Antitussive, expectorant, and anti-inflammatory activities of four caffeoylquinic acids isolated from Tussilago farfara
Antitussive, expectorant, and anti-inflammatory activities of four caffeoylquinic acids isolated from Tussilago farfara
复制标题
DOI：
10.3109/13880209.2015.1075048
复制
发表时间：
2016-07-01
影响因子：
3.8
通讯作者：
Xu, Xiang-hong
中科院分区：
文献类型：
--
作者：
Wu, Qi-zhen;Zhao, Dong-xia;Xu, Xiang-hong
背景：金雀花(Tussilago farfara L.(Compositae))是治疗咳嗽、痰、支气管炎和哮喘的中草药之一。目的：从金雀花的乙酸乙酯提取物(ETE)中分离得到4种咖啡酰奎宁酸，并对其镇咳、祛痰、抗炎活性进行评价。材料和方法：通过波谱分析确定化合物1-4的结构。分别以10 mg/kg和20 mg/kg的剂量给小鼠灌胃给药(按5：28：41：26的比例)，连续3d，分别用氨水诱导模型和酚红分泌模型评价止咳、祛痰作用。结果：4个化合物分别鉴定为绿原酸(1)、3，5-二咖啡酰奎宁酸(2)、3，4-二咖啡酰奎宁酸(3)和4，5-二咖啡酰奎宁酸(4)。所有化合物均有明显的镇咳作用，尤其是化合物4(对咳嗽的抑制率为58.0%)。而该合剂对咳嗽的抑制作用最强，为61.7%。所有化合物均有明显的祛痰作用，其中化合物2对酚红分泌的促进作用最强，达35.7%。讨论与结论：咖啡酰奎宁酸及其混合物具有明显的镇咳、祛痰、抗炎作用，可作为FTF的主要有效成分，且可能是一种集体协同作用。
Context: The flower bud of Tussilago farfara L. (Compositae) (FTF) is one of the traditional Chinese medicinal herbs used to treat cough, phlegm, bronchitic, and asthmatic conditions.Objective: The objective of this study is to isolate four caffeoylquinic acids from the ethyl acetate extract (EtE) of FTF and to evaluate their antitussive, expectorant, and anti-inflammatory activities.Materials and methods: The structures of compounds 1-4 isolated from EtE were determined by spectral analysis. Mice were orally treated with these compounds and their mixture (in a ratio of 5:28:41:26 as in EtE) at doses of 10 and 20mg/kg once daily for 3 d. The antitussive and expectorant activities were evaluated separately with the ammonia liquor-induced model and the phenol red secretion model. The anti-inflammation activity was evaluated using leukocyte count in the bronchoalveolar lavage fluid after ammonia liquor-induced acute airway inflammation.Results: The four compounds were identified as chlorogenic acid (1), 3,5-dicaffeoylquinic acid (2), 3,4-dicaffeoylquinic acid (3), and 4,5-dicaffeoylquinic acid (4). All compounds, especially compound 4 (58.0% inhibition in cough frequency), showed a significant antitussive effect. However, the mixture was the most effective to inhibit the cough frequency by 61.7%. All compounds also showed a significant expectorant effect, while compound 2 was the most potent to enhance the phenol red secretion by 35.7%. All compounds significantly alleviated inflammation, but compound 4 showed the strongest effect to inhibit the leukocytosis by 49.7%.Discussion and conclusion: The caffeoylquinic acids and their mixture, exhibiting significant antitussive, expectorant, and anti-inflammatory effects, could be considered as the main effective ingredients of FTF, and they may act in a collective and synergistic way.