土茯苓通过血管舒张和心肌抑制作用的降压活性。

Antihypertensive Activity of Sauromatum guttatum Mediated by Vasorelaxation and Myocardial Depressant Effects.

机构信息

COMSATS University Islamabad - Abbottabad Campus - Department of Pharmacy, Abbottabad, Khyber Pakhtunkhwa - Paquistão.

Ibadat International University Islamabad, Islamabad - Paquistão.

出版信息

Arq Bras Cardiol. 2021 Dec;117(6):1093-1103. doi: 10.36660/abc.20200055.

DOI:10.36660/abc.20200055

PMID:35613166

原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC8757165/

Abstract

BACKGROUND

Sauromatum guttatum (S. guttatum) is used in the treatment of blood disorders and reportedly has a spasmolytic activity through Ca2+ channel inhibition.

OBJECTIVES

The aim of this study was to investigate the antihypertensive potential of S. guttatum in high salt-induced hypertensive Sprague-Dawley (SD) rat model (HSHRs).

METHODS

SD rats were divided into normotensive, hypertensive, S. guttatum and verapamil treated groups. S. guttatum crude extract (Sg.Cr) (100, 150 and 300 mg/kg/day) and verapamil (5, 10 and 15 mg/kg/day) were administered orally along with NaCl. Aortic rings and right atrial strips from normotensive rats were used to investigate the underlying mechanisms. The level of statistical significance was set at 5%.

RESULTS

Mean arterial pressure decreased in the Sg.Cr and verapamil-treated hypertensive groups in a dose-dependent manner (p < 0.001). In the vascular reactivity study, acetylcholine induced relaxations with an EC50 value of 0.6 µg/mL (0.3-1.0) in Sg.Cr-treated hypertensive rats (300 mg/kg), suggesting endothelial preservation. In isolated normotensive rat aorta, Sg.Cr-treated rats showed vasorelaxation with an EC50 value of 0.15 mg/mL (0.10-0.20), ablated by endothelial denudation or pretreatment with L-NAME and atropine. Sg.Cr treatment caused relaxation against high K+-induced contractions, like verapamil. Sg.Cr showed negative inotropic (82%) and chronotropic effects (56%) in isolated rat atrial preparations reduced with atropine. The phytochemical investigation indicated presence of alkaloids, flavonoids and tannins.

CONCLUSION

S. guttatum has a vasodilatory effect through endothelial function preservation, muscarinic receptor-mediated NO release and Ca2+ movement inhibition, while atrial myocardial depressant effect can be linked to the muscarinic receptor. These findings provide pharmacological base for using S. guttatum extract as an antihypertensive medication.

摘要

背景

Sauromatum guttatum（S. guttatum）用于治疗血液疾病，据报道通过抑制钙通道具有平滑肌松弛活性。

目的

本研究旨在探讨 Sauromatum guttatum 对高盐诱导的高血压 Sprague-Dawley（SD）大鼠模型（HSHRs）的降压潜力。

方法

将 SD 大鼠分为正常血压组、高血压组、S. guttatum 处理组和维拉帕米处理组。S. guttatum 粗提取物（Sg.Cr）（100、150 和 300 mg/kg/天）和维拉帕米（5、10 和 15 mg/kg/天）经口给药，同时给予 NaCl。使用正常大鼠的主动脉环和右心房条带来研究潜在机制。统计学意义水平设定为 5%。

结果

Sg.Cr 和维拉帕米处理的高血压组的平均动脉压呈剂量依赖性降低（p<0.001）。在血管反应性研究中，乙酰胆碱诱导的舒张作用在 Sg.Cr 处理的高血压大鼠（300 mg/kg）中具有 EC50 值为 0.6 µg/mL（0.3-1.0），表明内皮保存。在分离的正常大鼠主动脉中，Sg.Cr 处理的大鼠表现出血管舒张作用，EC50 值为 0.15 mg/mL（0.10-0.20），内皮剥脱或用 L-NAME 和阿托品预处理后可消除。Sg.Cr 处理可引起对高 K+诱导收缩的舒张作用，类似于维拉帕米。Sg.Cr 在分离的大鼠心房制剂中表现出负性变力（82%）和变时（56%）作用，用阿托品可降低该作用。植物化学研究表明存在生物碱、类黄酮和单宁。