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万寿菊地上部分乙醇提取物及其主要生物活性代谢产物的降压和血管舒张作用方式。

Antihypertensive and vasorelaxant mode of action of the ethanol-soluble extract from Tagetes lucida Cav. aerial parts and its main bioactive metabolites.

作者信息

Estrada-Soto Samuel, González-Trujano Ma Eva, Rendón-Vallejo Priscila, Arias-Durán Luis, Ávila-Villarreal Gabriela, Villalobos-Molina Rafael

机构信息

Facultad de Farmacia, Universidad Autónoma del Estado de Morelos, Cuernavaca, Morelos, Mexico.

Laboratorio de Neurofarmacología de Productos Naturales de la Dirección de Investigaciones en Neurociencias del Instituto Nacional de Psiquiatría Ramón de la Fuente Muñiz, Ciudad de México, Mexico.

出版信息

J Ethnopharmacol. 2021 Feb 10;266:113399. doi: 10.1016/j.jep.2020.113399. Epub 2020 Sep 20.

DOI:10.1016/j.jep.2020.113399
PMID:32961278
Abstract

ETHNOPHARMACOLOGICAL RELEVANCE

Tagetes lucida Cav. commonly known as "yauhtli" or "pericón" is used in Mexican traditional medicine for the treatment of anxiety, depressant diseases, pain, hypertension, among others.

AIM

To evaluate the antihypertensive and vasorelaxant modes of action of a crude ethanolic extract from T. lucida aerial parts and to isolate the bioactive compounds.

MATERIALS AND METHODS

Ethanolic extract was tested in an in vivo assay in SHR rats by intragastric administration at 10 and 100 mg/kg dosages, to measure and to compare hemodynamic parameters like diastolic and systolic blood pressure and heart rate. Also, extract (3.03-1000 μg/ml), fractions (3.03-1000 μg/ml) and pure isolated compounds (1.75-550 μM) were evaluated on isolated aortic rings contracted with noradrenaline (0.1 μM) to determine their vasorelaxant effect and extract-mode of action.

RESULTS

Ethanolic extract of T. lucida lowered systolic and diastolic blood pressure on SHR rats without heart rate modification (P > 0.05). Moreover, the extract showed concentration-dependent relaxant effect in a partially endothelium-dependent manner (P < 0.05), through NO/cGMP system activation and calcium channel blockade. 6,7,8-trimethoxycoumarin (1), 6,7-dimethoxycoumarin (2), and 7-methoxycoumarin (3) from T. lucida are the main bioactive compounds of the extract and showed significant vasorelaxant activity.

CONCLUSIONS

Results provide evidence and endorsed the antihypertensive properties attributed to T. lucida in traditional medicine, which is produced by vasorelaxant effect mainly through multitarget NO/cGMP system activation and calcium channel blockade. Coumarin derivatives 1, 2 and 3 are the responsible of the vasorelaxant activity.

摘要

民族药理学相关性

万寿菊(Tagetes lucida Cav.)俗称“yauhtli”或“pericón”,在墨西哥传统医学中用于治疗焦虑、抑郁症、疼痛、高血压等疾病。

目的

评估万寿菊地上部分粗乙醇提取物的降压和血管舒张作用方式,并分离生物活性化合物。

材料与方法

乙醇提取物以10和100mg/kg的剂量通过灌胃给药在SHR大鼠体内进行试验,以测量和比较舒张压、收缩压和心率等血流动力学参数。此外,提取物(3.03 - 1000μg/ml)、馏分(3.03 - 1000μg/ml)和纯分离化合物(1.75 - 550μM)在与去甲肾上腺素(0.1μM)收缩的离体主动脉环上进行评估,以确定其血管舒张作用和提取物的作用方式。

结果

万寿菊乙醇提取物可降低SHR大鼠的收缩压和舒张压,且心率无变化(P > 0.05)。此外,提取物通过激活NO/cGMP系统和阻断钙通道,以部分内皮依赖性方式表现出浓度依赖性舒张作用(P < 0.05)。万寿菊中的6,7,8 - 三甲氧基香豆素(1)、6,7 - 二甲氧基香豆素(2)和7 - 甲氧基香豆素(3)是提取物的主要生物活性化合物,并表现出显著的血管舒张活性。

结论

结果提供了证据,支持了传统医学中归因于万寿菊的降压特性,这主要是由血管舒张作用产生的,主要通过多靶点激活NO/cGMP系统和阻断钙通道实现。香豆素衍生物1、2和3是血管舒张活性的原因。

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