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

机译:苦参总黄酮类化合物三叶草苷抑制乙酰胆碱引起的气道平滑肌收缩

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摘要

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 new 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 Sophora flavescens (S. flavescens), but not Ganoderma lucidum (G. lucidum) or Glycyrrhiza uralensis (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.
机译:哮喘是世界范围内严重的健康问题,尤其是在工业化国家中。尽管对哮喘的病理生理学有了更好的了解,但在知识上仍然存在相当大的空白,并且需要新型药物。 ASHMI™(抗哮喘草药干预)是灵芝(岩),苦参(苦参)和甘草(甘草)的水提取物。前DC(甘草)。它可防止小鼠过敏性哮喘气道反应过度,并抑制乙酰胆碱(ACh)诱导的过敏性哮喘小鼠气管环中的气道平滑肌(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。发现苦参(S. flavescens)而不是灵芝(G. lucidum)或甘草(G. uralensis)水性提取物抑制哮喘小鼠气管环的ASM收缩。生物测定指导下的二氯甲烷萃取,制备型HPLC分级分离以及LC-MS和NMR光谱分析法对类黄酮馏分/化合物的分离和鉴定表明,三叶草苷是抑制乙酰胆碱介导的ASM收缩或直接放松预收缩的活性成分。 ASM独立于β2-肾上腺素能受体。

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