Piperine suppresses the Wnt/β-catenin pathway and has anti-cancer effects on colorectal cancer cells.

Scientific Reports
Gracielle C de AlmeidaJose G Abreu

Abstract

More than 94% of colorectal cancer cases have mutations in one or more Wnt/β-catenin signaling pathway components. Inactivating mutations in APC or activating mutations in β-catenin (CTNNB1) lead to signaling overactivation and subsequent intestinal hyperplasia. Numerous classes of medicines derived from synthetic or natural small molecules, including alkaloids, have benefited the treatment of different diseases, including cancer, Piperine is a true alkaloid, derived from lysine, responsible for the spicy taste of black pepper (Piper nigrum) and long pepper (Piper longum). Studies have shown that piperine has a wide range of pharmacological properties; however, piperine molecular mechanisms of action are still not fully understood. By using Wnt/β-catenin pathway epistasis experiment we show that piperine inhibits the canonical Wnt pathway induced by overexpression of β-catenin, β-catenin S33A or dnTCF4 VP16, while also suppressing β-catenin nuclear localization in HCT116 cell line. Additionally, piperine impairs cell proliferation and migration in HCT116, SW480 and DLD-1 colorectal tumor cell lines, while not affecting the non-tumoral cell line IEC-6. In summary, piperine inhibits the canonical Wnt signaling pathway and display...Continue Reading

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Citations

Jan 15, 2021·European Journal of Medicinal Chemistry·Manjinder Singh PhullPrathama S Mainkar
Mar 6, 2021·Phytomedicine : International Journal of Phytotherapy and Phytopharmacology·Sonal SrivastavaSrikanta Kumar Rath
May 1, 2021·International Journal of Molecular Sciences·Karolina WojtowiczRadosław Januchowski

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Methods Mentioned

BETA
ubiquitination
nuclear translocation
IEC-6
xenografts
column chromatography
Assay
flow cytometry
electrophoresis

Software Mentioned

GraphPad Prism
GraphPad
CellQuest

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