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Anti‐cancer activity of trans ‐chalcone in osteosarcoma: Involvement of Sp1 and p53
Author(s) -
Silva Gabriel,
Marins Mozart,
Fachin Ana Lúcia,
Lee SeongHo,
Baek Seung Joon
Publication year - 2016
Publication title -
molecular carcinogenesis
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.254
H-Index - 97
eISSN - 1098-2744
pISSN - 0899-1987
DOI - 10.1002/mc.22386
Subject(s) - osteosarcoma , chalcone , biology , apoptosis , cancer research , cancer , cancer cell , cell culture , metastasis , genetics , chemistry , stereochemistry
Osteosarcoma is the most common bone cancer. Although the emergence of multidrug therapies has improved available treatments for osteosarcoma, approximately 30% of patients will still develop metastasis. Currently, much anticancer therapy uses drugs that affect oncogenes/tumor suppressor genes, such as p53 (up‐regulation) and Sp1 (down‐regulation). Chalcones are secondary metabolites of plants and have been demonstrated to induce apoptosis in human cancer cells. Building on this knowledge, we evaluated the ability of trans ‐chalcone to reduce viability, to induce apoptosis, and to alter gene expression of p53 and Sp1 in human osteosarcoma cell lines. We found that treatment of trans ‐chalcone inhibited growth of osteosarcoma cells in a dose‐ and time‐dependent manner, with significant inhibition at 10 μM after 48 h; apoptosis was also induced in a dose‐dependent manner, with 1.9‐ and 3.6‐fold induction at 10 μM and 50 μM, respectively, compared to non‐treated cells. Further experiments suggest that trans ‐chalcone affected Sp1 down‐regulation at the transcriptional level, whereas trans ‐chalcone up‐regulated p53 expression at the post‐translational level. trans ‐chalcone and its derivatives could be important in the development of future clinical trials in osteosarcoma. © 2015 Wiley Periodicals, Inc.