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.
Highlights
Hypercholesterolemia is a disorder characterized by the presence of high levels of cholesterol in the blood
The first-line remedies against hypercholesterolemia are represented by statins, either synthetic or contained in natural extracts such as the one obtained from red yeast rice made by fermenting white rice with various strains of the mold Monascus purpureus [2,3]
Hesperidin and naringin content of the extract were quantified in 310.5 ± 8.4 and 188.7 ± 5.6 ppm, respectively, while the content of hesperetin and naringenin resulted in 86.3 ± 6.4 and 212.0 ± 7.8 ppm, respectively
Summary
Hypercholesterolemia is a disorder characterized by the presence of high levels of cholesterol in the blood. The first-line remedies against hypercholesterolemia are represented by statins, either synthetic or contained in natural extracts such as the one obtained from red yeast rice made by fermenting white rice with various strains of the mold Monascus purpureus [2,3] These drugs have been shown to be capable of inhibiting hydroxymethylglutaryl-CoA reductase (HMGCR), the enzyme that plays a central role in the production of cholesterol in the liver. Several preparations obtained from various parts of plants belonging to the Citrus genus have been recognized as effective in mildly lowering hematic cholesterol This activity was attributed to diverse compounds such as phenol derivatives, polyphenols, and sterols that are present in juices and purees of these fruits [10]. The capability of the aglycones to bind the enzyme active site was investigated by docking studies
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