title: A synthetic chalcone derivative, 2-hydroxy-3',5,5'-trimethoxychalcone (DK-139), suppresses the TNFα-induced invasive capability of MDA-MB-231 human breast cancer cells by inhibiting NF-κB-mediated GROα expression.
abstract: 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 (GROα) 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 (TNFα)-induced GROα gene promoter activity by inhibiting of IκB kinase (IKK) in MDA-MB231 cells. In addition, DK-139 prevented the TNFα-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-κB-mediated GROα expression.
authors.affiliation: Division of Biological Sciences, Biology w/Spec Bioinformatics, Revelle College, University of California, San Diego, CA 92093, USA.
authors.forename: Da Young
authors.initials: DY
authors.lastname: Lee
authors.affiliation: Department of Biological Sciences, College of Biological Science and Biotechnology, Konkuk University, 120 Neundong-ro, Gwangjin-gu, Seoul 05029, Republic of Korea.
authors.forename: Da Hyun
authors.initials: DH
authors.lastname: Lee
authors.affiliation: Cancer and Metabolism Institute, Konkuk University, Seoul 143-701, Republic of Korea.
authors.forename: Jung You
authors.initials: JY
authors.lastname: Jung
authors.affiliation: Department of Applied Chemistry, Dongduk Women's University, Seoul 136-714, Republic of Korea.
authors.forename: Dongsoo
authors.initials: D
authors.lastname: Koh
authors.affiliation: Department of Herbal Crop Research, National Institute of Horticultural and Herbal Science, Rural Development Administration, Eumseong 369-873, Republic of Korea.
authors.forename: Geum-Soog
authors.initials: GS
authors.lastname: Kim
authors.affiliation: Department of Herbal Crop Research, National Institute of Horticultural and Herbal Science, Rural Development Administration, Eumseong 369-873, Republic of Korea.
authors.forename: Young-Sup
authors.initials: YS
authors.lastname: Ahn
authors.affiliation: Department of Biological Sciences, College of Biological Science and Biotechnology, Konkuk University, 120 Neundong-ro, Gwangjin-gu, Seoul 05029, Republic of Korea; Cancer and Metabolism Institute, Konkuk University, Seoul 143-701, Republic of Korea.
authors.forename: Young Han
authors.initials: YH
authors.lastname: Lee
authors.affiliation: Division of Bioscience and Biotechnology, BMIC, Konkuk University, Seoul 143-701, Republic of Korea.
authors.forename: Yoongho
authors.initials: Y
authors.lastname: Lim
authors.affiliation: Department of Biological Sciences, College of Biological Science and Biotechnology, Konkuk University, 120 Neundong-ro, Gwangjin-gu, Seoul 05029, Republic of Korea; Cancer and Metabolism Institute, Konkuk University, Seoul 143-701, Republic of Korea. Electronic address: shinsy@konkuk.ac.kr.
authors.forename: Soon Young
authors.initials: SY
authors.lastname: Shin
mesh_terms: D001943:Breast Neoplasms / Q000188:drug therapy* / Q000235:genetics / Q000378:metabolism / Q000473:pathology; D045744:Cell Line, Tumor; D047188:Chalcones / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D054360:Chemokine CXCL1 / Q000096:biosynthesis* / Q000235:genetics; D004305:Dose-Response Relationship, Drug; D005260:Female; D006801:Humans; D015394:Molecular Structure; D016328:NF-kappa B / Q000037:antagonists & inhibitors* / Q000378:metabolism; D009361:Neoplasm Invasiveness / Q000517:prevention & control*; D012333:RNA, Messenger / Q000235:genetics; D013329:Structure-Activity Relationship; D014409:Tumor Necrosis Factor-alpha / Q000378:metabolism*
chemical_list: C576975:2-hydroxy-3',5,5'-trimethoxychalcone; D047188:Chalcones; D054360:Chemokine CXCL1; D016328:NF-kappa B; D012333:RNA, Messenger; D014409:Tumor Necrosis Factor-alpha
keywords: 2-Hydroxy-3′,5,5′-trimenthoxyochalcone; Growth-regulated oncogene-alpha; Human breast cancer; Invasion; IκB kinase; Tumor necrosis factor alpha