A medicinal extract of Scutellaria baicalensis and Acacia catechu acts as a dual inhibitor of cyclooxygenase and 5-lipoxygenase to reduce inflammation
A medicinal extract of Scutellaria baicalensis and Acacia catechu acts as a dual inhibitor of cyclooxygenase and 5-lipoxygenase to reduce inflammation
复制标题
DOI：
10.1089/jmf.2006.255
复制
发表时间：
2007-09-01
影响因子：
2.4
通讯作者：
Levy, R. M.
中科院分区：
文献类型：
--
作者：
Burnett, B. P.;Jia, Q.;Levy, R. M.
通过酶、细胞和体内模型测试了含有两种天然黄酮类化合物（黄芩中的黄芩苷和金合欢儿茶中的儿茶素）的混合提取物对环氧合酶 (COX) 和 5-脂氧合酶 (5-LOX) 的抑制作用。抑制绵羊COX-1和COX-2过氧化物酶活性的50％抑制浓度为15μg/mL，而混合提取物显示马铃薯5-LOX酶活性的值为25μg/mL。混合提取物在表达 COX-2 的人骨肉瘤细胞中抑制前列腺素 E-2 的产生，同时在两种人细胞系、永生化 THP-1 单核细胞和 HT-29 结直肠腺癌中白三烯的产生受到抑制。在花生四烯酸诱导的小鼠耳肿胀模型中，提取物以剂量依赖性方式减少水肿。当花生四烯酸直接注射到小鼠踝关节的关节腔内时，混合提取物减轻了肿胀并恢复了转鼓步行模型的功能。这些结果表明，这种天然类黄酮混合物通过 COX 和 LOX 酶的“双重抑制”发挥作用，减少体内炎症模型中促炎类二十烷酸的产生并减轻水肿。
A mixed extract containing two naturally occurring flavonoids, baicalin from Scutellaria baicalensis and catechin from Acacia catechu, was tested for cyclooxygenase (COX) and 5-lipoxygenase (5-LOX) inhibition via enzyme, cellular, and in vivo models. The 50% inhibitory concentration for inhibition of both ovine COX-1 and COX-2 peroxidase enzyme activities was 15 mu g/mL, while the mixed extract showed a value for potato 5-LOX enzyme activity of 25 mu g/mL. Prostaglandin E-2 generation was inhibited by the mixed extract in human osteosarcoma cells expressing COX-2, while leukotriene production was inhibited in both human cell lines, immortalized THP-1 monocyte and HT-29 colorectal adenocarcinoma. In an arachidonic acid-induced mouse ear swelling model, the extract decreased edema in a dose-dependent manner. When arachidonic acid was injected directly into the intra-articular space of mouse ankle joints, the mixed extract abated the swelling and restored function in a rotary drum walking model. These results suggest that this natural, flavonoid mixture acts via "dual inhibition" of COX and LOX enzymes to reduce production of pro-inflammatory eicosanoids and attenuate edema in an in vivo model of inflammation.