Department of Pharmacy, Health and Nutritional Sciences, University of Calabria, Ampl. Polifunzionale, Via P. Bucci, 87036 Rende, Italy.
CNR-NANOTEC, SS Rende (CS), Department of Physics, University of Calabria, Via P. Bucci, 87036 Rende, Italy.
Molecules. 2021 Sep 21;26(18):5718. doi: 10.3390/molecules26185718.
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.
塔克莱是一种由克莱门氏小柑橘和塔罗科血橙杂交而成的柑橘类水果。这种水果由于富含多酚类物质，具有很大的潜在药用价值，其中主要成分为两种糖苷柚皮苷和橙皮苷。本文通过体外试验评估了塔克莱提取物抑制羟甲基戊二酰辅酶 A 还原酶的能力，该酶在胆固醇生物合成中起着关键作用。试验结果促使我们研究观察到的抗酶活性是否可能是由于柚皮苷和橙皮苷苷元与酶催化部位的直接相互作用所致。分子对接模拟表明，这两种化合物能够以与他汀类药物相似的结合模式和亲和力与蛋白质结合，他汀类药物是治疗高胆固醇血症的主流药物。总体结果表明塔克莱具有有趣的营养保健品潜力，提示其提取物可用于治疗中度高胆固醇血症的膳食补充。
