Facultad de Farmacia, Universidad Autónoma del Estado de Morelos, Cuernavaca, Morelos, 62209, Mexico.
Facultad de Farmacia, Universidad Autónoma del Estado de Morelos, Cuernavaca, Morelos, 62209, Mexico.
J Ethnopharmacol. 2020 May 10;253:112643. doi: 10.1016/j.jep.2020.112643. Epub 2020 Feb 5.
Achillea millefolium L. (Asteraceae) is used for the treatment of respiratory diseases, diabetes, and hypertension.
to explore its tracheal relaxant properties and clarify its functional mechanism of action on smooth muscle cells, which allow us to propose it as a potential anti-asthmatic drug.
organic and hydro-alcoholic extracts from A. millefolium were obtained by macerations, then their relaxing effect on ex vivo isolated rat trachea rings was determined. Most active extract (hexanic extract, EHAm) was studied to determine its functional mechanism of action using synergic, antagonist and inhibitor agents related with the contraction/relaxation process of the smooth muscle. Also, EHAm was subjected to bio-guided fractionation by open-column chromatography (on silica gel) using cyclohexane-EtOAc (80:20) in an isocratic way to isolate main bioactive compounds.
organic and hydro-alcoholic extracts showed relaxant effect in a concentration-response dependent manner, being EHAm the most active. The functional mechanism of action indicates that EHAm induced a non-competitive antagonism to the muscarinic receptors ; in addition, the NO/cGMP pathway is involved in the relaxation process of the tracheal smooth muscle. However, the most important mechanism of action showed by EHAm was related with the calcium channel blockade influx into the smooth muscle cells. On the other hand, epimeric sesquiterpene lactones leucodin (1) and achillin (2) were isolated and purified, which are responsible for the observed smooth muscle relaxant activity of the extract.
hexanic extract of A. millefollium induced a significant relaxant effect on tracheal rat rings by calcium channel blockade and NO release.
蓍草（菊科）用于治疗呼吸道疾病、糖尿病和高血压。
探讨其气管松弛特性，并阐明其对平滑肌细胞的作用机制，从而将其作为一种潜在的抗哮喘药物。
通过浸渍法从蓍草中获得有机和水醇提取物，然后测定其对离体大鼠气管环的舒张作用。最活跃的提取物（己烷提取物，EHAm）用于研究其功能机制，使用与平滑肌收缩/松弛过程相关的协同、拮抗剂和抑制剂来确定其功能机制。此外，EHAm 通过使用硅胶的开管色谱（环己烷-EtOAc，80:20）进行生物导向分段，以等度方式分离主要的生物活性化合物。
有机和水醇提取物以浓度依赖性方式显示舒张作用，EHAm 最为活跃。作用机制表明，EHAm 对毒蕈碱受体产生非竞争性拮抗作用；此外，NO/cGMP 途径参与了气管平滑肌的松弛过程。然而，EHAm 表现出的最重要的作用机制与钙通道内流阻断进入平滑肌细胞有关。另一方面，分离并纯化了差向立体的倍半萜内酯白屈菜素（1）和阿基林（2），它们负责提取物观察到的平滑肌松弛活性。
蓍草的己烷提取物通过钙通道阻断和 NO 释放对大鼠气管环产生显著的舒张作用。
