Department of Pharmacology, Center of Biological Sciences, Federal University of Paraná, Curitiba, Brazil.
J Pharm Pharmacol. 2011 Jun;63(6):875-81. doi: 10.1111/j.2042-7158.2010.01240.x. Epub 2011 May 3.
This study aimed to investigate the in-vitro and in-vivo cardiovascular effects of the crude hydroalcoholic extract from Polygala paniculata (HEPP) in rats.
The procedures were performed on aortic rings and on normotensive anaesthetized rats.
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.
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.
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。
在主动脉环和正常血压麻醉大鼠上进行了这些程序。
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。
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。