title: 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.
abstract: 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 μM) was associated with significantly increased levels of p53, p21 and p27 and decreased levels of cyclin D1. Concerning COLO 205 cell apoptosis, apiole (>150 μM) 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.
authors.affiliation: Department of Chemistry, Tunghai University, Taichung, Taiwan.
authors.forename: Hsiu-Man
authors.initials: HM
authors.lastname: Lien
authors.forename: Po-Tsun
authors.initials: PT
authors.lastname: Kuo
authors.forename: Chao-Lu
authors.initials: CL
authors.lastname: Huang
authors.forename: Jung-Yie
authors.initials: JY
authors.lastname: Kao
authors.forename: Ho
authors.initials: H
authors.lastname: Lin
authors.forename: Ding-Yah
authors.initials: DY
authors.lastname: Yang
authors.forename: Ya-Yun
authors.initials: YY
authors.lastname: Lai