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从远志中提取得到的提取物及分离得到的黄酮类芦丁具有血管舒张和降压作用。

Vasorelaxant and hypotensive effects of the extract and the isolated flavonoid rutin obtained from Polygala paniculata L.

机构信息

Department of Pharmacology, Center of Biological Sciences, Federal University of Paraná, Curitiba, Brazil.

出版信息

J Pharm Pharmacol. 2011 Jun;63(6):875-81. doi: 10.1111/j.2042-7158.2010.01240.x. Epub 2011 May 3.

DOI:10.1111/j.2042-7158.2010.01240.x
PMID:21585387
Abstract

OBJECTIVES

This study aimed to investigate the in-vitro and in-vivo cardiovascular effects of the crude hydroalcoholic extract from Polygala paniculata (HEPP) in rats.

METHODS

The procedures were performed on aortic rings and on normotensive anaesthetized rats.

KEY FINDINGS

When tested in endothelium-intact aorta rings, HEPP (30-1000 µg/ml) produced a significant non-concentration-dependent relaxing effect (∼40%), which was completely prevented by incubation with L-NAME (nitric oxide synthase inhibitor), ODQ (soluble guanylate cyclase inhibitor) and partially inhibited by tetraethylammonium (TEA; a non-selective potassium channel blocker) and charybdotoxin (a large- and intermediate-conductance calcium-activated potassium channel blocker). In contrast, atropine (a muscarinic receptor antagonist) or pyrilamine(a histamine H1 receptor antagonist) had no effect. Furthermore, oral administration of HEPP (30-300 mg/kg) in anaesthetized rats caused a dose-dependent and sustained hypotensive action. This effect was unchanged by atropine or TEA, but was strongly reduced in rats continuously infused with L-NAME or methylene blue. Moreover, rutin (1-3 mg/kg) administered by an intravenous route also caused a dose-dependent hypotensive effect in rats.

CONCLUSIONS

Our results demonstrated that the extract obtained from P. paniculata induces potent hypotensive and vasorelaxant effects that are dependent on the nitric oxide/guanylate cyclase pathway. These effects could be related, at least in part, to the rutin contents in this extract.

摘要

目的

本研究旨在探讨远志水醇提取物(HEPP)在大鼠体内外的心血管作用。

方法

在主动脉环和正常血压麻醉大鼠上进行了这些程序。

主要发现

当在具有完整内皮的主动脉环中进行测试时,HEPP(30-1000μg/ml)产生了显著的非浓度依赖性舒张作用(约 40%),这完全被 L-NAME(一氧化氮合酶抑制剂)、ODQ(可溶性鸟苷酸环化酶抑制剂)孵育所阻止,并且部分被四乙铵(TEA;非选择性钾通道阻滞剂)和芋螺毒素(大电导和中电导钙激活钾通道阻滞剂)抑制。相比之下,阿托品(毒蕈碱受体拮抗剂)或苯海拉明(组胺 H1 受体拮抗剂)没有作用。此外,HEPP(30-300mg/kg)口服给予麻醉大鼠引起剂量依赖性和持续的降压作用。这种作用不受阿托品或 TEA 影响,但在连续输注 L-NAME 或亚甲蓝的大鼠中强烈减少。此外,静脉给予芦丁(1-3mg/kg)也在大鼠中引起剂量依赖性的降压作用。

结论

我们的结果表明,从远志中获得的提取物诱导出强大的降压和血管舒张作用,这依赖于一氧化氮/鸟苷酸环化酶途径。这些作用至少部分与该提取物中的芦丁含量有关。

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