title: Antineuroinflammatory and Antiproliferative Activities of Constituents from Tilia amurensis.
abstract: As part of our ongoing search for bioactive constituents of natural Korean medicinal resources, we found in a preliminary study that the methanol (MeOH) extract from the trunks of Tilia amurensis RUPR. showed an inhibitory effect on nitric oxide (NO) production in an activated murine microglial cell line. A bioassay-guided fractionation and chemical investigation of the MeOH extract resulted in the isolation and identification of a new isoflavonoid glycoside, orobol 4'-O-β-D-apiofuranosyl-(1→6)-β-D-glucopyranoside (1) and 16 known compounds (2-17). The structure of the new compound was determined by spectroscopic methods, i.e., one-dimensional (1D) and two-dimensional (2D)-NMR techniques and high resolution (HR)-MS, and chemical methods. The antineuroinflammatory activities of the isolated compounds were determined by measuring NO levels in the medium using murine microglial BV-2 cells. Among them, 12 compounds, including compound 1 (most active with an IC50 value of 23.42 µM), inhibited NO production in lipopolysaccharide-stimulated BV-2 cells. Moreover, compounds 1-4 showed moderate antiproliferative activities against the SK-MEL-2 cell line, with IC50 values ranging from 12.31 to 19.67 µM.
authors.affiliation: School of Pharmacy, Sungkyunkwan University.
authors.forename: Ki Hyun
authors.initials: KH
authors.lastname: Kim
authors.forename: Eunjung
authors.initials: E
authors.lastname: Moon
authors.forename: Joon Min
authors.initials: JM
authors.lastname: Cha
authors.forename: Seulah
authors.initials: S
authors.lastname: Lee
authors.forename: Jae Sik
authors.initials: JS
authors.lastname: Yu
authors.forename: Chung Sub
authors.initials: CS
authors.lastname: Kim
authors.forename: Sun Yeou
authors.initials: SY
authors.lastname: Kim
authors.forename: Sang Un
authors.initials: SU
authors.lastname: Choi
authors.forename: Kang Ro
authors.initials: KR
authors.lastname: Lee
mesh_terms: D000818:Animals; D000893:Anti-Inflammatory Agents / Q000737:chemistry* / Q000494:pharmacology*; D000972:Antineoplastic Agents, Phytogenic / Q000737:chemistry* / Q000494:pharmacology*; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D004354:Drug Screening Assays, Antitumor; D006027:Glycosides / Q000737:chemistry / Q000494:pharmacology; D006801:Humans; D007529:Isoflavones / Q000737:chemistry* / Q000494:pharmacology*; D051379:Mice; D017628:Microglia / Q000166:cytology / Q000187:drug effects / Q000276:immunology; D009369:Neoplasms / Q000188:drug therapy; D009569:Nitric Oxide / Q000276:immunology; D032384:Tilia / Q000737:chemistry*
chemical_list: D000893:Anti-Inflammatory Agents; D000972:Antineoplastic Agents, Phytogenic; D006027:Glycosides; D007529:Isoflavones; D009569:Nitric Oxide