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: Kenji Matsumoto, Yukihiro Akao, Kenji Ohguchi, Tetsuro Ito, Toshiyuki Tanaka, Munekazu Iinuma, Yoshinori Nozawa
• Journal: Bioorganic & medicinal chemistry (Bioorg Med Chem) Vol. 13 Issue 21 Pg. 6064-9 (Nov 01 2005) ISSN: 0968-0896 [Print] England
• PMID: 16112579 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)

Chemical References

• Xanthones
• mangostin

Topics

• Apoptosis (drug effects)
• Cell Cycle (drug effects)
• Cell Line, Tumor
• Cell Proliferation (drug effects)
• Colonic Neoplasms (pathology)
• G1 Phase (drug effects)
• Humans
• Molecular Structure
• S Phase (drug effects)
• Xanthones (chemistry, pharmacology)