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Anti-Cancer Effects of Xanthones from Pericarps of Mangosteen
Gifu International Institute of Biotechnology, 1-1 Naka-Fudogaoka, Kakamigahara, Gifu 504-0838, Japan
* Author to whom correspondence should be addressed.
Received: 10 January 2008; in revised form: 13 February 2008 / Accepted: 15 February 2008 / Published: 14 March 2008
Abstract: Mangosteen, Garcinia mangostana Linn, is a tree found in South East Asia, and its pericarps have been used as traditional medicine. Phytochemical studies have shown that they contain a variety of secondary metabolites, such as oxygenated and prenylated xanthones. Recent studies revealed that these xanthones exhibited a variety of biological activities containing anti-inflammatory, anti-bacterial, and anti-cancer effects. We previously investigated the anti-proliferative effects of four prenylated xanthones from the pericarps; α-mangostin, β-mangostin, γ-mangostin, and methoxy-β-mangostin in various human cancer cells. These xanthones are different in the number of hydroxyl and methoxy groups. Except for methoxy-β-mangostin, the other three xanthones strongly inhibited cell growth at low concentrations from 5 to 20 μM in human colon cancer DLD-1 cells. Our recent study focused on the mechanism of α-mangostin-induced growth inhibition in DLD-1 cells. It was shown that the anti-proliferative effects of the xanthones were associated with cell-cycle arrest by affecting the expression of cyclins, cdc2, and p27; G1 arrest by α- mangostin and β-mangostin, and S arrest by γ-mangostin. α-Mangostin found to induce apoptosis through the activation of intrinsic pathway following the down-regulation of signaling cascades involving MAP kinases and the serine/threonine kinase Akt. Synergistic effects by the combined treatment of α-mangostin and anti-cancer drug 5-FU was to be noted. α-Mangostin was found to have a cancer preventive effect in rat carcinogenesis bioassay and the extract from pericarps, which contains mainly α-mangostin and γ- mangostin, exhibited an enhancement of NK cell activity in a mouse model. These findings could provide a relevant basis for the development of xanthones as an agent for cancer prevention and the combination therapy with anti-cancer drugs.
Keywords: anti-cancer effect; Xanthones; apoptosis; α-mangostin
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MDPI and ACS Style
Akao, Y.; Nakagawa, Y.; Nozawa, Y. Anti-Cancer Effects of Xanthones from Pericarps of Mangosteen. Int. J. Mol. Sci. 2008, 9, 355-370.
Akao Y, Nakagawa Y, Nozawa Y. Anti-Cancer Effects of Xanthones from Pericarps of Mangosteen. International Journal of Molecular Sciences. 2008; 9(3):355-370.
Akao, Yukihiro; Nakagawa, Yoshihito; Nozawa, Yoshinori. 2008. "Anti-Cancer Effects of Xanthones from Pericarps of Mangosteen." Int. J. Mol. Sci. 9, no. 3: 355-370.