title: Xanthones induce cell-cycle arrest and apoptosis in human colon cancer DLD-1 cells.
abstract: We investigated the antiproliferative effects of four structurally similar prenylated xanthones, alpha-mangostin, beta-mangostin, gamma-mangostin, and methoxy-beta-mangostin, in human colon cancer DLD-1 cells. These xanthones differ in the number of hydroxyl and methoxy groups. Except for methoxy-beta-mangostin, the other three xanthones strongly inhibited cell growth at 20 microM and their antitumor efficacy was correlated with the number of hydroxyl groups. Hoechst 33342 nuclear staining and nucleosomal DNA-gel electrophoresis revealed that the antiproliferative effects of alpha- and gamma-mangostin, but not that of beta-mangostin, were associated with apoptosis. It was also shown that their antiproliferative effects were associated with cell-cycle arrest by affecting the expression of cyclins, cdc2, and p27; G1 arrest was by alpha-mangostin and beta-mangostin, and S arrest by gamma-mangostin. These findings provide a relevant basis for the development of xanthones as an agent for cancer prevention and combination therapy with anti-cancer drugs.
authors.affiliation: Gifu International Institute of Biotechnology, 1-1 Naka-Fudogaoka, Kakamigahara, Gifu 504-0838, Japan. matsumoto@bio.rd.pref.gifu.jp
authors.forename: Kenji
authors.initials: K
authors.lastname: Matsumoto
authors.forename: Yukihiro
authors.initials: Y
authors.lastname: Akao
authors.forename: Kenji
authors.initials: K
authors.lastname: Ohguchi
authors.forename: Tetsuro
authors.initials: T
authors.lastname: Ito
authors.forename: Toshiyuki
authors.initials: T
authors.lastname: Tanaka
authors.forename: Munekazu
authors.initials: M
authors.lastname: Iinuma
authors.forename: Yoshinori
authors.initials: Y
authors.lastname: Nozawa
mesh_terms: D017209:Apoptosis / Q000187:drug effects*; D002453:Cell Cycle / Q000187:drug effects*; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D003110:Colonic Neoplasms / Q000473:pathology*; D016193:G1 Phase / Q000187:drug effects; D006801:Humans; D015394:Molecular Structure; D016196:S Phase / Q000187:drug effects; D044004:Xanthones / Q000737:chemistry / Q000494:pharmacology*
chemical_list: D044004:Xanthones; C021053:mangostin