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Cochlospermum vitifolium 通过激活 NO/cGMP 信号通路主要诱导血管舒张和降压作用。

Cochlospermum vitifolium induces vasorelaxant and antihypertensive effects mainly by activation of NO/cGMP signaling pathway.

机构信息

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

出版信息

J Ethnopharmacol. 2010 Aug 9;130(3):477-84. doi: 10.1016/j.jep.2010.05.037. Epub 2010 May 27.

Abstract

AIM OF THE STUDY

Cochlospermum vitifolium is a medicinal plant used for the treatment of diabetes, hepatobilary and cardiovascular illnesses. The aim of current study was to determine the in vivo antihypertensive and in vitro functional vasorelaxant mechanism of methanol extract of Cochlospermum vitifolium (MECv) and naringenin (NG).

MATERIALS AND METHODS

Test material was assayed on rat isolated aorta rings test with- and without-endothelium to determine their vasorelaxant mechanism. Also, the in vivo antihypertensive effect was evaluated on spontaneously hypertensive rat (SHR) model. In addition, presence of NG into the extract was confirmed by reverse phase high performance liquid chromatography (RP-HPLC) analysis.

RESULTS

MECv (120 mg/kg) and NG (50 and 160 mg/kg) showed acute antihypertensive effects on SHR when systolic and diastolic pressure were decreased at 1 h and 24 h after administration, respectively. Vasorelaxant effect of MECv and NG was shifted to the right when endothelium-intact aortic rings were pre-incubated with L-NAME (10 microM) and ODQ (1 microM). Also, NG relaxant curves were displaced to the right in the presence of tetraethylammonium (TEA, 1 mM) and 2-aminopyridine (2-AP, 100 microM) on endothelium-denuded aortic rings.

CONCLUSION

Experiments described above showed that MECv play an important role in hypertension regulation through NO synthesis and may be PGI(2) production and potassium channel activation on excessive endothelial dysfunction conditions. Unfortunately, presence of NG into the extract is not significant on bioactivity of the extract; however, this compound could be tested and evaluated as structural scaffold for future drug design for development of antihypertensive agents.

摘要

研究目的

Cochlospermum vitifolium 是一种用于治疗糖尿病、肝胆和心血管疾病的药用植物。本研究旨在确定 Cochlospermum vitifolium(MECv)甲醇提取物和柚皮苷(NG)的体内降压和体外功能性血管舒张机制。

材料和方法

在有和无内皮的情况下,用大鼠离体主动脉环试验检测受试物的血管舒张机制。此外,还在自发性高血压大鼠(SHR)模型中评价了体内降压作用。此外,通过反相高效液相色谱(RP-HPLC)分析确认提取物中存在 NG。

结果

MECv(120mg/kg)和 NG(50 和 160mg/kg)在给药后 1 小时和 24 小时分别降低收缩压和舒张压时,对 SHR 表现出急性降压作用。当完整内皮的主动脉环预先用 L-NAME(10μM)和 ODQ(1μM)孵育时,MECv 和 NG 的血管舒张作用曲线向右侧移位。此外,当存在四乙铵(TEA,1mM)和 2-氨基吡啶(2-AP,100μM)时,内皮去神经的主动脉环上的 NG 松弛曲线向右侧移位。

结论

上述实验表明,MECv 通过 NO 合成在高血压调节中发挥重要作用,并且在过度内皮功能障碍的情况下可能通过 PGI(2)产生和钾通道激活来发挥作用。不幸的是,提取物中 NG 的存在对提取物的生物活性没有显著影响;然而,该化合物可以作为结构支架进行测试和评估,用于开发具有降压作用的药物。

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