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丹参(唇形科)的降压活性:ACE 抑制作用和血管紧张素 II 拮抗作用。

Antihypertensive activity of Salvia elegans Vahl. (Lamiaceae): ACE inhibition and angiotensin II antagonism.

机构信息

Centro de Investigación Biomédica del Sur, Instituto Mexicano del Seguro Social (IMSS), Xochitepec, Morelos, Mexico.

出版信息

J Ethnopharmacol. 2010 Jul 20;130(2):340-6. doi: 10.1016/j.jep.2010.05.013. Epub 2010 May 19.

Abstract

ETHNOPHARMACOLOGICAL RELEVANCE

Salvia elegans Vahl. (Lamiaceae), recognized with the popular name of "mirto" is widely used in Mexico for healing purposes, and also them as antihypertensive treatment.

AIM OF THE STUDY

The high prevalence of this illness and the side effects of antihypertensive drugs conducted us to the evaluation of the Salvia elegans extract on angiotensin II action.

MATERIALS AND METHODS

The acute response of blood pressure to angiotensin II administration was measured in mice. We also tested in vitro the inhibitory effect on angiotensin convertase enzyme. Additionally, characterization of the pharmacological effect of the extract fraction was obtained.

RESULTS

We obtained dose-response curve for the administration of complete extract and extract fractions. Due to the hydroalcoholic extract (SeHA) treatment blood pressure decreased significantly from systolic dose of 0.75 mg kg(-1) (p<0.05) and even had an antihypertensive effect that was greater than that treatment with losartan. SeHA extract decreased the E(max) of the AG II hypertensive effect by about 20% in both systolic and diastolic pressures, treatment with losartan also decreased the same parameter between 6% and 8% for systolic and diastolic pressures, respectively. Fractions SeF8 and SeF8-8 showed similar levels of AG II ED(50) for both pressures compared with losartan, these fractions showed major compounds with maximum absorbance peaks at 221, 289 and 330 nm typical of flavonoids. In the inhibition assay the activity of angiotensin converting enzyme (ACE), the extract SeHA showed percentage inhibition (%IACE) of 50.27+/-5.09% (n=5). SeBuOH fraction is found to have greater inhibitory capacity of achieving a IACE 78.40+/-2.24% (n=5), which was similar to the values obtained in the presence of the SeF8-22 fraction (82.61+/-1.74%) and lisinopril (87.18+/-1.16%). The changes in the value of K(M) suggest that components of the extracts and fractions were recognized by the enzyme's active site. The main compounds of the fractions SeBuOH, SeF8-22 were by flavonoid and phenyl propanoid types, according to UV absorption spectra of the fractions.

CONCLUSIONS

The experimental results demonstrated the antihypertensive effect of Salvia elegans and it was due to the AG II antagonism and inhibition of angiotensin converting enzyme.

摘要

民族药理学相关性

鼠尾草(唇形科),俗称“迷迭香”,在墨西哥被广泛用于治疗,也被用作抗高血压药物。

目的

这种疾病的高发病率和抗高血压药物的副作用促使我们评估鼠尾草提取物对血管紧张素 II 作用的影响。

材料和方法

在小鼠中测量了血管紧张素 II 给药后的急性血压反应。我们还在体外测试了对血管紧张素转化酶的抑制作用。此外,还获得了提取物部分的药理作用特征。

结果

我们获得了全提取物和提取物部分给药的剂量反应曲线。由于水醇提取物(SeHA)的治疗,收缩压从 0.75mgkg(-1)的剂量开始显著降低(p<0.05),甚至具有比氯沙坦更强的降压作用。SeHA 提取物使 AG II 高血压效应的 E(max)降低约 20%,无论是收缩压还是舒张压,氯沙坦的治疗分别降低了 6%至 8%。SeF8 和 SeF8-8 两种压力下的 AG II ED(50)相似,与氯沙坦相比,这些部分显示出最大吸收峰在 221、289 和 330nm 的主要化合物,典型的类黄酮。在血管紧张素转化酶(ACE)抑制试验中,提取物 SeHA 显示出 50.27+/-5.09%(n=5)的 ACE 抑制百分比(%IACE)。SeBuOH 部分发现具有更大的抑制能力,达到 78.40+/-2.24%(n=5)的 IACE,这与在 SeF8-22 部分存在时获得的值相似(82.61+/-1.74%)和赖诺普利(87.18+/-1.16%)。K(M)值的变化表明提取物和部分的成分被酶的活性位点识别。根据部分的紫外吸收光谱,SeBuOH 和 SeF8-22 部分的主要化合物为黄酮类和苯丙素类。

结论

实验结果表明,鼠尾草具有抗高血压作用,这是由于其对血管紧张素 II 的拮抗作用和对血管紧张素转化酶的抑制作用。

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