Department of Pharmacogonosy, West China College of Pharmacy, Sichuan University, No. 17, Duan 3, Renmin Nan Road, Chengdu 610041, PR China.
J Ethnopharmacol. 2012 Jan 6;139(1):189-93. doi: 10.1016/j.jep.2011.10.036. Epub 2011 Nov 10.
Bulbus Fritillaria Cirrhosae (BFC), known by the Chinese name "Chuan-Bei-Mu", is used as an antitussive, antiasthmatic and expectorant drug for more than 2000 years in China, and Bulbus of Fritillaria wabuensis S. Y. Tang & S. C. Yueh (BFW) was recorded in the 2010 edition of China Pharmacopoeia as one of sources for BFC. The primary objective of this study was to evaluate the antitussive, expectorant and anti-inflammatory effects of alkaloids - imperialine, imperialine-β-N-oxide, isoverticine, and isoverticine-β-N-oxide, which were isolated from BFW, and to provide experimental evidence for its traditional use.
The alkaloids were isolated using phytochemical methods, and their structures were determined by spectroscopic analysis. Their antitussive effects were measured using murine model of ammonia induced cough, the expectorant effects were evaluated by measuring mice's tracheal phenol red output, and the anti-inflammatory effects were assessed by using the murine model of xylene induced ear edema.
The structures of the four alkaloids - imperialine, imperialine-β-N-oxide, isoverticine, and isoverticine-β-N-oxide isolated from BFW were confirmed. The four alkaloids significantly inhibited cough frequency and increased latent period of cough in mice induced by ammonia. Imperialine and isoverticine showed obviously antitussive activities in a dose-dependent manner. Besides, the four alkaloids markedly enhanced mice's tracheal phenol red output in expectorant assessment and significantly inhibited the development of ear edema in anti-inflammatory evaluation assay. Moreover, significant differences were found between the structure-activity relationships of the four alkaloids.
The four alkaloids exhibited significant antitussive, expectorant and anti-inflammatory activities. We suggest that they may be the active ingredients of BFW. The results of the present study provided evidence for BFW to be used as an antitussive and expectorant Traditional Chinese Medicine (TCM).
贝母（Bulbus Fritillaria Cirrhosae，BFC），在中国被称为“川贝母”，已有 2000 多年的止咳、平喘和祛痰的药用历史。2010 年版《中国药典》收录了川贝母的另一个来源——湖北贝母（Bulbus Fritillaria wabuensis S. Y. Tang & S. C. Yueh，BFW）。本研究的主要目的是评估从 BFW 中分离得到的生物碱——浙贝甲素、浙贝甲素-β-N-氧化物、去氢浙贝甲素和去氢浙贝甲素-β-N-氧化物的镇咳、祛痰和抗炎作用，为其传统应用提供实验依据。
采用植物化学方法分离生物碱，通过光谱分析确定其结构。采用小鼠氨水引咳模型测定生物碱的镇咳作用，通过测定小鼠气管酚红排泌量评价其祛痰作用，采用二甲苯致小鼠耳肿胀模型评估其抗炎作用。
从 BFW 中分离得到的 4 种生物碱——浙贝甲素、浙贝甲素-β-N-氧化物、去氢浙贝甲素和去氢浙贝甲素-β-N-氧化物的结构得到了确认。这 4 种生物碱均能显著抑制氨水诱导的小鼠咳嗽次数，增加咳嗽潜伏期。浙贝甲素和去氢浙贝甲素在一定剂量范围内表现出明显的镇咳活性。此外，这 4 种生物碱在祛痰评价中明显增加小鼠气管酚红排泌量，在抗炎评价中显著抑制耳肿胀的发展。而且，这 4 种生物碱的结构-活性关系存在显著差异。
这 4 种生物碱表现出明显的镇咳、祛痰和抗炎活性。提示它们可能是 BFW 的活性成分。本研究结果为 BFW 作为止咳、祛痰的中药提供了依据。
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