Anti-oxidant and inflammatory mediator's growth inhibitory effects of compounds isolated from Phyllanthus urinaria
Anti-oxidant and inflammatory mediator's growth inhibitory effects of compounds isolated from Phyllanthus urinaria
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DOI：
10.1016/j.jep.2007.11.040
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发表时间：
2008-03-05
影响因子：
5.4
通讯作者：
Tzeng, Yew-Min
中科院分区：
文献类型：
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作者：
Fang, Shih-Hua;Rao, Yerra Koteswara;Tzeng, Yew-Min
叶下珠（Phyllanthus urinaria Linnea）（大戟科）是台湾传统的抗肝炎草药。为了继续寻找有效的天然抗炎剂，从这种植物的乙醇提取物中分离出9种化合物，包括叶下珠素（1）、叶下珠四氢化萘（2）、3，4-脱氢诃子酸三甲酯（3）、没食子酸甲酯（4）和鼠李柠檬苷（5）、短叶苏木素羧酸甲酯（6）、β-谷甾醇-3-O-β-D-吡喃葡萄糖苷（7）、槲皮苷（8）和芦丁（9）。化合物3和6的结构经核磁共振和质谱确证。研究了分离物1-9的体外抗氧化和抗炎活性。在抗氧化试验中，分离物3，4和6表现出显着的DPPH自由基清除活性的IC 50值分别为9.4，9.8和8.9 μ M。另一方面，在LPS/干扰素（IFN）-γ-激活的腹腔巨噬细胞的炎症介质生长抑制试验中，除7株外，所有菌株均显著且剂量依赖性地抑制NO自由基的产生，并且这种调节与肿瘤坏死因子（TNF）-α和白细胞介素（IL）-6的抑制密切相关。此外，30 μ M的分离物3和6以及50 μ M的分离物4显著地将有丝分裂原刺激的脾细胞阻滞在G 0/G1期。这是第一次报道叶下珠分离物对炎症介质的生长抑制活性，除了脾细胞周期阻滞在G 0/G1期。因此，叶下珠的这些分离物可用于治疗细胞介导的免疫性疾病。(C)2007爱思唯尔爱尔兰有限公司保留所有权利。
Phyllanthus urinaria Linnea (Euphorbiaceae), is a traditional anti-hepatitis herb used in Taiwan. In continuation of our search for potent natural anti-inflammatory agents, from the ethanolic extract of this plant, nine compounds including phyllanthin (1), phyltetralin (2), trimethyl-3,4-dehydrochebulate (3), methylgallate (4), and rhamnocitrin (5), methyl brevifolincarboxylate (6), beta-sitosterol-3-O-beta-D-glucopyranoside (7), quercitrin (8), and rutin (9) were isolated. The structures of compounds 3 and 6 were established based on NMR and mass spectral studies. The isolates 1-9 were investigated for their antioxidant, and anti-inflammatory activities in vitro. In the antioxidant assay, the isolates 3, 4 and 6 exhibited significant DPPH radical scavenging activity with an IC50 value of 9.4, 9.8 and 8.9 mu M, respectively. On the other hand, in the inflammatory mediators growth inhibitory assay from LPS/interferon (IFN)-gamma-activated peritoneal macrophages, all the isolates except 7, significantly and dose-dependently inhibited the enhanced production of NO radicals, and such modulation was closely associated with the inhibition of tumor necrosis factor (TNF)-alpha and interleukin (IL)-6. In addition, 30 mu M of isolates 3 and 6, and 50 mu M of 4, significantly arrest the mitogen-stimulated spleen cells in G0/G1 stage. This is the first report on Phyllanthus urinaria isolates for their growth inhibitory activities against inflammatory mediators, in addition to spleen cell cycle arrest in G0/G1 stage. Therefore, these isolates from Phyllanthus urinaria may be useful for the treatment of cell-mediated immune diseases. (C) 2007 Elsevier Ireland Ltd. All rights reserved.