via P. Bucci, 87036 Rende, Italy; mariaantonietta.occhiuzzi@unical.it (M.A.O.); mariarosaria.perri@unical.it (M.R.P.); giuseppina.ioele@unical.it (G.I.); giancarlo.statti@unical.it (G.S.); antonio.garofalo@unical.it (A.G.)
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Snippet Tacle® is a citrus fruit obtained from the crossbreeding of Clementine and Tarocco cultivars. This fruit retains a promising nutraceutical potential most...
Tacle ® is a citrus fruit obtained from the crossbreeding of Clementine and Tarocco cultivars. This fruit retains a promising nutraceutical potential most...
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proquest
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StartPage 5718
SubjectTerms Aglycones
anti-enzymatic assays
Binding sites
Biosynthesis
Cholesterol
Citrus fruits
Communication
Cross-breeding
Cultivars
Dietary supplements
Enzymatic activity
Enzymes
flavanones
Flavonoids
Fruits
Functional foods & nutraceuticals
Glycosides
Hesperidin
Hydroxymethylglutaryl-CoA reductase
Hypercholesterolemia
Investigations
Molecular docking
Naringenin
Polyphenols
Prescription drugs
Proteins
Reductases
Statins
Sterols
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Title Polyphenols from Citrus Tacle® Extract Endowed with HMGCR Inhibitory Activity: An Antihypercholesterolemia Natural Remedy
URI https://www.proquest.com/docview/2576477394
https://search.proquest.com/docview/2577448653
https://pubmed.ncbi.nlm.nih.gov/PMC8470345
https://doaj.org/article/580c2a413c124249b79437e778255d25
Volume 26
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