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BMC Complementary Medicine and Therapies

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Open Access 01-12-2018 | Research article

Gigantol inhibits Wnt/β-catenin signaling and exhibits anticancer activity in breast cancer cells

Authors: Shubin Yu, Zhongyuan Wang, Zijie Su, Jiaxing Song, Liang Zhou, Qi Sun, Shanshan Liu, Shiyue Li, Ying Li, Meina Wang, Guo-Qiang Zhang, Xue Zhang, Zhong-Jian Liu, Desheng Lu

Published in: BMC Complementary Medicine and Therapies | Issue 1/2018

Abstract

Background

Gigantol is a bibenzyl compound derived from several medicinal orchids. This biologically active compound has been shown to have promising therapeutic potential against cancer cells, but its mechanism of action remains unclear.

Methods

The inhibitory effect of gigantol on Wnt/β-catenin signaling was evaluated with the SuperTOPFlash reporter system. The levels of phosphorylated low-density lipoprotein receptor related protein 6 (LRP6), total LRP6 and cytosolic β-catenin were determined by Western blot analysis. The expression of Wnt target genes was analyzed using real-time PCR. Cell viability was measured with a MTT assay. The effect of gigantol on cell migration was examined using scratch wound-healing and transwell migration assays.

Results

Gigantol decreased the level of phosphorylated LRP6 and cytosolic β-catenin in HEK293 cells. In breast cancer MDA-MB-231 and MDA-MB-468 cells, treatment with gigantol reduced the level of phosphorylated LRP6, total LRP6 and cytosolic β-catenin in a dose-dependent manner, resulting in a decrease in the expression of Wnt target genes Axin2 and Survivin. We further demonstrated that gigantol suppressed the viability and migratory capacity of breast cancer cells.

Conclusion

Gigantol is a novel inhibitor of the Wnt/β-catenin pathway. It inhibits Wnt/β-catenin signaling through downregulation of phosphorylated LRP6 and cytosolic β-catenin in breast cancer cells.

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Title: Gigantol inhibits Wnt/β-catenin signaling and exhibits anticancer activity in breast cancer cells
Authors: Shubin Yu
Zhongyuan Wang
Zijie Su
Jiaxing Song
Liang Zhou
Qi Sun
Shanshan Liu
Shiyue Li
Ying Li
Meina Wang
Guo-Qiang Zhang
Xue Zhang
Zhong-Jian Liu
Desheng Lu
Publication date: 01-12-2018
Publisher: BioMed Central
Published in: BMC Complementary Medicine and Therapies / Issue 1/2018
Electronic ISSN: 2662-7671
DOI: https://doi.org/10.1186/s12906-018-2108-x

Keynote webinar | Spotlight on medication adherence

Springer Medicine

Gigantol inhibits Wnt/β-catenin signaling and exhibits anticancer activity in breast cancer cells

Abstract

Background

Methods

Results

Conclusion

Keynote webinar | Spotlight on medication adherence

Springer Medicine

Abstract

Background

Methods

Results

Conclusion

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