Department of Oriental Pharmacy, College of Pharmacy, Wonkwang University, Wonkwang Oriental Medicines Research Institute, Jeonbuk 570-749, Korea.
Molecules. 2010 Jan 18;15(1):385-98. doi: 10.3390/molecules15010385.
Luteolin (3',4',5,7-tetrahydroxylflavone) is a plant flavonoid and pharmacologically active agent that has been isolated from several plant species. In the present study, the effect of luteolin from the flowers of Lonicera japonica on phorbol 12-myristate 13-acetate (PMA) plus A23187-induced mast cell activation was examined. Luteolin significantly inhibited the induction of inflammatory cytokines such as tumor necrosis factor (TNF)-alpha, interleukin (IL)-8, IL-6 and granulocyte-macrophage colony-stimulating factor (GM-CSF) by PMA plus A23187. Moreover, luteolin attenuated cyclooxygenase (COX)-2 expression and intracellular Ca2+ levels. In activated HMC-1 cells, the phosphorylation of extra-signal response kinase (ERK 1/2) and c-jun N-terminal Kinase (JNK 1/2), but not p38 mitogen-activated protein kinase (p38 MAPK) were decreased by treatment of the cells with luteolin. Luteolin inhibited PMA plus A23187-induced nuclear factor (NF)-kappaB activation, IkappaB degradation, and luciferase activity. Furthermore, luteolin suppressed the expression of TNF-alpha, IL-8, IL-6, GM-CSF, and COX-2 through a decrease in the intracellular Ca2+ levels, and also showed a suppression of the ERK 1/2, JNK 1/2, and NF-kappaB activation. These results indicated that luteolin from the flowers of Lonicera japonica exerted a regulatory effect on mast cell-mediated inflammatory diseases, such as RA, allergy disease and IBD.
木樨草素（3'，4'，5，7-四羟基黄酮）是一种植物类黄酮和具有药理活性的物质，已从几种植物中分离得到。在本研究中，研究了从金银花的花中提取的木樨草素对佛波醇 12-肉豆蔻酸 13-乙酸酯（PMA）加 A23187 诱导的肥大细胞活化的影响。木樨草素显著抑制 PMA 加 A23187 诱导的炎症细胞因子（如肿瘤坏死因子（TNF）-α、白细胞介素（IL）-8、IL-6 和粒细胞-巨噬细胞集落刺激因子（GM-CSF）的产生。此外，木樨草素减弱环氧化酶（COX）-2 的表达和细胞内 Ca2+水平。在活化的 HMC-1 细胞中，木樨草素处理细胞后，细胞外信号调节激酶（ERK 1/2）和 c-jun N 末端激酶（JNK 1/2）的磷酸化，但 p38 丝裂原活化蛋白激酶（p38 MAPK）没有减少。木樨草素抑制 PMA 加 A23187 诱导的核因子（NF）-κB 活化、IκB 降解和荧光素酶活性。此外，木樨草素通过降低细胞内 Ca2+水平抑制 TNF-α、IL-8、IL-6、GM-CSF 和 COX-2 的表达，并且还显示出对 ERK 1/2、JNK 1/2 和 NF-κB 活化的抑制作用。这些结果表明，从金银花的花中提取的木樨草素对 RA、过敏疾病和 IBD 等肥大细胞介导的炎症性疾病具有调节作用。
