title: Trisindoline synthesis and anticancer activity.
abstract: Expression of a Rhodococcus-derived oxygenase gene in Escherichia coli yielded indigo metabolites with cytotoxic activity against cancer cells. Bioactivity-guided fractionation of these indigo metabolites led to the isolation of trisindoline as the agent responsible for the observed in vitro cytotoxic activity against cancer cells. While the cytotoxicity of etoposide, a common anticancer drug, was dramatically decreased in multidrug-resistant (MDR) cancer cells compared with treatment of parental cells, trisindoline was found to have similar cytotoxicity effects on both parental and MDR cell lines. In addition, the cytotoxic effects of trisindoline were resistant to P-glycoprotein overexpression, one of the most common mechanisms of drug resistance in cancer cells, supporting its use to kill MDR cancer cells.
authors.affiliation: Department of Biology, Yonsei University, 134 Shinchon, Seoul 120-749, Republic of Korea.
authors.forename: Miyoun
authors.initials: M
authors.lastname: Yoo
authors.forename: Sang-Un
authors.initials: SU
authors.lastname: Choi
authors.forename: Ki Young
authors.initials: KY
authors.lastname: Choi
authors.forename: Gyu Hwan
authors.initials: GH
authors.lastname: Yon
authors.forename: Jong-Chan
authors.initials: JC
authors.lastname: Chae
authors.forename: Dockyu
authors.initials: D
authors.lastname: Kim
authors.forename: Gerben J
authors.initials: GJ
authors.lastname: Zylstra
authors.forename: Eungbin
authors.initials: E
authors.lastname: Kim