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DACT2 Epigenetic Stimulator Exerts Dual Efficacy for Colorectal Cancer Prevention and Treatment

Linlin Lu1, Ying Wang1, Rilan Ou1

  • 1International Institute for Translational Chinese Medicine, Guangzhou University of Chinese Medicine, Guangzhou, Guangdong, 510006, China.

Pharmacological Research
|December 5, 2017
PubMed

Insights

Kaempferol reactivates the DACT2 tumor suppressor gene in colorectal cancer (CRC) by reducing DNA methylation. This epigenetic restoration inhibits Wnt/β-catenin signaling, slowing CRC progression and reducing tumor load.

Area of Science:

  • Oncology
  • Epigenetics
  • Nutritional Biochemistry

Background:

  • DACT2, a tumor suppressor, is often silenced by hypermethylation in colorectal cancer (CRC).
  • DACT2 down-regulation correlates with poor CRC prognosis.
  • Epigenetic restoration of DACT2 is a potential therapeutic strategy for CRC.

Purpose of the Study:

  • To identify nutritional compounds that can epigenetically stimulate DACT2 expression.
  • To investigate if DACT2 epigenetic restoration can reverse CRC tumorigenesis.

Main Methods:

  • Screening of twelve nutritional compounds for DACT2 epigenetic stimulatory activity.
  • Assessing kaempferol's effect on DACT2 expression and methylation in CRC cells (HCT116, HT29, YB5).
  • Investigating kaempferol's mechanism of action, including binding to DNMT1 and Wnt/β-catenin pathway inhibition.
  • Evaluating kaempferol's efficacy in an AOM/DSS-induced CRC mouse model.

Main Results:

  • Kaempferol significantly increased DACT2 expression (up to 3.47-fold) in CRC cells.
  • Kaempferol decreased DACT2 methylation (19.58%-67.00%) and increased unmethylated DACT2 (13.72-fold) by inhibiting DNMT1.
  • Kaempferol suppressed Wnt/β-catenin signaling, reducing CRC cell proliferation and migration.
  • Kaempferol administration reduced tumor load in a CRC mouse model (50.00%-73.52%).

Conclusions:

  • Kaempferol acts as a DACT2 epigenetic stimulator, reversing CRC-associated hypermethylation.
  • Epigenetic reactivation of DACT2 by kaempferol demonstrates chemopreventive and chemotherapeutic potential against CRC.
Keywords:
ChemopreventionDACT2Epigenetic restorationWnt/β-catenin signaling

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