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標題: 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: Lien, H.M.
赫, 林
Kuo, P.T.
Huang, C.L.
Kao, J.Y.
Lin, H.
Yang, D.Y.
Lai, Y.Y.
關鍵字: chemical-composition;cycle arrest;p53;apoptosis;therapy;suppression;activation;principles;inhibitors;induction
Project: Evidence-Based Complementary and Alternative Medicine
期刊/報告no:: Evidence-Based Complementary and Alternative Medicine, Page(s) 1-8.
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 (75-225 mu M) was associated with significantly increased levels of p53, p21 and p27 and decreased levels of cyclin D1. Concerning COLO 205 cell apoptosis, apiole (> 150 mu M) 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.
ISSN: 1741-427X
DOI: 10.1093/ecam/nep230
Appears in Collections:生命科學系所

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