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苏木中高异黄酮类成分对大鼠离体胸主动脉环的舒张作用
引用本文:何文君,方泰惠 张可 屠鹏飞.苏木中高异黄酮类成分对大鼠离体胸主动脉环的舒张作用[J].中国中药杂志,2009,34(6):731-734.
作者姓名:何文君  方泰惠 张可 屠鹏飞
作者单位:1. 南京中医药大学,药学院,江苏,南京,210029;北京大学药学院,天然药物及仿生药物国家重点实验室,北京,100191
2. 南京中医药大学,药学院,江苏,南京,210029
3. 北京大学药学院,天然药物及仿生药物国家重点实验室,北京,100191
摘    要:目的:研究苏木药材主要成分高异黄酮类成分对大鼠离体胸主动脉环的舒张作用.方法:采用大鼠胸主动脉环张力测定法,观察苏木中4个高异黄酮类成分:巴西苏木素(brazlin,1)、(E)-3-(3,4-dihydroxybenzylidene)-7-hydroxychroman-4-one(2)、苏木酮B(sappanone B,3 )、去氧苏木酮B(3-deoxysappaJlone B,4)(50~1 000μmol·L~(-1))对由苯肾上腺素(PE)和氯化钾(KCl)预收缩的大鼠离体胸主动脉环的舒张作用.结果:4个高异黄酮类成分均能舒张由PE和KCl预收缩的内皮完整的血管环;除变异的高异黄酮类成分巴西苏木素(1)外,高异黄酮类成分(2,3,4)也可显著舒张由PE和Kcl预收缩的内皮去除的血管环;而内皮抑制剂(L-NNA)和亚甲蓝(MB)可以抑制变异高异黄酮类成分巴西苏木素的舒血管作用.结论:正常高异黄酮类成分的舒血管作用可能是非内皮依赖性的,而变异的高异黄酮类成分的舒血管作用是内皮依赖性的,并提示可能由一氧化氮-环磷酸鸟苷(NO-cGMP)通路介导.研究结果一定程度上解释了苏木的药理作用.

关 键 词:苏木  高异黄酮类  苏木素  胸主动脉环  血管舒张

Vasorelaxation effects of homoisoflavonoids from Caesalpinia sappan in  rat thoracic aortic rings
HE Wen-Jun-,Fang-Tai-Hui-,Zhang-Ge-,Tu-Feng-Fei-.Vasorelaxation effects of homoisoflavonoids from Caesalpinia sappan in  rat thoracic aortic rings[J].China Journal of Chinese Materia Medica,2009,34(6):731-734.
Authors:HE Wen-Jun-  Fang-Tai-Hui-  Zhang-Ge-  Tu-Feng-Fei-
Institution:1.  Department of Pharmacology, School of Pharmaceutical Sciences, Nanjing University of  Traditional Chinese Medicine, Nanjing 210029, China;
2.  State Key Laboratory of Natural and Biomimetic Drugs, School of Pharmaceutical Sciences, Peking University
 Health Science Center, Beijing 100191, China
Abstract:

Objective: To identify and elucidate the vasorelaxant activity of homoisoflavonoids, the main chemical components from Lignum Sappan (the stems of Caesalpinia sappan), in isolated rat thoracic aortic rings pre contracted with phenylephrine (PE, 1 μmol·L-1) and KCl (60 mmol·L-1).  Method: The tension of rat thoracic aorta rings was used to evaluated the vasorelaxant activities of four homoisoflavonoids, brazlin (1), (E) 3 (3, 4 dihydroxybenzylidene) 7 hydroxychroman 4 one (2), sappanone B (3), 3 deoxysappanone B (4).  Result: Cumulative addition of homoisoflavonoids (2, 3 and 4) (50 1 000 μmol·L-1) exhibited an acute relaxation either in endothelium intact or endothelium denuded rings in a concentration dependent manner. However, this relaxation was significantly inhibited in endothelium denuded condition and in the presence of endothelial nitric oxide synthase (eNOS) inhibitor, Nw nitro L arginine methyl ester (L NNA, 100 μmol·L-1), and a soluble guanylate cylcase (sGC) inhibitor, methylene blue (MB, 10 μmol·L-1) when addition of variation homoisoflavonoids brazlin (1) (50 1 000 μmol·L-1).  Conclusion: These results indicate that normo homoisoflavonoids (2, 3 and 4) from Caesalpinia sappan mediates endothelium independent vasodilator action in rat thoracic aortic rings, while the variation homoisoflavonoids brazlin elicits endothelium dependent relaxation might via nitric oxide (NO) cGMP pathway. This research could explain the pharmacological activities of homoisoflavonoids to a certain degree.

Keywords:

Caesalpinia sappan  homoisoflavonoids  hematoxylin  thoracic aorta rings  vasodilation

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