Lee Seung Hoon, Bae Eun-Ah, Park Eun-Kyung, Shin Yong-Wook, Baek Nam-In, Han Eun-Joo, Chung Hae-Gon, Kim Dong-Hyun
College of Pharmacy, Kyung-Hee University, 1, Hoegi, Dongdaemun-ku, Seoul 130-701, South Korea.
Int Immunopharmacol. 2007 Dec 15;7(13):1678-84. doi: 10.1016/j.intimp.2007.08.028. Epub 2007 Sep 25.
To understand the antiallergic effect of Artemisia princeps (AP), which has been found to show inhibitory activity against degranulation and a passive cutaneous anaphylaxis (PCA) reaction, eupatilin and jaceosidin, as the active components, were isolated by degranulation-inhibitory activity-guided fractionation, with their antiallergic activity investigated. These isolated components potently inhibited the release of beta-hexosaminidase from RBL-2H3 cells induced by the IgE-antigen complex, with IC(50) values of 3.4 and 4.5muM, respectively. Eupatilin and jaceosidin potently inhibited the PCA reaction and scratching behaviors induced by IgE- antigen complex and compound 48/80, respectively. Orally administered jaceosidin more potently inhibited the PCA reaction than that of eupatilin, although the PCA reaction-inhibitory activity of intraperitoneally administered jaceosidin was nearly the same as that of eupatilin. Eupatilin and jaceosidin inhibited the gene expressions of TNF-alpha and IL-4 in RBL-2H3 cells stimulated by IgE-antigen complex. Eupatilin and jaceosidin inhibited the activation of NF-kB. Based on these findings, eupatilin and jaceosidin may be useful for protection from the PCA and itching reactions, which are IgE-mediated representative skin allergic diseases.
为了解已被发现对脱颗粒和被动皮肤过敏反应（PCA）具有抑制活性的魁蒿（AP）的抗过敏作用，通过脱颗粒抑制活性导向分离法分离出活性成分灯盏乙素和蒙花苷，并对其抗过敏活性进行了研究。这些分离出的成分能有效抑制IgE-抗原复合物诱导的RBL-2H3细胞中β-己糖胺酶的释放，IC（50）值分别为3.4和4.5μM。灯盏乙素和蒙花苷分别有效抑制了IgE-抗原复合物和化合物48/80诱导的PCA反应和搔抓行为。口服蒙花苷比灯盏乙素更有效地抑制PCA反应，尽管腹腔注射蒙花苷的PCA反应抑制活性与灯盏乙素几乎相同。灯盏乙素和蒙花苷抑制了IgE-抗原复合物刺激的RBL-2H3细胞中TNF-α和IL-4的基因表达。灯盏乙素和蒙花苷抑制了NF-κB的激活。基于这些发现，灯盏乙素和蒙花苷可能有助于预防PCA和瘙痒反应，这两种反应是IgE介导的典型皮肤过敏性疾病。
