Journal Articles

Activity of the anti-estrogenic cajanin stilbene acid towards breast cancer

July 22, 2015

Activity of the anti-estrogenic cajanin stilbene acid towards breast cancer, July 22, 2015, In Press Accepted Manuscript, Yujie Fu, Onat Kadioglu, Benjamin Wiench, Zuofu Wei, Wei Wang, Meng Luo, Xiaohe Yang, Chengbo Gu, Yuangang Zu, Thomas Efferth

NC Central University


Anti-estrogenic therapy is a mainstay for estrogen receptor (ERα)-positive breast cancer. Due to the development of resistance to established anti-hormones such as tamoxifen, novel compounds are required. The low abundant cajanin stilbene acid (CSA) recently isolated by us from Pigeon Pea (Cajanus cajan) has structural similarities with estrogen. We analyzed the cytotoxic and anti-cancer activity of CSA in ERα-positive and –negative human breast cancer cells in vitro, in vivo and in silico. CSA exerts anti-cancer and anti-estrogenic activities towards ERα-positive breast cancer and it showed cytotoxicity towards tamoxifen-resistant MCF-7 cells, implying that CSA may be active against tamoxifen resistant breast cancer cells. CSA showed low cytotoxicity in ERα-negative breast tumor cells as expected. Comparable cytotoxicity was observed towards p53 negative MCF-7 cells, implying that CSA is effective independent of the p53 status. Xenografted MCF-7 cells in nude mice were better inhibited by CSA than by cyclophosphamide. Testing of 8 primary cell cultures derived from human breast cancer biopsies showed that cell cultures from ER-positive tumors were more sensitive than from ER-negative ones. Dose dependent decrease in ERα protein levels was observed upon CSA treatment. Synergistic effect with tamoxifen was observed in terms of increased p53 protein level. CSA affected pathways related to p53, cancer and cell proliferation. Gene promoter analyses supported the ERα regulation. CSA bound to the same site as 17β-estradiol and tamoxifen on ERα. In conclusion, CSA exerts its anticancer effects in ERα-positive breast cancer cells by binding and inhibiting ERα.


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