A synthetic chalcone derivative, 2-hydroxy-3 ',5,5 '-trimethoxychalcone (DK-139), suppresses the TNF alpha-induced invasive capability of MDA-MB-231 human breast cancer cells by inhibiting NF-kappa B-mediated GRO alpha expression

作者：Lee Da Young; Lee Da Hyun; Jung Jung You; Koh Dongsoo; Kim Geum Soog; Ahn Young Sup; Lee Young Han; Lim Yoongho; Shin Soon Young^*

来源：Bioorganic & Medicinal Chemistry Letters, 2016, 26(1): 203-208.

DOI：10.1016/j.bmcl.2015.10.094

• 2-Hydroxy-3 ',5,5 '-trimenthoxyochalcone
• Growth-regulated oncogene-alpha
• Tumor necrosis factor alpha
• I kappa B kinase
• Invasion
• Human breast cancer

2-Hydroxy-3',5,5'-trimenthoxyochalcone (DK-139) is a synthetic chalcone-derived compound. This study evaluated the biological activity of DK-139 on the inhibition of tumor metastasis. Growth-regulated oncogene-alpha (GRO alpha) plays an important role in the progression of tumor development by stimulating angiogenesis and metastasis. In this study, DK-139 inhibited tumor necrosis factor alpha (TNF alpha)-induced GRO alpha gene promoter activity by inhibiting of I kappa B kinase (IKK) in MDA-MB231 cells. In addition, DK-139 prevented the TNF alpha-induced cell migration, F-actin formation, and invasive capability of MDA-MB-231 cells. These findings suggest that DK-139 is a potential drug candidate for the inhibition of tumor cell locomotion and invasion via the suppression of NF-kappa B-mediated GRO alpha expression.

• 出版日期2016-1-1