title: Gymnasterkoreayne G, a new inhibitory polyacetylene against NFAT transcription factor from Gymnaster koraiensis.
abstract: A new polyacetylene, gymnasterkoreayne G (1) and seven known (2--8) constituents were isolated from the leaves of Gymnaster koraiensis. Base on extensive 1D and 2D NMR spectroscopic data, the structure of the new compound was identified as erythro-8(S)-9(Z),16-heptadecadiene-4,6-diyne-2,3,8-triol. Isolated compounds were evaluated for their ability to inhibit NFAT transcription factor. While other components did not show activity, most of polyacetylene components markedly inhibit NFAT transcription factor. Of these compounds, gymnasterkoreayne B (3) was the most potent (IC(50) 1.44+/-0.59 microM). In term of the isomers, compound 1 (IC(50) 43.9+/-2.24 microM) with an erythro-configuration showed less inhibition than 2 (IC(50) 7.24+/-0.42 microM) with a threo-configuration.
authors.affiliation: College of Pharmacy, Chungnam National University, Daejeon 305-764, Korea.
authors.forename: Nguyen Tien
authors.initials: NT
authors.lastname: Dat
authors.forename: Xing Fu
authors.initials: XF
authors.lastname: Cai
authors.forename: Quanghai
authors.initials: Q
authors.lastname: Shen
authors.forename: Im Seon
authors.initials: IS
authors.lastname: Lee
authors.forename: Eun Joo
authors.initials: EJ
authors.lastname: Lee
authors.forename: Yong Ki
authors.initials: YK
authors.lastname: Park
authors.forename: Kihwan
authors.initials: K
authors.lastname: Bae
authors.forename: Young Ho
authors.initials: YH
authors.lastname: Kim
mesh_terms: D000114:Acetylene / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000494:pharmacology; D000480:Alkynes / Q000138:chemical synthesis* / Q000494:pharmacology*; D019659:Asteraceae / Q000737:chemistry*; D002021:Buffers; D004268:DNA-Binding Proteins / Q000037:antagonists & inhibitors*; D006801:Humans; D007202:Indicators and Reagents; D019169:Jurkat Cells; D009682:Magnetic Resonance Spectroscopy; D050778:NFATC Transcription Factors; D009687:Nuclear Proteins / Q000037:antagonists & inhibitors*; D010936:Plant Extracts / Q000737:chemistry; D015302:Simian Immunodeficiency Virus; D016339:Spectrometry, Mass, Fast Atom Bombardment; D013055:Spectrophotometry, Infrared; D013778:Tetrazolium Salts; D013844:Thiazoles; D014157:Transcription Factors / Q000037:antagonists & inhibitors*
chemical_list: D000480:Alkynes; D002021:Buffers; D004268:DNA-Binding Proteins; D007202:Indicators and Reagents; D050778:NFATC Transcription Factors; D009687:Nuclear Proteins; D010936:Plant Extracts; D013778:Tetrazolium Salts; D013844:Thiazoles; D014157:Transcription Factors; C505039:gymnasterkoreayne G; C022616:thiazolyl blue; D000114:Acetylene