Research Papers:

Cyanidin-3-o-glucoside directly binds to ERα36 and inhibits EGFR-positive triple-negative breast cancer

Li Wang, Haifeng Li, Shiping Yang, Wenqiang Ma, Mei Liu, Shichao Guo, Jun Zhan, Hongquan Zhang, Suk Ying Tsang, Ziding Zhang, Zhaoyi Wang, Xiru Li, Yang-Dong Guo, _ Xiangdong Li

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Oncotarget. 2016; 7:68864-68882. https://doi.org/10.18632/oncotarget.12025

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Li Wang1,*, Haifeng Li1,*, Shiping Yang1, Wenqiang Ma1, Mei Liu2, Shichao Guo1, Jun Zhan3, Hongquan Zhang3, Suk Ying Tsang4, Ziding Zhang1, Zhaoyi Wang5, Xiru Li2, Yang-Dong Guo1, Xiangdong Li1

1State Key Laboratory of the Agro-Biotechnology, College of Horticultural Science, China Agricultural University, Beijing, China

2Department of General Surgery, The 301th Hospital of PLA, Beijing, China

3Key Laboratory of Carcinogenesis and Translational Research, Ministry of Education, State Key Laboratory of Natural and Biomimetic Drugs, Peking University Health Science Center, Beijing, China

4School of Life Sciences and State Key Laboratory of Agro-Biotechnology, Chinese University of Hong Kong, Hong Kong, China

5Beijing Shenogen Pharma Group, Beijing, China

*These authors have contributed equally to this work

Correspondence to:

Yang-Dong Guo, email: yaguo@cau.edu.cn

Xiru Li, email: 2468li@sina.com

Zhaoyi Wang, email: charlie.wang@shenogen.com

Xiangdong Li, email: xiangdongli@cau.edu.cn

Keywords: Cy-3-glu, ERα36, EGFR, triple-negative breast cancer, apoptosis

Received: December 03, 2015    Accepted: September 02, 2016    Published: September 15, 2016


Anthocyanins have been shown to inhibit the growth and metastatic potential of breast cancer (BC) cells. However, the effects of individual anthocyanins on triple-negative breast cancer (TNBC) have not yet been studied. In this study, we found that cyanidin-3-o-glucoside (Cy-3-glu) preferentially promotes the apoptosis of TNBC cells, which co-express the estrogen receptor alpha 36 (ERα36) and the epidermal growth factor receptor (EGFR). We demonstrated that Cy-3-glu directly binds to the ligand-binding domain (LBD) of ERα36, inhibits EGFR/AKT signaling, and promotes EGFR degradation. We also confirmed the therapeutic efficacy of Cy-3-glu on TNBC in the xenograft mouse model. Our data indicates that Cy-3-glu could be a novel preventive/therapeutic agent against the TNBC co-expressed ERα36/EGFR.

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