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- Title
Evodiamine Stabilizes Topoisomerase I-DNA Cleavable Complex to Inhibit Topoisomerase I Activity.
- Authors
Chan, Agnes L.-F.; Wen-Shin Chang; Li-Min Chen; Chi-Ming Lee; Chiao-En Chen; Chun-Mao Lin; Jau-Lang Hwang
- Abstract
Evodiamine (EVO), an alkaloidal compound isolated from Evodia rutaecarpa (Juss.), has been reported to affect many physiological functions. Topoisomerase inhibitors have been developed in a variety of clinical applications. In the present study, we report the topoisomerase I (TopI) inhibitory activity of EVO, which may have properties that lead to improved therapeutic benefits. EVO is able to inhibit supercoiled plasmid DNA relaxation catalyzed by TopI. Upon treatment 0~10 μM EVO TopI was depleted in MCF-7 breast cancer cells in a concentration-dependent and time-dependent manner in 0~120 min. A K-SDS precipitation assay was performed to measure the extent of Top I-trapped chromosomal DNA. The ability of EVO to cause the formation of a TopI-DNA complex increased in a concentration-dependent manner, in that the DNA trapped increased by 24.2% in cells treated with 30 μM. The results suggest that EVO inhibits TopI by stabilizing the enzyme and DNA covalent complex.
- Subjects
PHYSIOLOGICAL effects of alkaloids; DNA topoisomerase I; BREAST cancer; CANCER treatment; CANCER cells; DNA; CATALYSIS; PLASMIDS; ENZYMES
- Publication
Molecules, 2009, Vol 14, Issue 4, p1342
- ISSN
1420-3049
- Publication type
Article
- DOI
10.3390/molecules14041342