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抗胆碱能和钙拮抗剂机制解释了民间将伊朗大蒜芥用于治疗胃肠道、气道和血管系统疾病的药理学基础。

Anti-cholinergic and Ca-antagonist mechanisms explain the pharmacological basis for folkloric use of Sisymbrium irio Linn. in gastrointestinal, airways and vascular system ailments.

作者信息

Hussain Musaddique, Waqas Hafiz Muhammad, Raza Shahid Masood, Farooq Umer, Ahmed Muhammad Masood, Majeed Abdul

机构信息

School of Pharmacy, The University of Faisalabad, Faisalabad, Pakistan.

College of Pharmaceutical Sciences, Zhejiang University, Hangzhou, China.

出版信息

J Ethnopharmacol. 2016 Dec 4;193:474-480. doi: 10.1016/j.jep.2016.09.028. Epub 2016 Sep 30.

DOI:10.1016/j.jep.2016.09.028
PMID:27693774
Abstract

ETHNOPHARMACOLOGICAL RELEVANCE

Seeds of Sisymbrium irio Linn has been used traditionally in different regions of Pakistan for the treatment of gastrointestinal, airways and vascular system ailments. To insight the pharmacological basis, in vitro study was conducted in order to validate its folkloric uses.

MATERIAL AND METHODS

70% aqueous-methanolic extract of seeds from S. irio (Si.MEs) was tested on isolated rabbit aorta, jejunum and trachea strip hanged in tissue bath having physiological solutions aerated with carbogen and their responses were measured and recorded via Power Lab.

RESULTS

The Si.MEs exhibited the transient spasmogenic effect (0.01-1.0mg/mL) on spontaneous jejunum contractions, followed by the spasmolytic effect. The addition of atropine resulted in blocking in spasmogenic effect while the spasmolytic effect was originated, suggesting the presence of an antimuscarinic effect. Likewise verapamil, Si.MEs (0.03-5mg/mL) repressed the high concentration K(80mM)-induced contraction and also drifted the Ca concentration-response curves toward right (0.3-3.0mg/mL), possibly signifying the Ca channel blockade. Furthermore, Si.MEs exhibited nonspecific relaxant effect on carbachol (1µM)- and high concentration K(80mM)-induced tracheal contractions in a way comparable to dicyclomine, suggesting the coexistence of Ca-antagonistic and/or antimuscarinic properties. Additionally, Si.MEs also relaxed the phenylephrine(1µM)- and high concentration K(80mM)-induced aortic contraction (0.01-3mg/mL), suggesting blockade of Ca channel. Moreover, oral administration of Si.MEs, as high as 6g per kg, did not produce lethality among the treated groups of mice.

CONCLUSIONS

Aqueous-methanolic extract of seeds from S. irio (Si.MEs) exhibited the bronchodilator and gut modulator (spasmogenic and spasmolytic) activities, probably through dual blockade of muscarinic receptors and Ca channels, whereas, vasodilator effect may be due to Ca channels blockade.

摘要

民族药理学关联

伊朗芥(Sisymbrium irio Linn)种子在巴基斯坦不同地区传统上用于治疗胃肠道、气道和血管系统疾病。为深入了解其药理学基础,进行了体外研究以验证其民间药用价值。

材料与方法

用生理溶液加混合气体充气的组织浴中,对伊朗芥种子的70%甲醇水溶液提取物(Si.MEs)作用于离体兔主动脉、空肠和气管条进行测试,并通过Power Lab测量和记录其反应。

结果

Si.MEs对空肠自发收缩表现出短暂的致痉作用(0.01 - 1.0mg/mL),随后是解痉作用。加入阿托品可阻断致痉作用,而解痉作用依然存在,提示存在抗毒蕈碱作用。同样,维拉帕米一样,Si.MEs(0.03 - 5mg/mL)可抑制高浓度钾(80mM)诱导的收缩,并使钙浓度 - 反应曲线右移(0.3 - 3.0mg/mL),可能表明存在钙通道阻滞。此外,Si.MEs对卡巴胆碱(1µM)和高浓度钾(80mM)诱导的气管收缩表现出非特异性松弛作用,其方式与双环维林相当,提示存在钙拮抗和/或抗毒蕈碱特性。另外,Si.MEs还可松弛去氧肾上腺素(1µM)和高浓度钾(80mM)诱导的主动脉收缩(0.01 - 3mg/mL),提示存在钙通道阻滞。此外,高达每千克6克的Si.MEs口服给药在受试小鼠组中未产生致死性。

结论

伊朗芥种子的甲醇水溶液提取物(Si.MEs)表现出支气管扩张和肠道调节(致痉和解痉)活性,可能是通过对毒蕈碱受体和钙通道的双重阻滞,而血管舒张作用可能归因于钙通道阻滞。

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