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异槲皮苷和旱金莲花提取物的降压作用:抑制血管紧张素转换酶的证据。

Antihypertensive effects of isoquercitrin and extracts from Tropaeolum majus L.: evidence for the inhibition of angiotensin converting enzyme.

机构信息

Department of Pharmacology, Universidade Paranaense, Umuarama, PR, Brazil.

出版信息

J Ethnopharmacol. 2011 Mar 24;134(2):363-72. doi: 10.1016/j.jep.2010.12.026. Epub 2010 Dec 24.

Abstract

AIM OF THE STUDY

Previous studies have shown that the extracts obtained from Tropaeolum majus L. exhibit pronounced diuretic properties. In the present study, we assessed whether the hypotensive and/or antihypertensive mechanism of hydroethanolic extract (HETM), semi-purified fraction (TMLR) obtained from T. majus and the flavonoids isoquercitrin (ISQ) and kaempferol (KPF) can be mediated by their interaction with angiotensin converting enzyme (ACE).

METHODS AND METHODS

Firstly, to evaluate changes in mean arterial pressure (MAP), different groups of normotensive and spontaneously hypertensive rats (SHR) were orally and intraduodenally treated with HETM (10-300 mg/kg) and TMLR (12.5-100mg/kg) and intravenously treated with ISQ and KPF being later anesthetized with ketamine (100mg/kg) and xylazine (20mg/kg). The left femoral vein and the right carotid artery were isolated, and polyethylene catheters were inserted for ISQ and KPF (0.5-4 mg/kg) administration and blood pressure recording, respectively. The plasmatic ACE activity was evaluated to indirect fluorimetry, in serum samples after orally treatment with HETM, TMLR, ISQ and KPF.

RESULTS

The oral administration of the HETM and its TMLR significantly reduced, in a dose-dependent manner, the MAP in both normotensive and SHR. In addition, these preparations significantly decreased the MAP for up to 3h after the administration of the extract. Additionally, the intravenous administration of ISQ, but not KPF, decreased MAP in rats. Otherwise, neither the extracts nor ISQ affected the heart rate. The oral administration of the HETM, TMLR or ISQ reduced ACE activity in serum samples at 90 min after administration. Finally, the intravenous administration of ISQ caused a significant reduction in the hypertensive response to angiotensin I, but not angiotensin II in normotensive rats.

CONCLUSION

Our results show that the hypotensive effects caused by the HETM, as well as by its TMLR, may be associated with the high levels of the flavonoid ISQ found in this plant. In addition, ISQ-induced hypotension in rats is an event dependent on the inhibition of angiotensin II generation by ACE.

摘要

目的

先前的研究表明,旱金莲(Tropaeolum majus L.)提取物具有明显的利尿作用。本研究旨在评估旱金莲水-乙醇提取物(HETM)、半纯化部分(TMLR)以及类黄酮异槲皮苷(ISQ)和山柰酚(KPF)的降压和/或抗高血压机制是否与血管紧张素转换酶(ACE)的相互作用有关。

方法

首先,为了评估平均动脉压(MAP)的变化,将正常血压和自发性高血压大鼠(SHR)的不同组分别经口和十二指肠内给予 HETM(10-300mg/kg)和 TMLR(12.5-100mg/kg),并静脉内给予 ISQ 和 KPF,之后用氯胺酮(100mg/kg)和甲苯噻嗪(20mg/kg)麻醉。分离左股静脉和右颈动脉,分别插入聚乙烯导管,用于 ISQ 和 KPF(0.5-4mg/kg)给药和血压记录。在经口给予 HETM、TMLR、ISQ 和 KPF 后,通过间接荧光法评估血清中的血浆 ACE 活性。

结果

HETM 及其 TMLR 的口服给药可剂量依赖性地降低正常血压和 SHR 的 MAP。此外,这些制剂在给药后长达 3 小时内显著降低 MAP。此外,静脉内给予 ISQ 而非 KPF 可降低大鼠的 MAP。另外,提取物和 ISQ 均不影响心率。HETM、TMLR 或 ISQ 的口服给药可降低给药后 90 分钟时血清样本中的 ACE 活性。最后,静脉内给予 ISQ 可显著降低正常大鼠血管紧张素 I 但不降低血管紧张素 II 的高血压反应。

结论

我们的结果表明,HETM 及其 TMLR 的降压作用可能与该植物中高水平的类黄酮 ISQ 有关。此外,ISQ 诱导的大鼠低血压是一种依赖于 ACE 抑制血管紧张素 II 生成的事件。

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