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

Ya Yun Lai, Hsiu Man Lien, Po Tsun Kuo, Chao Lu Huang, Jung Yie Kao, Ho Lin, Ding Yah Yang

Research output: Contribution to journalArticle

14 Citations (Scopus)

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 (75-225μM) 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.

Original languageEnglish (US)
Article number450529
JournalEvidence-based Complementary and Alternative Medicine
Volume2011
DOIs
StatePublished - 2011

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Antrodia
Colonic Neoplasms
G1 Phase Cell Cycle Checkpoints
Caspase 8
Cyclin D1
DNA Fragmentation
Structure-Activity Relationship
Human Activities
Caspase 3
Colorectal Neoplasms
Flow Cytometry
Epithelial Cells
apiole
1,3-benzodioxole
Apoptosis
Growth

ASJC Scopus subject areas

  • Complementary and alternative medicine

Cite this

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. / Lai, Ya Yun; Lien, Hsiu Man; Kuo, Po Tsun; Huang, Chao Lu; Kao, Jung Yie; Lin, Ho; Yang, Ding Yah.

In: Evidence-based Complementary and Alternative Medicine, Vol. 2011, 450529, 2011.

Research output: Contribution to journalArticle

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