title: 20S proteasome inhibitory activity of flavonoids isolated from Spatholobus suberectus.
abstract: The promising biological role of the ubiquitin proteasome pathway (UPP) in cancer therapy has recently emerged. Inhibition of proteasome has been proposed as a new therapeutic target for treatment of cancer. Bioassay-guided fractionation of a MeOH extract of the stems of Spatholobus suberectus resulted in seven compounds, liquiritigenin (1), isoliquiritigenin (2), genistein (3), daidzein (4), medicarpin (5), 7-hydroxyflavanone (6) and formononetin (7), which were evaluated for the first time for their inhibitory effect on 20S proteasome. Among the isolated compounds, 2, 3 and 6 exhibited inhibitory activities on human 20S proteasome with IC(50) values of 4.88 ± 1.5, 9.26 ± 1.2 and 5.21 ± 1.5 µm, respectively.
authors.affiliation: School of Biotechnology, Yeungnam University, Gyeongsan 712-749, South Korea. shshim29@ynu.ac.kr
authors.forename: Sang Hee
authors.initials: SH
authors.lastname: Shim
mesh_terms: D000818:Animals; D002851:Chromatography, High Pressure Liquid; D004791:Enzyme Inhibitors / Q000494:pharmacology*; D007887:Fabaceae / Q000737:chemistry*; D005419:Flavonoids / Q000302:isolation & purification / Q000494:pharmacology*; D006801:Humans; D009682:Magnetic Resonance Spectroscopy; D010936:Plant Extracts / Q000494:pharmacology*; D061988:Proteasome Inhibitors
chemical_list: D004791:Enzyme Inhibitors; D005419:Flavonoids; D010936:Plant Extracts; D061988:Proteasome Inhibitors