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苦参黄酮化合物苦参碱抑制乙酰胆碱诱导的气道平滑肌收缩。

The Sophora flavescens flavonoid compound trifolirhizin inhibits acetylcholine induced airway smooth muscle contraction.

机构信息

Department of Pediatrics, Center for Chinese Herbal Therapy for Asthma and Allergy, Jaffe Food Allergy Institute, 4105 Old Main Hill, Logan, UT 84322.

Department of Biological Engineering, Utah State University, 4105 Old Main Hill, Logan, UT 84322.

出版信息

Phytochemistry. 2013 Nov;95:259-267. doi: 10.1016/j.phytochem.2013.07.023. Epub 2013 Aug 27.

Abstract

Asthma is a serious health problem worldwide, particularly in industrialized countries. Despite a better understanding of the pathophysiology of asthma, there are still considerable gaps in knowledge as well as a need for classes of drugs. ASHMI™ (Anti-asthma Herbal Medicine Intervention) is an aqueous extract of Ganoderma lucidum (Fr.) P. Karst (Ling Zhi), Sophora flavescens Aiton (Ku Shen) and Glycyrrhiza uralensis Fisch. ex DC (Gan Cao). It prevents allergic asthma airway hyper-reactivity in mice and inhibits acetylcholine (ACh) induced airway smooth muscle (ASM) contraction in tracheal rings from allergic asthmatic mice. The purpose of this research was to identify individual herb(s) and their active compound(s) that inhibit ASM contraction. It was found that S. flavescens, but not G. lucidum or G. uralensis aqueous extracts, inhibited ASM contraction in tracheal rings from asthmatic mice. Bioassay-guided isolation and identification of flavonoid fractions/compound(s) via methylene chloride extraction, preparative HPLC fractionation, and LC-MS and NMR spectroscopic analyses showed that trifolirhizin is an active constituent that inhibits acetylcholine mediated ASM contraction or directly relaxes pre-contracted ASM independent of β2-adrenoceptors.

摘要

哮喘是一个全球性的严重健康问题,特别是在工业化国家。尽管对哮喘的病理生理学有了更好的理解,但在知识方面仍存在相当大的差距,并且需要新的药物类别。ASHMI™(抗哮喘草药干预)是灵芝(Fr.)P. Karst(灵芝),苦参(Ku Shen)和甘草(甘草)的水提取物。它可预防小鼠过敏性哮喘气道高反应性,并抑制过敏性哮喘小鼠气管环中乙酰胆碱(ACh)诱导的气道平滑肌(ASM)收缩。这项研究的目的是确定抑制 ASM 收缩的单个草药及其活性化合物。结果发现,苦参水提取物可抑制哮喘小鼠气管环中的 ASM 收缩,但灵芝或甘草水提取物无此作用。通过亚甲基氯萃取、制备高效液相色谱分离、LC-MS 和 NMR 光谱分析进行的基于生物测定的分离和鉴定黄酮类化合物/化合物表明,三叶豆紫檀苷是一种抑制乙酰胆碱介导的 ASM 收缩或直接松弛预先收缩的 ASM 的活性成分,与β2-肾上腺素能受体无关。

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