Hinokitiol Inhibits Cell Growth through Induction of S-Phase Arrest and Apoptosis in Human Colon Cancer Cells and Suppresses Tumor Growth in a Mouse Xenograft Experiment

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• 作者：Youn-Sun Lee ; Kyeong-Mi Choi ; Wonkyun Kim ; Young-Soo Jeon ; Yong-Moon Lee ; Jin-Tae Hong ; Yeo-Pyo Yun ; Hwan-Soo Yoo
• 刊名：Journal of Natural Products
• 出版年：2013
• 出版时间：December 27, 2013
• 年：2013
• 卷：76
• 期：12
• 页码：2195-2202
• 全文大小：602K
• ISSN：1520-6025

文摘

Hinokitiol (1), a tropolone-related natural compound, induces apoptosis and has anti-inflammatory, antioxidant, and antitumor activities. In this study, the inhibitory effects of 1 were investigated on human colon cancer cell growth and tumor formation of xenograft mice. HCT-116 and SW-620 cells derived from human colon cancers were found to be similarly susceptible to 1, with IC₅₀ values of 4.5 and 4.4 渭M, respectively. Compound 1 induced S-phase arrest in the cell cycle progression and decreased the expression levels of cyclin A, cyclin E, and Cdk2. Conversely, 1 increased the expression of p21, a Cdk inhibitor. Compound 1 decreased Bcl-2 expression and increased the expression of Bax, and cleaved caspase-9 and -3. The effect of 1 on tumor formation when administered orally was evaluated in male BALB/c-nude mice implanted intradermally separately with HCT-116 and SW-620 cells. Tumor volumes and tumor weights in the mice treated with 1 (100 mg/kg) were decreased in both cases. These results suggest that the suppression of tumor formation by compound 1 in human colon cancer may occur through cell cycle arrest and apoptosis.