Butein downregulates phorbol 12-myristate 13-acetate-induced COX-2 transcriptional activity in cancerous and non-cancerous breast cells
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香港中文大學研究人員

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摘要Butein is a flavonoid isolated from the bark of Rhus verniciflua Stokes and the flowers of Buten monosperma, and is known to be a potential therapeutic drug for treating inflammation and cancer. Cyclooxygenase (COX) converts arachidonic add to prostanoids, and increased expression of its isoform COX-2 has been observed in breast cancer tissues. It has been suggested that COX inhibitors can be used as chemopreventive agents against breast carcinogenesis. This study examined the potential suppressive effect of the flavonoid on phorbol 12-myristate 13-acetate (PMA)-induced COX-2 expression in the non-tumorigenic MCF-10A and cancerous MCF-7 breast cells. Immunoblot and mRNA analyses revealed that butein at or below 10 mu M significantly inhibited PMA-induced COX-2 expression in these breast cells. The blocking of the PKC signaling pathway appeared to be the underlying mechanism. Butein treatment reduced the amount of phospho-mitogen activated protein kinase (MAPK) ERK-1/2, and the total activity of PKC. Activated ERKs might trigger the transcriptional activation of COX-2. Reporter gene assays as well as electrophoretic mobility shift assays (EMSA) illustrated that butein inhibited transcription of this gene. This study showed that butein down-regulated PMA-induced COX-2 expression in both cancerous and non-cancerous breast cells, and such findings could provide the basis for pharmaceutical development of butein. (C) 2010 Elsevier B.V. All rights reserved.
著者Lau GTY, Huang H, Lin SM, Leung LK
期刊名稱European Journal of Pharmacology
出版年份2010
月份12
日期1
卷號648
期次1-3
出版社Elsevier
頁次24 - 30
國際標準期刊號0014-2999
電子國際標準期刊號1879-0712
語言英式英語
關鍵詞Breast cell; Butein; COX-2; Phorbol 12-myristate 13-acetate; PKC
Web of Science 學科類別Pharmacology & Pharmacy; PHARMACOLOGY & PHARMACY

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