School of Biomedical Sciences, Faculty of Medicine, The Chinese University of Hong Kong, Hong Kong Special Administrative Region; Li Dak Sum Yip Yio Chin R & D Centre for Chinese Medicine, The Chinese University of Hong Kong, Hong Kong Special Administrative Region; Laboratory of Molecular Pharmacology, Department of Pharmacology, School of Pharmacy, Southwest Medical University, Luzhou, Sichuan, PR China.
Department of Food and Health Sciences, Faculty of Science and Technology, Technological and Higher Education Institute of Hong Kong, Hong Kong Special Administrative Region.
J Ethnopharmacol. 2018 Jan 10;210:39-46. doi: 10.1016/j.jep.2017.08.027. Epub 2017 Aug 31.
Fritillariae Bulbus (Beimu in Chinese) is derived from the bulbus of many Fritillaria species (family Liliaceae), which has been used as an antitussive herb in traditional Chinese medicine for more than 2000 years. Due to the complexity of plant origins and significant variations in chemical profiles, the characterization of the profile of the major bioactive constituents and its association with pharmacological activity are important for the quality control of Beimu herbs from different origins.
This study aims to investigate the distribution of major bioactive isosteroidal alkaloids in Beimu herbs of different origins and its correlation with the tracheobronchial relaxant activity.
Quantification of 7 main bioactive 5α-cevanine isosteroidal alkaloids, including ebeiedine, ebeiedinone, hupehenine, isoverticine, verticine, verticinone and imperialine, in 23 Fritillaria species was performed using gas chromatography. The relaxant effect of different extracts of 4 commonly used Beimu herbs, namely Zhe-Beimu (F. thunbergii Miq.), Chuan-Beimu (F. cirrhosa D. Don), Hubei-Beimu (F. hupehensis Hsiao et K. C. Hsia) and Yi-Beimu (F. pallidiflora Schrenk), was evaluated using rat isolated tracheal and bronchial preparations pre-contracted with carbachol, the well established in vitro antitussive model.
Amongst 23 Fritillaria species detected, significant variations of the types and quantities of 7 major isosteroidal alkaloids were determined, which served as an important indicator for the classification of different Beimu herbs with distinct geographic distributions. Based on the type and quantity of these alkaloids, different origins of Beimu could be clearly clustered into several subgroups by principal component analysis. Furthermore, both crude alkaloid and water extracts of all 4 Beimu herbs showed a dose-dependent tracheobronchial relaxation with different potencies. The total content of alkaloids (weight adjusted based on the activity of individual alkaloids) in Beimu extracts significantly correlated with their tracheobronchial relaxation effects (r > 0.9, p < 0.001).
The results demonstrated that the differences in chemical profile of major bioactive isosteroidal alkaloids and pharmacological activity of Beimu could be incorporated into a simple and unified method for quality control and potential prediction of activity of Beimu herbs from different origins.
贝母（Beimu）来源于百合科多种贝母属植物的鳞茎，在中国传统医学中已被用作止咳草药超过 2000 年。由于植物起源的复杂性和化学成分的显著差异，主要生物活性成分的特征图谱及其与药理活性的关联对于不同来源的贝母药材的质量控制非常重要。
本研究旨在研究不同来源贝母药材中主要生物活性甾体生物碱的分布及其与气管支气管舒张活性的相关性。
采用气相色谱法对 23 种贝母属植物中的 7 种主要生物活性 5α-头孢烷生物碱，包括伊贝定、伊贝定酮、胡贝因、异伏康定、伏康定、伏康定酮和罂粟碱，进行定量分析。采用乙酰胆碱预收缩的大鼠离体气管和支气管标本，评价 4 种常用贝母药材（浙贝母、川贝母、湖北贝母和伊贝母）不同提取物的舒张作用，这是一种已建立的体外镇咳模型。
在所检测的 23 种贝母属植物中，确定了 7 种主要甾体生物碱的类型和数量的显著差异，这是区分具有不同地理分布的不同贝母属植物的重要指标。基于这些生物碱的类型和数量，通过主成分分析可以清楚地将不同来源的贝母聚类成几个亚组。此外，4 种贝母的粗生物碱和水提物均表现出剂量依赖性的气管支气管舒张作用，且具有不同的效力。贝母提取物中生物碱的总含量（根据单个生物碱的活性进行重量调整）与气管支气管舒张作用显著相关（r > 0.9，p < 0.001）。
结果表明，主要生物活性甾体生物碱的化学成分差异和不同来源的贝母的药理活性可以纳入一种简单统一的方法，用于控制不同来源的贝母药材的质量和潜在活性预测。
