2. Academic Validation
  3. Triptonide Effectively Inhibits Wnt/β-Catenin Signaling via C-terminal Transactivation Domain of β-catenin

Triptonide Effectively Inhibits Wnt/β-Catenin Signaling via C-terminal Transactivation Domain of β-catenin

  • Sci Rep. 2016 Sep 6;6:32779. doi: 10.1038/srep32779.
Jessica Chinison 1,  Jose S Aguilar 1,  Alan Avalos 1,  Ying Huang 2,  Zhijun Wang 2,  D Joshua Cameron 3,  Jijun Hao 1 4
Affiliations

Affiliations

  • 1 College of Veterinary Medicine, Western University of Health Sciences, Pomona, CA 91766, USA.
  • 2 College of Pharmacy, Western University of Health Sciences, Pomona, CA 91766, USA.
  • 3 College of Optometry, Western University of Health Sciences, Pomona, CA 91766, USA.
  • 4 Graduate College of Biomedical Sciences, Western University of Health Sciences, Pomona, CA 91766, USA.
PMID: 27596363 DOI: 10.1038/srep32779
Abstract

Abnormal activation of canonical Wnt/β-catenin signaling is implicated in many diseases including Cancer. As a result, therapeutic agents that disrupt this signaling pathway have been highly sought after. Triptonide is a key bioactive small molecule identified in a traditional Chinese medicine named Tripterygium wilfordii Hook F., and it has a broad spectrum of biological functions. Here we show that triptonide can effectively inhibit canonical Wnt/β-catenin signaling by targeting the downstream C-terminal transcription domain of β-catenin or a nuclear component associated with β-catenin. In addition, triptonide treatment robustly rescued the zebrafish "eyeless" phenotype induced by GSK-3β antagonist 6-bromoindirubin-30-oxime (BIO) for Wnt signaling activation during embryonic gastrulation. Finally, triptonide effectively induced Apoptosis of Wnt-dependent Cancer cells, supporting the therapeutic potential of triptonide.

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