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| 题名: | Study of the anti-proliferative activity of 5-substituted 4,7-dimethoxy-1,3-benzodioxole derivatives of sy-1 from Antrodia camphorata on human COLO 205 colon cancer cells |
| 作者: | Lai, Y.-Y., Lien, H.-M., Kuo, P.-T., Huang, C.-L., Kao, J.-Y., Lin, H., Yang, D.-Y. |
| 贡献者: | Department of Chemistry, Tunghai University |
| 关键词: | 1,3 benzodioxole derivative;5 substituted 4,7 dimethoxy 1,3 benzodioxole derivative;Antrodia camphorata extract;apiole;caspase 3;caspase 8;caspase 9;cyclin D1;plant extract;protein Bax;protein bcl 2;protein p21;protein p27;protein p53;sy 1;unclassified drug |
| 日期: | 2011 |
| 上传时间: | 2013-05-14T09:02:32Z (UTC)
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| 摘要: | A set of 10 4,7-dimethoxy-1,3-benzodioxole derivatives based on a lead compound previously discovered by our group, SY-1, which was isolated from Antrodia camphorata, were evaluated for their in vitro inhibitory activity on human colorectal carcinoma cells (COLO 205). Structure-activity relationship studies of the 10 compounds indicated the importance of the chain length of the alkyl group at the 5-position, and the 2-propenyl substituent named apiole exhibited the most potent inhibitory activity. In the present study, we demonstrate that the SY-1 analogue apiole decreased the proliferation of COLO 205 cells, but not that of normal human colonic epithelial cells (FHC). The G0/G1 cell cycle arrest induced by apiole (75-225μM) was associated with significantly increased levels of p53, p21 and p27 and decreased levels of cyclin D1. Concerning COLO 205 cell apoptosis, apiole (>150M) treatment significantly increased the levels of cleaved caspases 3, 8, 9 and bax/bcl-2 ratio and induced ladder formation in DNA fragmentation assay and sub-G1 peak in flow cytometry analysis. These findings suggest that apiole can suppress COLO 205 cell growth; however, the detailed mechanisms of these processes require further investigation. Copyright ? 2011 Hsiu-Man Lien et al. |
| 關聯: | Evidence-based Complementary and Alternative Medicine 2011 , art. no. 450529 |
| 显示于类别: | [化學系所] 期刊論文
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