Emetine exhibits anticancer activity in breast cancer cells as an antagonist of Wnt/β‑catenin signaling

依米丁作为 Wnt/β-catenin 信号拮抗剂,在乳腺癌细胞中表现出抗癌活性

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作者:Qi Sun, Qiuxia Fu, Shiyue Li, Junjun Li, Shanshan Liu, Zhongyuan Wang, Zijie Su, Jiaxing Song, Desheng Lu

Abstract

Emetine, an amoebicidal drug, exerts potent anticancer activity against various solid tumors, however, the underlying molecular mechanism remains unclear. In the present study, the effects of emetine were investigated on various proteins involved in the Wnt/β‑catenin signaling pathway, which has been linked to various human cancers. It was revealed that emetine blocked Wnt/β‑catenin signaling by targeting components of this pathway, including the low‑density lipoprotein‑receptor‑related protein 6 (LRP6) and disheveled (DVL). Moreover, nanomolar concentrations of emetine decreased phosphorylation of these proteins and suppressed the expression of Wnt target genes, including fibronectin, frizzled‑7 (Fzd7), c‑Myc, Nanog and CD133 in MDA‑MB‑231 and MDA‑MB‑468 breast cancer cells. Additionally, emetine treatment induced apoptosis and suppressed the viability, migration, invasion, and sphere formation of breast cancer cells. Collectively the present results indicated that emetine antagonizes Wnt/β‑catenin signaling, providing insight into the molecular mechanism underlying the anticancer activity of emetine.

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