Department of Pharmacology, Faculty of Pharmacy, Mahidol University, Bangkok, Thailand.
Planta Med. 2012 Oct;78(15):1626-32. doi: 10.1055/s-0032-1315198. Epub 2012 Aug 7.
Overactivation of the renin-angiotensin system is one of the most important risk factors for the development of hypertension. The use of the crude extracts and/or active compounds, such as anthocyanins and quercetin, of herbal plants that have antihypertensive effects is beneficial for decreasing of blood pressure level. However, the molecular mechanisms by which anthocyanins (delphinidin and cyanin) and quercetin regulate the renin-angiotensin system are not completely understood. In this study, we demonstrate that delphinidin, cyanin, and quercetin interrupt the renin-angiotensin system signaling pathway by inhibiting the angiotensin-converting enzyme activity and decreasing its mRNA production. Furthermore, treatment with either delphinidin or cyanin significantly inhibited renin mRNA production. However, delphinidin, cyanin, and quercetin did not act as the angiotensin II type 1 receptor antagonist and did not play roles in the regulation of its internalization. The direct inhibition of components of the renin-angiotensin system advances our understanding of the antihypertensive effects of these compounds.
肾素-血管紧张素系统的过度激活是高血压发展的最重要危险因素之一。使用具有降压作用的草药的粗提取物和/或活性化合物，如花色苷和槲皮素，有利于降低血压水平。然而，花色苷（飞燕草素和矢车菊素）和槲皮素调节肾素-血管紧张素系统的分子机制尚不完全清楚。在这项研究中，我们证明飞燕草素、矢车菊素和槲皮素通过抑制血管紧张素转换酶活性和减少其 mRNA 产生来中断肾素-血管紧张素系统信号通路。此外，用飞燕草素或矢车菊素处理可显著抑制肾素 mRNA 的产生。然而，飞燕草素、矢车菊素和槲皮素不作为血管紧张素 II 型 1 受体拮抗剂，也不参与其内化的调节。对肾素-血管紧张素系统成分的直接抑制加深了我们对这些化合物降压作用的理解。
