title: Biscoumarin derivatives from Edgeworthia gardneri that inhibit the lyase activity of DNA polymerase beta.
abstract: Bioassay-guided fractionation of an active methyl ethyl ketone extract of Edgeworthia gardneri, using an assay to monitor DNA polymerase beta lyase inhibition, resulted in the isolation of three known biscoumarin derivatives, 7-hydroxy-3,7'-dicoumaryl ether (edgeworin, 1), 7-hydroxy-6-methoxy-3,7'-dicoumaryl ether (daphnoretin, 2), and 6,7-dihydroxy-3,7'-dicoumaryl ether (edgeworthin, 3). Compounds 1-3 inhibited the lyase activity of DNA polymerase beta with IC(50) values of 7.3 microg/mL (22.5 microM), 43.0 microg/mL (122.3 microM), and 32.1 microg/mL (94.8 microM), respectively.
authors.affiliation: Department of Chemistry, University of Virginia, Charlottesville, Virginia 22901, USA.
authors.forename: Shi-Sheng
authors.initials: SS
authors.lastname: Li
authors.forename: Zhijie
authors.initials: Z
authors.lastname: Gao
authors.forename: Xizhi
authors.initials: X
authors.lastname: Feng
authors.forename: Sidney M
authors.initials: SM
authors.lastname: Hecht
mesh_terms: D001631:Bhutan; D003374:Coumarins / Q000737:chemistry / Q000302:isolation & purification* / Q000494:pharmacology*; D019951:DNA Polymerase beta / Q000037:antagonists & inhibitors*; D004791:Enzyme Inhibitors / Q000494:pharmacology*; D020128:Inhibitory Concentration 50; D008190:Lyases / Q000037:antagonists & inhibitors*; D029645:Thymelaeaceae / Q000737:chemistry*
chemical_list: D003374:Coumarins; D004791:Enzyme Inhibitors; C093655:edgeworin; C493142:edgeworthin; C035316:daphnoretin; D019951:DNA Polymerase beta; D008190:Lyases