title: Inhibition of LFA-1/ICAM-1-mediated cell adhesion by stilbene derivatives from Rheum undulatum.
abstract: Six stilbenes were isolated from the methanol extract of Rheum undulatum rhizomes by bioactivity-guided fractionation. The structures of the compounds were determined by spectroscopic analysis ((1)H-, (13)C-NMR and MS), to be desoxyrhapontigenin (1), rhapontigenin (2), trans-resveratrol (3), piceatannol (4), piceatannol-3'-O-β-D-glucopyranoside (5) and isorhapontin (6). Compounds 1-4 inhibited the direct binding between sICAM-1 and LFA-1 of the THP-1 cells in a dose-dependent manner with IC(50) values of 50.1, 25.4, 33.4 and 45.9 μM, respectively. On the other hand, the other compounds 5 and 6 with a glucose moiety in each molecule did not show any inhibitory activity in the cell adhesion assay (IC(50) values of >100.0 μM). Compounds 2, 3 and 4 also had an inhibitory effect on direct binding between sVCAM-1 and VLA-4 of THP-1 cells. This suggests that the stilbenes from Rheum undulatum rhizomes are good candidates for therapeutic strategies towards inflammation.
authors.affiliation: Bioindustrial Process Research Center, Bio-Materials Research Institute, Jeongeup-si, Korea.
authors.forename: Seung Woong
authors.initials: SW
authors.lastname: Lee
authors.forename: Byung Soon
authors.initials: BS
authors.lastname: Hwang
authors.forename: Mi-Hwa
authors.initials: MH
authors.lastname: Kim
authors.forename: Chan-Sun
authors.initials: CS
authors.lastname: Park
authors.forename: Woo Song
authors.initials: WS
authors.lastname: Lee
authors.forename: Hyun-Mee
authors.initials: HM
authors.lastname: Oh
authors.forename: Mun-Chual
authors.initials: MC
authors.lastname: Rho
mesh_terms: D000893:Anti-Inflammatory Agents / Q000302:isolation & purification* / Q000494:pharmacology; D001665:Binding Sites; D002448:Cell Adhesion / Q000187:drug effects; D045744:Cell Line, Tumor; D002470:Cell Survival / Q000187:drug effects; D002851:Chromatography, High Pressure Liquid; D004305:Dose-Response Relationship, Drug; D006801:Humans; D018799:Intercellular Adhesion Molecule-1 / Q000378:metabolism*; D008024:Ligands; D016169:Lymphocyte Function-Associated Antigen-1 / Q000378:metabolism*; D009682:Magnetic Resonance Spectroscopy; D015394:Molecular Structure; D010946:Plants, Medicinal; D012250:Rheum / Q000737:chemistry*; D027343:Rhizome / Q000737:chemistry; D021241:Spectrometry, Mass, Electrospray Ionization; D013267:Stilbenes / Q000737:chemistry / Q000302:isolation & purification* / Q000494:pharmacology
chemical_list: D000893:Anti-Inflammatory Agents; D008024:Ligands; D016169:Lymphocyte Function-Associated Antigen-1; D013267:Stilbenes; D018799:Intercellular Adhesion Molecule-1