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黄花蒿提取物及分离的倍半萜内酯对介导豚鼠回肠和气管收缩的受体的作用。

Actions of Artemisia vulgaris extracts and isolated sesquiterpene lactones against receptors mediating contraction of guinea pig ileum and trachea.

机构信息

Welsh School of Pharmacy, Cardiff University, King Edward VII Avenue, Cardiff CF10 3NB, UK.

出版信息

J Ethnopharmacol. 2011 Sep 1;137(1):808-16. doi: 10.1016/j.jep.2011.06.042. Epub 2011 Jul 5.

Abstract

AIM OF THE STUDY

The present study evaluates the Philippine medicinal plant Artemisia vulgaris for antagonistic activity at selected biogenic amine receptors on smooth muscle of the airways and gastrointestinal tract in order to explain its traditional use in asthma and hyperactive gut.

MATERIALS AND METHODS

The antagonistic activity of chloroform crude extract (AV-CHCl(3)) and methanol crude extract (AV-MeOH) of Artemisia vulgaris was studied against concentration-response curves for contractions of the guinea pig ileum and trachea to 5-hydroxytrptamine (5-HT(2) receptors), methacholine (M(3) muscarinic receptors), histamine (H(1) receptors) and β-phenylethylamine (trace amine-associated receptors, TAAR1).

RESULTS AND DISCUSSION

The Artemisia vulgaris chloroform (AV-CHCl(3)) and methanol (AV-MeOH) extract showed histamine H1 antagonism in the ileum and trachea. Further analysis of AV-CHCl(3) isolated two major components, yomogin and 1,2,3,4-diepoxy-11(13)-eudesmen-12,8-olide. Yomogin, a sesquiterpene lactone, exhibited a novel histamine H1 receptor antagonism in the ileum.

CONCLUSION

The presence of a specific, competitive histamine receptor antagonist and smooth muscle relaxant activity in Artemisia vulgaris extracts on the smooth muscle in ileum and trachea explains its traditional use in the treatment of asthma and hyperactive gut.

摘要

目的

本研究评估了菲律宾药用植物青蒿在气道和平滑肌和胃肠道中选定的生物胺受体上的拮抗活性,以解释其在哮喘和高反应性肠道中的传统用途。

材料和方法

研究了青蒿氯仿粗提物(AV-CHCl3)和甲醇粗提物(AV-MeOH)对豚鼠回肠和气管对 5-羟色胺(5-HT2 受体)、乙酰甲胆碱(M3 毒蕈碱受体)、组胺(H1 受体)和β-苯乙胺(痕量胺相关受体,TAAR1)收缩的浓度反应曲线的拮抗活性。

结果与讨论

青蒿氯仿(AV-CHCl3)和甲醇(AV-MeOH)提取物在回肠和气管中显示出组胺 H1 拮抗作用。对 AV-CHCl3 进行进一步分析,分离出两种主要成分,即莪术醇和 1,2,3,4-环氧-11(13)-桉叶烷-12,8-内酯。莪术醇,一种倍半萜内酯,在回肠中表现出新型组胺 H1 受体拮抗作用。

结论

青蒿提取物中存在特异性、竞争性组胺受体拮抗剂和平滑肌松弛活性,这解释了其在治疗哮喘和高反应性肠道方面的传统用途。

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