Baicalein inhibits progression of osteosarcoma cells through inactivation of the Wnt/β-catenin signaling pathway

// Guo Dai 1, * , Di Zheng 1, * , Qianliang Wang 2 , Jian Yang 1 , Gaiwei Liu 1 , Qi Song 1 , Xiangran Sun 1 , Chunjie Tao 1 , Qingzhu Hu 1 , Tian Gao 3 , Ling Yu 1 and Weichun Guo 1 1 Department of Orthopedics, Renmin Hospital of Wuhan University, Wuhan 430060, Hubei Province, P. R. China 2 Department of Urology Surgery, Renmin Hospital of Wuhan University, Wuhan 430060, Hubei Province, P. R. China 3 Department of Orthopedic Oncology, Key Laboratory of Carcinogenesis and Translational Research, Ministry of Education, Peking University Cancer Hospital & Institute, Beijing 100000, P. R. China * These authors have contributed equally to this work Correspondence to: Weichun Guo, email: guoweichun@aliyun.com Ling Yu, email: scaling@whu.edu.cn Keywords: baicalein, osteosarcoma, proliferation, apoptosis, Wnt signaling pathway Received: July 17, 2017     Accepted: August 29, 2017     Published: September 18, 2017 ABSTRACT Osteosarcoma is a very common type of malignant bone tumor in children and young adults and aberrant activation of Wnt/β-catenin signaling pathway has been discovered in osteosarcoma. The traditional Chinese medicine baicalein was proved to have anti-proliferative and anti-metastatic properties in osteosarcoma, but the mechanism remained poorly understood. In the present study, we assessed the effects of baicalein on osteosarcoma and detected the potential molecular mechanism. We found that baicalein significantly suppressed the proliferation of osteosarcoma cells in a concentration- and time-dependent manner. In additional, baicalein could induce apoptosis and cell cycle arrest and reduce cell motility. Moreover, the level of β-catenin and its target genes, including c-myc, cyclinD1, and survivin significantly decreased in baicalein-treated osteosarcoma cells, whereas exogenous expression of β-catenin could reverse the anti-proliferative and anti-metastatic effects of baicalein. Subsequently, we established a 143B xenograft tumor model and found that baicalein treatment significantly inhibited tumor growth accompanied with inhibiting Wnt/β-catenin pathway. Thus, these findings suggest that baicalein may be a potentially effective Chinese herbal medicine for therapeutics of osteosarcoma and Wnt/β-catenin signaling pathway may serve as an efficient molecular marker or predictive target for osteosarcoma.