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金银花提取物对COX-2的三功能抑制作用:直接抑制、转录和转录后下调。

Trifunctional inhibition of COX-2 by extracts of Lonicera japonica: direct inhibition, transcriptional and post-transcriptional down regulation.

作者信息

Xu Yibing, Oliverson Bryant G, Simmons Daniel L

机构信息

Department of Chemistry and Biochemistry, Benson Science Building, Brigham Young University, Provo, UT 84602, USA.

出版信息

J Ethnopharmacol. 2007 May 22;111(3):667-70. doi: 10.1016/j.jep.2007.01.017. Epub 2007 Jan 19.

DOI:10.1016/j.jep.2007.01.017
PMID:17314019
Abstract

The anti-inflammatory properties of aqueous extracts from Lonicera japonica (LJ) flower, an anti-inflammatory treatment in traditional Chinese medicine, were tested by radioimmunoassay of cyclooxygenase isoenzyme-generated prostaglandin E2 (PGE2) synthesis as well as by Western and Northern blot analysis of COX-2 protein and mRNA expression, respectively. Boiled LJ aqueous extracts directly inhibited both COX-1 and COX-2 activity, while non-boiled extracts stimulated COX-1. Boiled LJ extracts also inhibited expression of IL-1beta-induced COX-2 protein expression and suppressed its mRNA induction by IL-1beta in A549 cells. Suppression of COX-2 mRNA induction required a significantly higher dose of aqueous extract than did suppression of protein expression, indicating that compounds in the extract act translationally or post-translationally at lower doses and transcriptionally or post-transcriptionally at higher doses. Direct inhibition of COX isoenzymes as well as down-regulation of COX-2 mRNA and protein may represent the mechanism by which this ancient herbal treatment decreases inflammation.

摘要

金银花(LJ)花水提取物作为一种传统中药抗炎疗法,其抗炎特性通过环氧化酶同工酶生成前列腺素E2(PGE2)合成的放射免疫分析以及分别通过COX - 2蛋白和mRNA表达的蛋白质免疫印迹和Northern印迹分析进行测试。煮沸的LJ水提取物直接抑制COX - 1和COX - 2活性,而非煮沸的提取物刺激COX - 1。煮沸的LJ提取物还抑制A549细胞中IL - 1β诱导的COX - 2蛋白表达,并抑制其IL - 1β诱导的mRNA表达。抑制COX - 2 mRNA诱导所需的水提取物剂量比抑制蛋白表达所需剂量显著更高,表明提取物中的化合物在较低剂量下以翻译或翻译后方式起作用,在较高剂量下以转录或转录后方式起作用。对COX同工酶的直接抑制以及COX - 2 mRNA和蛋白的下调可能代表了这种古老草药疗法减轻炎症的机制。

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