1 Department of Physiology, Dongguk University College of Medicine, Gyeongju 38066, Republic of Korea.
2 Channelopathy Research Center (CRC), Dongguk University College of Medicine, Gyeonggi-do 10326, Republic of Korea.
Am J Chin Med. 2018;46(5):1079-1092. doi: 10.1142/S0192415X18500568. Epub 2018 Jul 5.
Flos Magnoliae (FM, Chinese name: Xin-yi) is an oriental medicinal herb commonly used for symptomatic relief from allergic rhinitis, sinusitis, and headache, including in traditional Chinese and Korean medicine formulations. FM inhibits histamine release from mast cells and cytokine secretion from T cells. However, the mechanism of action of FM on the anoctamin-1 (ANO1) ion channel, which is responsible for nasal hypersecretion in allergic rhinitis, has not been elucidated. Therefore, in this study, we investigated the effect of a 30% ethanolic extract of FM (FM) and its chemical constituents on ANO1 activity. We used high-performance liquid chromatography analysis to identify five major chemical constituents of FM: vanillic acid, tiliroside, eudesmin, magnolin, and fargesin. Using a conventional whole-cell patch clamp method, we found that FM (30, 100, and 300[Formula: see text][Formula: see text]g/mL) and its chemical constituent tiliroside inhibited ANO1 activity in ANO1-overexpressing HEK293T cells. In addition, we found that the treatment of the airway epithelial cell line Calu-3 with interleukin 4 significantly increased Ca[Formula: see text] activated Cl[Formula: see text] current (I), but not cystic fibrosis transmembrane conductance regulator (CFTR)-mediated chloride current (I). FM and tiliroside specifically inhibited I. Thus, in this study, we identified a novel mechanism underlying the alleviation of allergic rhinitis by FM. Our results indicate that FM and its chemical constituent tiliroside are promising and potent agents for the prevention and treatment of allergic rhinitis.
辛夷（Flos Magnoliae，FM）是一种东方药用植物，常用于缓解过敏性鼻炎、鼻窦炎和头痛等症状，包括在中药和韩国药配方中。FM 可抑制肥大细胞释放组胺和 T 细胞分泌细胞因子。然而，FM 对负责过敏性鼻炎鼻分泌物过多的 anoctamin-1（ANO1）离子通道的作用机制尚未阐明。因此，在本研究中，我们研究了 FM（FM）及其化学成分对 ANO1 活性的影响。我们使用高效液相色谱分析鉴定了 FM 的五种主要化学成分：香草酸、丁香苷、土木香内酯、木兰脂素和法呢脂素。使用传统的全细胞膜片钳方法，我们发现 FM（30、100 和 300[Formula: see text][Formula: see text]g/mL）及其化学成分丁香苷抑制了 ANO1 过表达 HEK293T 细胞中的 ANO1 活性。此外，我们发现白细胞介素 4 处理气道上皮细胞系 Calu-3 显著增加了 Ca[Formula: see text]激活的 Cl[Formula: see text]电流（I），但不增加囊性纤维化跨膜电导调节因子（CFTR）介导的氯离子电流（I）。FM 和丁香苷特异性抑制 I。因此，在本研究中，我们确定了 FM 缓解过敏性鼻炎的新机制。我们的结果表明，FM 及其化学成分丁香苷是预防和治疗过敏性鼻炎的有前途和有效的药物。
