期刊
BIOLOGICAL & PHARMACEUTICAL BULLETIN
卷 36, 期 6, 页码 1040-1044出版社
PHARMACEUTICAL SOC JAPAN
DOI: 10.1248/bpb.b13-00158
关键词
cardamonin; colon cancer; beta-catenin; protein degradation
资金
- Basic Science Research Program [2012R1A2A2A01002941]
- Fundamental Technology Program through the National Research Foundation of Korea (NRF) [2012M3A9B2028335]
- Ministry of Education, Science and Technology
- National Research Foundation of Korea [2012M3A9B2028335] Funding Source: Korea Institute of Science & Technology Information (KISTI), National Science & Technology Information Service (NTIS)
Aberrant accumulation of intracellular beta-catenin and subsequent activation of beta-catenin response transcription (CRT) in intestinal epithelial cells is a frequent early event during the development of colon cancer. Here we show that cardamonin, a chalcone isolated from Aplinia katsumadai HAYATA, inhibited CRT in SW480 colon cancer cells that carry inactivating mutation in the adenomatous polyposis coli (APC) gene. Cardamonin also down-regulated intracellular beta-catenin levels in SW480 cells without affecting its mRNA levels. Interestingly, pharmacological inhibition of the proteasome prevented the cardamonin-induced down-regulation of beta-catenin. In addition, cardamonin suppressed the expression of cyclin D1 and c-myc, which are known beta-catenin/T cell factor (TCF)-dependent genes. Moreover, cardamonin inhibited the growth of various colon cancer cells and induced G2/M cell cycle arrest in SW480 colon cancer cells. These findings indicate that cardamonin is a potential chemotherapeutic agent against colon cancer.
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