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 |
|
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)
|