Nat Prod Sci.  2022 Jun;28(2):80-88. 10.20307/nps.2022.28.2.80.

Anti-metastatic Effect of Natural Product-motivated Synthetic PPAR-γ Ligands

  • 1College of Pharmacy, Pusan National University, Busan 46241, Republic of Korea
  • 2College of Pharmacy, Kyung Hee University, Seoul 02447, Republic of Korea


Colorectal cancer is one of the most common cancers globally, ranking second for the number of cancer-related deaths. Metastasis has been reported as the main cause of death in patients with colorectal cancer. Peroxisome proliferator-activated receptor gamma (PPAR-γ) is a transcription factor that functions as a tumor suppressor by inhibiting cellular proliferation, migration, and invasion. In our previous efforts to generate natural product-motivated PPAR-γ ligands, the compounds 1 and 2 were obtained. These compounds activated PPAR-γ and inhibited the migration and invasion of HCT116 colorectal cancer cells, and they were also found to inhibit the epithelial-to-mesenchymal transition, which is a key process in cancer metastasis. Compounds 1 and 2 upregulated expression of the epithelial marker (E-cadherin), and downregulated expression of the mesenchymal marker (N-cadherin) and transcriptional factor (Snail). Therefore, the PPAR-γ agonists 1 and 2 could serve as a valuable model for the study on anti-metastatic leads for the treatment of colorectal cancer.


PPAR-γ agonists; anti-metastasis; epithelial-to-mesenchymal transition; colorectal cancer
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