Department of Pharmacology and Toxicology, Faculty of Pharmacy in Hradec Kralove, Charles University, Hradec Kralove, Czech Republic.
INSERM (French National Institute of Health and Medical Research), UMR 1260, Regenerative Nanomedicine (RNM), FMTS, Université de Strasbourg, Faculté de Pharmacie, Illkirch, France.
Planta Med. 2020 Jul;86(10):708-716. doi: 10.1055/a-1158-9422. Epub 2020 May 14.
The dietary intake of flavonoids seems to be inversely related to cardiovascular mortality. The consumption of isoflavonoids is increasing in the general population, especially due to the use of food supplements and a variety of isoflavonoid-rich foods. However, detailed studies on the vascular influence of individual pure isoflavonoids are mostly missing. For this study, 16 isoflavonoids were initially screened for their vasorelaxant properties on rat aortas. The 2 most potent of them, biochanin A and glycitein, were further tested for the mechanism of action on porcine coronary arteries. They both induced an endothelium independent vascular relaxation, with EC below 6 and 17 µM, respectively. Biochanin A, but not glycitein, was able to block the vasoconstriction caused by KCl, CaCl, serotonin, and U46619 in a dose-dependent manner. Another series of experiments suggested that the major mechanism of action of biochanin A was the inhibition of L-type calcium channels. Moreover, biochanin A in relatively small concentrations (2 - 4 µM) interfered with the cGMP, but not cAMP, pathway in isolated coronary arteries. These results indicate that some isoflavonoids, in particular biochanin A, are able to have vasodilatory effects in micromolar concentrations, which is of potential clinical interest for the management of cardiovascular pathologies.
黄酮类化合物的饮食摄入量似乎与心血管死亡率呈负相关。异黄酮的消费在普通人群中不断增加，特别是由于食品补充剂的使用和各种富含异黄酮的食物。然而，关于个别纯异黄酮对血管的影响的详细研究大多缺失。在这项研究中，最初在大鼠主动脉上筛选了 16 种异黄酮以评估其血管舒张特性。其中最有效的两种，大豆苷元和染料木黄酮，进一步在猪冠状动脉上测试其作用机制。它们都诱导了内皮细胞独立的血管舒张，EC50 分别低于 6 和 17 μM。大豆苷元而不是染料木黄酮能够以剂量依赖的方式阻断由 KCl、CaCl、血清素和 U46619 引起的血管收缩。另一系列实验表明，大豆苷元的主要作用机制是抑制 L 型钙通道。此外，大豆苷元在相对较低的浓度（2-4 μM）下干扰了分离的冠状动脉中的 cGMP，但不干扰 cAMP 通路。这些结果表明，一些异黄酮，特别是大豆苷元，能够在微摩尔浓度下产生血管舒张作用，这对于心血管疾病的治疗具有潜在的临床意义。
