title: Inhibitory lignans against NFAT transcription factor from Acanthopanax koreanum.
abstract: Three lignans isolated from the roots of A. koreanum (Araliaceae), namely eleutheroside E (1), tortoside A (2), and hemiariensin (4), were evaluated for their ability to inhibit NFAT transcription factor. Of these compounds, compound 4, possessing a diarylbutane skeleton, exhibited potent inhibitory activity against NFAT transcription factor (IC50: 36.3 +/- 2.5 microM). However, the activities of 1 (IC50: > 500 microM) and 2 (IC50: 136.1 +/- 9.4 microM), which possess bisaryldioxabicyclooctane skeletons, were lower. As the lignan derivatives of the same skeletons, hinokinin (5) and (-)-yatein (6) with diarylbutane skeletons and (+)-syringaresinol (3) with a bisaryldioxabicyclooctane skeleton were also studied for their inhibitory effects on NFAT transcription factor.
authors.affiliation: College of Pharmacy, Chungnam National University, Daejon 305-764, Korea.
authors.forename: Xing Fu
authors.initials: XF
authors.lastname: Cai
authors.forename: Im Seon
authors.initials: IS
authors.lastname: Lee
authors.forename: Nguyen Tien
authors.initials: NT
authors.lastname: Dat
authors.forename: Guanghai
authors.initials: G
authors.lastname: Shen
authors.forename: Jong Seong
authors.initials: JS
authors.lastname: Kang
authors.forename: Dong Hyun
authors.initials: DH
authors.lastname: Kim
authors.forename: Young Ho
authors.initials: YH
authors.lastname: Kim
mesh_terms: D002021:Buffers; D002851:Chromatography, High Pressure Liquid; D002855:Chromatography, Thin Layer; D004268:DNA-Binding Proteins / Q000235:genetics*; D028001:Eleutherococcus / Q000737:chemistry*; D006801:Humans; D007202:Indicators and Reagents; D019169:Jurkat Cells; D017705:Lignans; D009682:Magnetic Resonance Spectroscopy; D050778:NFATC Transcription Factors; D009687:Nuclear Proteins / Q000235:genetics*; D013056:Spectrophotometry, Ultraviolet; D014157:Transcription Factors / Q000235:genetics*; D014158:Transcription, Genetic / Q000187:drug effects
chemical_list: D002021:Buffers; D004268:DNA-Binding Proteins; D007202:Indicators and Reagents; D017705:Lignans; D050778:NFATC Transcription Factors; D009687:Nuclear Proteins; D014157:Transcription Factors