从假马齿苋（Bacopa monniera (L.) Wettst.）中分离得到的提取物对脂氧合酶和环氧化酶-2的抑制作用
Inhibition of lipoxygenases and cyclooxygenase-2 enzymes by extracts isolated from Bacopa monniera (L.) Wettst.
作者信息
Viji V, Helen A
机构信息
Department of Biochemistry, University of Kerala, Kariavattom, Thiruvananthapuram, Kerala 695 581, India.
出版信息
J Ethnopharmacol. 2008 Jul 23;118(2):305-11. doi: 10.1016/j.jep.2008.04.017. Epub 2008 Apr 24.
AIM OF THE STUDY
Bacopa monniera Linn is described in the Ayurvedic Materia Medica, as a therapeutically useful herb for the treatment of inflammation. In the current study, we investigated the anti-inflammatory activity of methanolic extract of Bacopa monniera (BME). For some experiments EtOAc and bacoside fractions were prepared from BME. The effect of these extracts in modulating key mediators of inflammation was evaluated.
MATERIALS AND METHODS
Carrageenan-induced rat paw edema, rat mononuclear cells and human whole blood assay were employed as in vivo and in vitro models.
RESULTS
In carrageenan-induced rat paw edema, BME brought about 82% edema inhibition at a dose of 100mg/kg i.p. when compared to indomethacin (INDO) (3mg/kg) that showed 70% edema inhibition. BME also significantly inhibited 5-lipoxygenase (5-LOX), 15-LOX and cyclooxygenase-2 (COX-2) activities in rat monocytes in vivo. Among the fractions tested in vitro, EtOAc fraction possessed significant 1,1-diphenyl-2-picrylhydrazyl radical scavenging activity with IC(50) value of 30 microg/ml compared to butylated hydroxyl toluene (IC(50) = 13 microg/ml). This fraction also exerted significant hydroxyl radical scavenging activity with IC(50) value of 25 microg/ml in comparison with quercetin (IC(50) = 5 microg/ml). Inhibitory effects of EtOAc and bacoside fractions on LOX and COX activities in Ca-A23187 stimulated rat mononuclear cells were also assessed. 5-LOX IC(50) values were 25 microg/ml for EtOAc, 68 microg/ml for bacosides and 2 microg/ml for nordihydroguaiaretic acid (NDGA) where as COX-2 IC(50) values were 1.32 microg/ml for EtOAc, 1.19 microg/ml for bacoside fraction and 0.23 microg/ml for indomethacin. EtOAc and bacoside fractions also brought about significant decrease in TNF-alpha release ex vivo.
CONCLUSION
Bacopa monniera possesses anti-inflammatory activity through inhibition of COX and LOX and downregulation of TNF-alpha.
研究目的
在阿育吠陀医学中，假马齿苋被描述为一种对治疗炎症有用的草药。在本研究中，我们调查了假马齿苋甲醇提取物（BME）的抗炎活性。对于一些实验，从BME中制备了乙酸乙酯和总苷部分。评估了这些提取物对炎症关键介质的调节作用。
材料与方法
采用角叉菜胶诱导的大鼠足肿胀、大鼠单核细胞和人全血试验作为体内和体外模型。
结果
在角叉菜胶诱导的大鼠足肿胀实验中，与显示70%肿胀抑制率的吲哚美辛（INDO）（3mg/kg）相比，BME腹腔注射100mg/kg剂量时产生了82%的肿胀抑制率。BME在体内还显著抑制大鼠单核细胞中的5-脂氧合酶（5-LOX）、15-脂氧合酶和环氧化酶-2（COX-2）活性。在体外测试的部分中，乙酸乙酯部分具有显著的1,1-二苯基-2-苦基肼自由基清除活性，IC(50)值为30μg/ml，而丁基化羟基甲苯的IC(50)值为13μg/ml。与槲皮素（IC(50)=5μg/ml）相比，该部分还具有显著的羟基自由基清除活性，IC(50)值为25μg/ml。还评估了乙酸乙酯和总苷部分对钙离子载体A23187刺激的大鼠单核细胞中脂氧合酶和环氧化酶活性的抑制作用。乙酸乙酯的5-LOX IC(50)值为25μg/ml，总苷为68μg/ml，去甲二氢愈创木酸（NDGA）为2μg/ml；而COX-2的IC(50)值，乙酸乙酯为1.32μg/ml，总苷部分为1.19μg/ml，吲哚美辛为0.23μg/ml。乙酸乙酯和总苷部分还使体外肿瘤坏死因子-α（TNF-α）释放显著降低。
结论
假马齿苋通过抑制COX和LOX以及下调TNF-α具有抗炎活性。
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