Xanthones induce cell-cycle arrest and apoptosis in human colon cancer DLD-1 cells

We investigated the antiproliferative effects of four structurally similar prenylated xanthones, α-mangostin, β-mangostin, γ-mangostin, and methoxy-β-mangostin, in human colon cancer DLD-1 cells. We investigated the antiproliferative effects of four structurally similar prenylated xanthones, α-mango...

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Veröffentlicht in:Bioorganic & medicinal chemistry 2005-11, Vol.13 (21), p.6064-6069
Hauptverfasser: Matsumoto, Kenji, Akao, Yukihiro, Ohguchi, Kenji, Ito, Tetsuro, Tanaka, Toshiyuki, Iinuma, Munekazu, Nozawa, Yoshinori
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container_end_page 6069
container_issue 21
container_start_page 6064
container_title Bioorganic & medicinal chemistry
container_volume 13
creator Matsumoto, Kenji
Akao, Yukihiro
Ohguchi, Kenji
Ito, Tetsuro
Tanaka, Toshiyuki
Iinuma, Munekazu
Nozawa, Yoshinori
description We investigated the antiproliferative effects of four structurally similar prenylated xanthones, α-mangostin, β-mangostin, γ-mangostin, and methoxy-β-mangostin, in human colon cancer DLD-1 cells. We investigated the antiproliferative effects of four structurally similar prenylated xanthones, α-mangostin, β-mangostin, γ-mangostin, and methoxy-β-mangostin, in human colon cancer DLD-1 cells. These xanthones differ in the number of hydroxyl and methoxy groups. Except for methoxy-β-mangostin, the other three xanthones strongly inhibited cell growth at 20 μM 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 α- and γ-mangostin, but not that of β-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 α-mangostin and β-mangostin, and S arrest by γ-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.
doi_str_mv 10.1016/j.bmc.2005.06.065
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subjects Anti-cancer
Antineoplastic agents
Apoptosis
Apoptosis - drug effects
Biological and medical sciences
Cell Cycle - drug effects
Cell Line, Tumor
Cell Proliferation - drug effects
Cell-cycle arrest
Colonic Neoplasms - pathology
G1 Phase - drug effects
General aspects
Humans
Medical sciences
Molecular Structure
Pharmacology. Drug treatments
S Phase - drug effects
Xanthone
Xanthones - chemistry
Xanthones - pharmacology
title Xanthones induce cell-cycle arrest and apoptosis in human colon cancer DLD-1 cells
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