Research Papers:

Arctigenin inhibits STAT3 and exhibits anticancer potential in human triple-negative breast cancer therapy

Tingting Feng, Wei Cao, Wanxiang Shen, Liang Zhang, Xinsheng Gu, Yang Guo, Hsiang-i Tsai, Xuewen Liu, Jian Li, Jingxuan Zhang, Shan Li, Fuyun Wu and Ying Liu _

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Oncotarget. 2017; 8:329-344. https://doi.org/10.18632/oncotarget.13393

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Tingting Feng1,2,*, Wei Cao3,*, Wanxiang Shen4, Liang Zhang1, Xinsheng Gu5, Yang Guo5, Hsiang-i Tsai4, Xuewen Liu1, Jian Li5, Jingxuan Zhang5, Shan Li5, Fuyun Wu5, Ying Liu1,5

1Laboratory of Molecular Target Therapy of Cancer, Institute of Basic Medical Sciences, Hubei University of Medicine, Shiyan, Hubei 442000, China

2School of Basic Medical Sciences, Anhui Medical University, Hefei, Anhui 230032, China

3MOE Key Laboratory of Industrial Fermentation Microbiology, College of Biotechnology, Tianjin University of Science & Technology, Tianjin 300457, China

4Graduate School at Shenzhen, Tsinghua University, Shenzhen, Guangdong 518055, China

5School of Basic Medical Sciences, Hubei University of Medicine, Shiyan, Hubei 442000, China

*These authors contributed equally to this work

Correspondence to:

Ying Liu, email: ying_liu1002@163.com

Keywords: arctigenin, STAT3, triple-negative breast cancers, computational docking, taxotere

Received: May 05, 2016     Accepted: November 11, 2016     Published: November 16, 2016


Triple-negative breast cancers (TNBCs) are the most aggressive and hard-to-treat breast tumors with poor prognosis, and exploration for novel therapeutic drugs is impending. Arctigenin (Atn), a bioactive lignan isolated from seeds of Arctium lappa L, has been reported to inhibit many cancer types; however, the effect of Atn on TNBC remains unclear. In this study, we demonstrated that Atn decreased proliferation, and induced apoptosis in TNBC cells. Furthermore, we explored the underlying mechanism of Atn inhibition on TNBC cells. Computational docking and affinity assay showed that Atn bound to the SH2 domain of STAT3. Atn inhibited STAT3 binding to genomic DNA by disrupting hydrogen bond linking between DNA and STAT3. In addition, Atn augmented Taxotere®-induced TNBC cell cytotoxicity. TNBC xenograft tests also confirmed the antitumor effect of Atn in vivo. These characteristics render Atn as a promising candidate drug for further development and for designing new effective STAT3 inhibitors.

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