title: Potent inhibition of bacterial neuraminidase activity by pterocarpans isolated from the roots of Lespedeza bicolor.
abstract: Bacterial neuraminidase has been highlighted as a key enzyme for pathogenic infection and sepsis. Six pterocarpans displaying significant levels of neuraminidase inhibitory activity were isolated from the root bark of Lespedeza bicolor. The isolated compounds were identified as three new pterocarpans (1-3) together with known compounds erythrabyssin II (4), lespebuergine G4 (5), and 1-methoxyerythrabyssin II (6). The new compounds were characterized as bicolosin A (1), bicolosin B (2), and bicolosin C (3). All compounds inhibited bacterial neuraminidase in a dose-dependent manner with significant inhibition (IC(50)=0.09-3.25 μM). All neuraminidase inhibitors screened were found to exhibit noncompetitive kinetics. The three most potent neuraminidase inhibitors (1, 3 and 6) feature a methoxy substitution on C-1.
authors.affiliation: Division of Applied Life Science (BK21 program), IALS, Gyeongsang National University, Jinju 660-701, Republic of Korea.
authors.forename: Hyun Sim
authors.initials: HS
authors.lastname: Woo
authors.forename: Dae Wook
authors.initials: DW
authors.lastname: Kim
authors.forename: Marcus J
authors.initials: MJ
authors.lastname: Curtis-Long
authors.forename: Byong Won
authors.initials: BW
authors.lastname: Lee
authors.forename: Ji Hye
authors.initials: JH
authors.lastname: Lee
authors.forename: Jun Young
authors.initials: JY
authors.lastname: Kim
authors.forename: Jae Eun
authors.initials: JE
authors.lastname: Kang
authors.forename: Ki Hun
authors.initials: KH
authors.lastname: Park
mesh_terms: D000900:Anti-Bacterial Agents / Q000302:isolation & purification* / Q000494:pharmacology*; D003016:Clostridium perfringens / Q000187:drug effects / Q000201:enzymology*; D004791:Enzyme Inhibitors / Q000302:isolation & purification / Q000494:pharmacology; D005738:Gas Gangrene / Q000188:drug therapy / Q000201:enzymology; D006801:Humans; D029884:Lespedeza / Q000737:chemistry*; D009439:Neuraminidase / Q000037:antagonists & inhibitors* / Q000378:metabolism; D018517:Plant Roots / Q000737:chemistry; D036343:Pterocarpans / Q000302:isolation & purification* / Q000494:pharmacology*
chemical_list: D000900:Anti-Bacterial Agents; D004791:Enzyme Inhibitors; D036343:Pterocarpans; D009439:Neuraminidase