College of Pharmacy, Yeungnam University, Gyeongsan 712-749, Republic of Korea.
J Ethnopharmacol. 2012 Aug 30;143(1):151-7. doi: 10.1016/j.jep.2012.06.015. Epub 2012 Jun 21.
The flowers of Inula japonica (Inulae Flos) have long been used in traditional medicine for the treatment of bronchitis, digestive disorders, and inflammation. However, the mechanisms underlying its anti-inflammatory effects remain yet to be elucidated. The objectives of this study were 1) to assess the anti-allergic activity of the ethanol extract of flowers of Inula japonica extract (IFE) in vivo, 2) to investigate the mechanism of its action on mast cells in vitro, and 3) to identify its major phytochemical compositions.
The anti-allergic activity of IFE was evaluated using mouse bone marrow-derived mast cells (BMMCs) in vitro and a passive cutaneous anaphylaxis (PCA) animal model in vivo. The effects of IFE on mast cell activation were evaluated in terms of degranulation, eicosanoid generation, Ca(2+) influx, and immunoblotting of various signaling molecules.
IFE inhibited degranulation and the generation of eicosanoids (PGD(2) and LTC(4)) in stem cell factor (SCF)-stimulated BMMCs. Biochemical analysis of the SCF-mediated signaling pathways demonstrated that IFE inhibited the activation of multiple downstream signaling processes including mobilization of intracellular Ca(2+) and phosphorylation of the mitogen-activated protein kinases (MAPKs), PLCγ1, and cPLA(2) pathways. When administered orally, IFE attenuated the mast cell-mediated PCA reaction in IgE-sensitized mice. Its major phytochemical composition included three sesquiterpenes, 1-O-acetylbritannilactone, britanin and tomentosin.
This study suggests that IFE modulates eicosanoids generation and degranulation through the suppression of SCF-mediated signaling pathways that would be beneficial for the prevention of allergic inflammatory diseases. Anti-allergic activity of IFE may be in part attributed particularly to the presence of britanin and tomentosin as major components evidenced by a HPLC analysis.
菊花（Inulae Flos）的花在传统医学中一直被用于治疗支气管炎、消化紊乱和炎症。然而，其抗炎作用的机制仍有待阐明。本研究的目的是 1）评估菊花乙醇提取物（IFE）在体内的抗过敏活性，2）体外研究其对肥大细胞作用的机制，3）鉴定其主要的植物化学成分。
在体外利用鼠骨髓来源的肥大细胞（BMMCs）和被动皮肤过敏反应（PCA）动物模型评估 IFE 的抗过敏活性。通过脱颗粒、花生四烯酸生成、Ca(2+)内流和各种信号分子的免疫印迹分析来评估 IFE 对肥大细胞活化的影响。
IFE 抑制了干细胞因子（SCF）刺激的 BMMCs 中的脱颗粒和花生四烯酸（PGD(2)和 LTC(4))的生成。SCF 介导的信号通路的生化分析表明，IFE 抑制了包括细胞内 Ca(2+)动员和丝裂原激活蛋白激酶（MAPKs）、PLCγ1 和 cPLA(2)途径在内的多个下游信号过程的激活。口服给予 IFE 可减轻 IgE 致敏小鼠的肥大细胞介导的 PCA 反应。其主要的植物化学成分包括三种倍半萜，1-O-乙酰britannilactone、britanin 和 tomentosin。
本研究表明，IFE 通过抑制 SCF 介导的信号通路来调节花生四烯酸生成和脱颗粒，这对预防过敏性炎症性疾病是有益的。IFE 的抗过敏活性可能部分归因于其作为主要成分的 britannin 和 tomentosin 的存在，这一点通过 HPLC 分析得到了证实。
