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黄芩和儿茶的药用提取物可作为环氧化酶和5-脂氧合酶的双重抑制剂来减轻炎症。

A medicinal extract of Scutellaria baicalensis and Acacia catechu acts as a dual inhibitor of cyclooxygenase and 5-lipoxygenase to reduce inflammation.

作者信息

Burnett B P, Jia Q, Zhao Y, Levy R M

机构信息

Primus Pharmaceuticals, Inc, Scottsdale, AZ 85251, USA.

出版信息

J Med Food. 2007 Sep;10(3):442-51. doi: 10.1089/jmf.2006.255.

Abstract

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 microg/mL, while the mixed extract showed a value for potato 5-LOX enzyme activity of 25 microg/mL. Prostaglandin E2 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.

摘要

一种含有两种天然黄酮类化合物的混合提取物,即黄芩中的黄芩苷和儿茶中的儿茶素,通过酶、细胞和体内模型对其进行环氧合酶(COX)和5-脂氧合酶(5-LOX)抑制作用测试。抑制绵羊COX-1和COX-2过氧化物酶活性的50%抑制浓度为15微克/毫升,而该混合提取物对马铃薯5-LOX酶活性的抑制值为25微克/毫升。在表达COX-2的人骨肉瘤细胞中,混合提取物抑制了前列腺素E2的生成,而在两种人类细胞系,即永生化THP-1单核细胞和HT-29结肠腺癌中,白三烯的生成均受到抑制。在花生四烯酸诱导的小鼠耳肿胀模型中,该提取物以剂量依赖性方式减轻了水肿。当将花生四烯酸直接注射到小鼠踝关节的关节腔内时,在转鼓行走模型中,混合提取物减轻了肿胀并恢复了功能。这些结果表明,这种天然的黄酮类混合物通过对COX和LOX酶的“双重抑制”作用,减少促炎类二十烷酸的产生,并在体内炎症模型中减轻水肿。

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