Xanthorrhizol is a natural
sesquiterpenoid compound isolated from the rhizome of Curcuma xanthorrhiza Roxb (Zingiberaceae).
Xanthorrhizol was tested for a variety of important pharmacological activities including
antioxidant and anti-inflammatory activities. An antiproliferation assay using the MTT method indicated that
xanthorrhizol inhibited the proliferation of the human
breast cancer cell line, MCF-7, with an EC50 value of 1.71 microg/ml. Three parameters including
annexin-V binding assay,
Hoechst 33258 staining and accumulation of sub-G1 population in
DNA histogram confirmed the apoptosis induction in response to
xanthorrhizol treatment. Western-blotting revealed down-regulation of the anti-apoptotic bcl-2
protein expression. However,
xanthorrhizol did not affect the expression of the
pro-apoptotic protein, bax, at a concentration of 1 microg/ml, 2.5 microg/ml and 5 microg/ml. The level of p53 was greatly increased, whilst PARP-1 was cleaved to 85 kDa subunits, following the treatment with
xanthorrhizol at a dose-dependent manner. These results, thereby, suggest that
xanthorrhizol has antiproliferative effects on MCF-7 cells by inducing apoptosis through the modulation of bcl-2, p53 and
PARP-1 protein levels.