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http://dx.doi.org/10.20307/nps.2022.28.2.80

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

Li, Dan-dan (College of Pharmacy, Pusan National University)
Wang, Ying (College of Pharmacy, Pusan National University)
Ju, Zhiran (College of Pharmacy, Pusan National University)
Kim, Eun La (College of Pharmacy, Pusan National University)
Hong, Jongki (College of Pharmacy, Kyung Hee University)
Jung, Jee H. (College of Pharmacy, Pusan National University)
Publication Information
Natural Product Sciences / v.28, no.2, 2022 , pp. 80-88 More about this Journal
Abstract
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.
Keywords
PPAR-${\gamma}$ agonists; anti-metastasis; epithelial-to-mesenchymal transition; colorectal cancer;
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