title: Biotransformation products of phellopterin by rat liver microsomes and the inhibition on NO production in LPS-activated RAW264.7 cells.
abstract: Four new coumarins (2',3'-dihydroxyphellopterin, E-5-methoxytrichoclin acetate, Z-5-methoxytrichoclin acetate, and E-5-methoxytrichoclin) and three known coumarins (byakangelicol, byakangelicin, and Z-5-methoxytrichoclin) were produced by liver microsomes from rats pre-treated with sodium phenobarbital. The chemical structures were elucidated on the basis of their spectroscopic data. The inhibitory activities of nitric oxide (NO) production in lipopolysaccharide-activated macrophage-like cell line RAW264.7 were tested. The main biotransformation product, byakangelicin, showed inhibitory activities of NO production with the IC₅₀ value of 217.83 μM, whereas the parent compound phellopterin showed cytotoxic effect on RAW264.7 cell at the concentration from 40 to 400 μM.
authors.affiliation: State Key Laboratory of Natural and Biomimetic Drugs, Department of Natural Medicines, School of Pharmaceutical Sciences, Peking University Health Science Center, Peking University, Beijing 100191, China.
authors.forename: Ai-Hong
authors.initials: AH
authors.lastname: Zhao
authors.forename: Xin-Bao
authors.initials: XB
authors.lastname: Yang
authors.forename: Xiu-Wei
authors.initials: XW
authors.lastname: Yang
authors.forename: You-Bo
authors.initials: YB
authors.lastname: Zhang
authors.forename: Wei
authors.initials: W
authors.lastname: Xu
authors.forename: Jian-Xun
authors.initials: JX
authors.lastname: Liu
mesh_terms: D000818:Animals; D003374:Coumarins / Q000494:pharmacology*; D008070:Lipopolysaccharides / Q000494:pharmacology*; D008264:Macrophages / Q000187:drug effects*; D008297:Male; D051379:Mice; D008862:Microsomes, Liver / Q000187:drug effects / Q000378:metabolism; D009569:Nitric Oxide / Q000037:antagonists & inhibitors* / Q000096:biosynthesis; D019906:Nuclear Magnetic Resonance, Biomolecular; D051381:Rats
chemical_list: D003374:Coumarins; D008070:Lipopolysaccharides; C514031:phellodenol H; C104601:phellopterin; D009569:Nitric Oxide