title: Flavonoids that mimic human ligands from the whole plants of Euphorbia lunulata.
abstract: In our investigation of a cell proliferation-based screening assay using human ligand-dependent cell lines for medicinal herbal extracts, the acetone extract of the whole plants of Euphorbia lunulata (EL) was observed for its proliferation activity for insulin- and interleukin-10 (IL-10)-dependent cell lines. Fractionation of the active extract led to the isolation of one new flavonoid galactoside, quercetin 3-O-(2'',3''-digalloyl)-beta-D-galactopyranoside (1), and four known ones, quercetin 3-O-(2''-galloyl)-beta-D-galactopyranoside (2), hyperin (3), quercetin (4), and gallic acid (5). Compounds 1 and 2 showed insulin-like activity. Compounds 4 and 5 showed IL-10-like activity. This is the first report of these activities of EL, and 1 and 2 will become the seed compounds for the development of a nonpeptidyl insulin substitutional medicine. Compounds 4 and 5 support the pharmacological use of EL, which has been employed as an herbal medicine for the treatment of bronchial asthma.
authors.affiliation: Research and Development Division, SSP CO., LTD, Tokyo, Japan.
authors.forename: Tadahiro
authors.initials: T
authors.lastname: Nishimura
authors.forename: Li-Yan
authors.initials: LY
authors.lastname: Wang
authors.forename: Kouji
authors.initials: K
authors.lastname: Kusano
authors.forename: Susumu
authors.initials: S
authors.lastname: Kitanaka
mesh_terms: D002460:Cell Line; D049109:Cell Proliferation / Q000187:drug effects; D004365:Drugs, Chinese Herbal / Q000737:chemistry* / Q000302:isolation & purification* / Q000494:pharmacology; D028481:Euphorbia / Q000737:chemistry*; D005419:Flavonoids / Q000737:chemistry / Q000302:isolation & purification* / Q000494:pharmacology*; D006131:Growth Inhibitors / Q000737:chemistry / Q000302:isolation & purification* / Q000494:pharmacology*; D006801:Humans; D008024:Ligands; D018716:Molecular Mimicry; D010946:Plants, Medicinal / Q000737:chemistry
chemical_list: D004365:Drugs, Chinese Herbal; D005419:Flavonoids; D006131:Growth Inhibitors; D008024:Ligands