Anti-inflammatory Activity of Pectolinarigenin and Pectolinarin Isolated from Cirsium chanroenicum
Anti-inflammatory Activity of Pectolinarigenin and Pectolinarin Isolated from Cirsium chanroenicum
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DOI：
10.1248/bpb.31.2063
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发表时间：
2008-11-01
影响因子：
2
通讯作者：
Kim, Hyun Pyo
中科院分区：
文献类型：
--
作者：
Lim, Hyun;Son, Kun Ho;Kim, Hyun Pyo
为了鉴定大蓟中的抗炎活性成分，制备了菊科植物的甲醇提取物和几种溶剂级分;甲醇提取物和乙酸乙酯部分抑制脂多糖处理的RAW 264.7细胞和A23187细胞中环氧合酶-2（考克斯-2）介导的前列腺素E-2（PGE（2））和5-脂氧合酶（5-LOX）介导的白三烯（LT）产生。处理的大鼠嗜碱性白血病（RBL-1）细胞。使用柱色谱法对乙酸乙酯级分进行进一步的生物活性导向分级，导致分离出柳珊瑚苷元（5，7-二羟基-4 '，6-二甲氧基黄酮）以及柳珊瑚苷[柳珊瑚苷元7-鼠李糖基-（1 ->）6）-葡萄糖苷]，沿着。当浓度>1 μ M时，海鞘皂苷元强烈抑制考克斯-2介导的PGE（2）和5-LOX介导的LT产生，表明它是考克斯-2/5-LOX的双重抑制剂。然而，柳松苷元并不影响考克斯-2的表达或核转录因子（NF-κ B）的激活。此外，体内研究表明，这两种化合物以20 - 100 mg/kg经口给药对几种炎症/变态反应动物模型产生相似的抑制活性：花生四烯酸诱导的小鼠耳水肿、角叉菜胶诱导的小鼠爪水肿和被动皮肤过敏反应。所有这些结果都表明，pectolinarigenin和pectolinarin具有抗炎活性，它们可以抑制炎症病变中类花生酸的形成。这些活性肯定有助于C. chanroenicum。
In order to identify the active anti-inflammatory ingredient(s) in Cirsium chanroenicum (Compositae), its methanol extract and several solvent fractions were prepared; the methanol extract and the ethylacetate fraction inhibited cyclooxygenase-2 (COX-2)-mediated prostaglandin E-2 (PGE(2)) and 5-lipoxygenase (5-LOX)-mediated leukotriene (LT) production in lipopolysaccharide-treated RAW 264.7 cells and A23187-treated rat basophilic leukemia (RBL-1) cells, respectively. Further bioactivity-guided fractionation of the ethylacetate fraction using column chromatography led to the isolation of pectolinarigenin (5,7-dihydroxy-4',6-dimethoxyflavone), along with pectolinarin [pectolinarigenin 7-rhamnosyl-(1 ->)6)-glucoside]. Pectolinarigenin strongly inhibited COX-2-mediated PGE(2) and 5-LOX-mediated LT production at >1 mu M, indicating that it is a dual inhibitor of COX-2/5-LOX. However, pectolinarigenin did not affect COX-2 expression or nuclear transcription factor (NF-kappa B) activation. In addition, in vivo studies demonstrated that oral administration of these two compounds at 20100 mg/kg resulted in similar inhibitory activities against several animal models of inflammation/allergy: arachidonic acid-induced mouse ear edema, carrageenan-induced mouse paw edema and passive cutaneous anaphylaxis. All of these results suggest that pectolinarigenin and pectolinarin possess anti-inflammatory activity and that they may inhibit eicosanoid formation in inflammatory lesions. These activities certainly contribute to the anti-inflammatory mechanism of C. chanroenicum.