Jin Young Kim1, Geumi Park2, Manigandan Krishnan3, Eunyoung Ha4, Kyung-Soo Chun5. 1. Department of Internal Medicine, Division of Hematology/Oncology, School of Medicine, Keimyung University, Daegu, Republic of Korea. 2. College of Pharmacy, Keimyung University, Daegu, Republic of Korea. 3. Department of Biochemistry, School of Medicine, Keimyung University Department of Biochemistry, School of Medicine, Keimyung University, Daegu, Republic of Korea. 4. Department of Biochemistry, School of Medicine, Keimyung University Department of Biochemistry, School of Medicine, Keimyung University, Daegu, Republic of Korea chunks@kmu.ac.kr eunyoungha@kmu.ac.kr. 5. College of Pharmacy, Keimyung University, Daegu, Republic of Korea chunks@kmu.ac.kr eunyoungha@kmu.ac.kr.
Abstract
BACKGROUND/AIM: To explore the possibility of a selective small-molecule β-catenin inhibitor, CWP232228, as a potential therapeutic drug in the treatment of colorectal cancer (CRC). MATERIALS AND METHODS: The effect of CWP2228 on HCT116 cells was analysed in vitro via flow cytometry, western immunoblotting, and luciferase reporter assays. NOD-scid IL2Rgammanull mice were employed for an in vivo xenograft study to validate the in vitro studies. RESULTS: CWP232228 treatment decreased the promoter activity and nuclear expression of β-catenin and induced a significant cytotoxic effect in HCT116 cells. CWP232228 treatment induced apoptosis and cell-cycle arrest in the G1 phase of the cell cycle. Furthermore, CWP232228 decreased the expression of aurora kinase A, c-Myc, cyclin D1 and microphthalmia-associated transcription factor. Lastly, CWP232228 also inhibited the growth of xenografted colon cancer cells in mice. CONCLUSION: Collectively, CWP232228 may be used as a potential therapeutic drug in CRC. Copyright
BACKGROUND/AIM: To explore the possibility of a selective small-molecule β-catenin inhibitor, CWP232228, as a potential therapeutic drug in the treatment of colorectal cancer (CRC). MATERIALS AND METHODS: The effect of CWP2228 on HCT116 cells was analysed in vitro via flow cytometry, western immunoblotting, and luciferase reporter assays. NOD-scid IL2Rgammanull mice were employed for an in vivo xenograft study to validate the in vitro studies. RESULTS:CWP232228 treatment decreased the promoter activity and nuclear expression of β-catenin and induced a significant cytotoxic effect in HCT116 cells. CWP232228 treatment induced apoptosis and cell-cycle arrest in the G1 phase of the cell cycle. Furthermore, CWP232228 decreased the expression of aurora kinase A, c-Myc, cyclin D1 and microphthalmia-associated transcription factor. Lastly, CWP232228 also inhibited the growth of xenografted colon cancer cells in mice. CONCLUSION: Collectively, CWP232228 may be used as a potential therapeutic drug in CRC. Copyright
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