Inhibition by berberine of cyclooxygenase-2 transcriptional activity in human colon cancer cells

Inhibition by berberine of cyclooxygenase-2 transcriptional activity in human colon cancer cells
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DOI:
10.1016/s0378-8741(98)00162-7
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发表时间:
1999-08-01
影响因子:
5.4
通讯作者:
Fujiwara, H
Fujiwara, H
中科院分区:
医学2区
文献类型:
--
作者:
Fukuda, K;Hibiya, Y;Fujiwara, H

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环氧化酶-2(考克斯-2)在结肠癌的癌灶中大量表达,在结肠肿瘤的发生中起关键作用。因此,抑制考克斯-2转录活性的化合物具有潜在的针对结肠肿瘤形成的化学预防性质。使用β-半乳糖苷酶报告基因系统建立了用于评估人结肠癌细胞中考克斯-2转录活性的测定方法,并对各种草药及其成分进行了对考克斯-2转录活性的抑制效果的检查。我们发现,小檗碱,一种存在于小檗属和黄连属植物中的异喹啉生物碱,在浓度高于0.3 μ M时以剂量和时间依赖性方式有效抑制结肠癌细胞中的考克斯-2转录活性。本研究结果可进一步解释小檗碱的抗炎和抗肿瘤作用机制。(C)1999爱思唯尔科学爱尔兰有限公司保留所有权利。
The enzyme cyclooxpgenase-2 (COX-2) is abundantly expressed in colon cancer dens and plays a key role in colon tumorigenesis. Compounds inhibiting COX-2 transcriptional activity have therefore potentially a chemopreventive property against colon tumor formation. An assay method for estimating COX-2 transcriptional activity in human colon cancer cells was established using a beta-galactosidase reporter gene system, and examination was made of various medicinal herbs and their ingredients for an inhibitory effect on COX-2 transcriptional activity. We found that berberine, an isoquinoline alkaloid present in plants of the genera Berberis and Coptis, effectively inhibits COX-2 transcriptional activity in colon cancer cells in a dose- and time-dependent manner at concentrations higher than 0.3 mu M. The present findings may further explain the mechanism of anti-inflammatory and anti-tumor promoting effects of berberine. (C) 1999 Elsevier Science Ireland Ltd. All rights reserved.