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多酚类营养补充剂 Taurisolo 的血管作用:关注对内皮功能的保护。

Vascular Effects of the Polyphenolic Nutraceutical Supplement Taurisolo: Focus on the Protection of the Endothelial Function.

机构信息

Department of Pharmacy, University of Pisa, Via Bonanno 6, 56126 Pisa, Italy.

Interdepartmental Research Center "Nutrafood: Nutraceutica e Alimentazione per la Salute", University of Pisa, 56126 Pisa, Italy.

出版信息

Nutrients. 2021 May 2;13(5):1540. doi: 10.3390/nu13051540.

DOI:10.3390/nu13051540
PMID:34063322
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC8147644/
Abstract

Preservation of vascular endothelium integrity and functionality represents an unmet medical need. Indeed, endothelial dysfunction leads to decreased nitric oxide biosynthesis, which is prodromic of hypertension and hypercoagulability. In this panorama, the nutraceutical supplement Taurisolo, a polyphenolic extract from Aglianico cultivar grape, rich in catechin and procyanidins, was evaluated as a vasoprotective, vasorelaxing, anti-hypertensive and anti-coagulant agent in: cell lines, isolated vessels, in vivo models of chronic hypertension and hypercoagulability, and in clinical tests of endothelial reactivity. Taurisolo demonstrated to fully protect vascular cell viability from oxidative stimulus at 100 µg/mL and evoke vasorelaxing effects (Emax = 80.6% ± 1.9 and pEC50 = 1.19 ± 0.03) by activation of the Sirtuins-AMPK-pathway. Moreover, Taurisolo, chronically administered at 20 mg/Kg/die in in vivo experiments, inhibited the onset of cardiac hypertrophy (heart weight/rat weight = 3.96 ± 0.09 vs. 4.30 ± 0.03), hypercoagulability (decrease of fibrinogen vs. control: < 0.01) and hypertension (mean of Psys: 200 ± 2 vs. control 234 ± 2 mmHg) and improved endothelial function (Emax = 88.9% ± 1.5 vs. control 59.6% ± 3.6; flow-mediated dilation in healthy volunteers after 400 mg twice daily for 8 weeks vs. baseline: = 0.019). In conclusion, Taurisolo preserves the vascular function against ox-inflamm-ageing process and the consequent cardiovascular accidents.

摘要

保护血管内皮细胞的完整性和功能是未满足的医学需求。事实上,内皮功能障碍导致一氧化氮生物合成减少,这是高血压和高凝状态的先兆。在这种情况下,营养补充剂 Taurisolo(一种富含儿茶素和原花青素的 Aglianico 葡萄多酚提取物)被评估为一种具有血管保护、血管舒张、抗高血压和抗凝血作用的药物:在细胞系、分离血管、慢性高血压和高凝状态的动物模型中,以及内皮反应的临床测试中。 Taurisolo 证明在 100μg/mL 时能完全保护血管细胞免受氧化刺激,通过激活 Sirtuins-AMPK 通路引起血管舒张作用(Emax=80.6%±1.9,pEC50=1.19±0.03)。此外, Taurisolo 在体内实验中每天 20mg/Kg 给药,可抑制心脏肥大的发生(心脏重量/大鼠体重=3.96±0.09 比 4.30±0.03)、高凝状态(纤维蛋白原减少与对照组相比:<0.01)和高血压(平均 Psys:200±2 比对照组 234±2mmHg),并改善内皮功能(Emax=88.9%±1.5 比对照组 59.6%±3.6;健康志愿者在 8 周内每天两次服用 400mg 后血流介导的舒张与基线相比:=0.019)。总之, Taurisolo 可防止血管功能受到氧化炎症过程的影响,从而预防心血管事件。

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