The objective of this study was to evaluate the chemopreventive effect of a novel
flavonoid,
ampelopsin (
AMP) on the growth and
metastasis of
prostate cancer cells.
AMP showed the more potent activity in inhibiting the proliferation of
androgen-sensitive LNCaP and, to less extent,
androgen-independent PC-3 human
prostate cancer cell lines in vitro, primarily by induction of apoptosis associated with down-regulation of bcl-2. On the other hand,
AMP showed much less activity in inhibiting the proliferation of normal prostate epithelial cells than that of
prostate cancer cell lines.
AMP also inhibited the migration and invasion of PC-3 cells in vitro associated with down-regulation of CXCR4 expression. In the animal study using an orthotopic prostate
tumor model,
AMP (150 and 300 mg/kg
body weight) inhibited the growth of PC-3
tumors and lymph node and lung
metastases in a dose-dependent manner. Compared to the control mice, mice treated with
AMP at 300 mg/kg BW had reduced final
tumor weight by 49.2% (P<0.05),
lymph node metastases by 54.5% (Pā=ā0.3) and lung
metastases by 93% (P<0.05), but had no apparent alteration on food intake or
body weight. The in vivo anti-growth and anti-
metastasis activities of
AMP were associated with induction of apoptosis and inhibition of proliferation of
prostate cancer cells, reduction of prostate
tumor angiogenesis, and reduction of CXCR4 expression. Our results provide supporting evidence to warrant further investigation to develop
AMP as a novel efficacious and safe candidate agent against progression and
metastasis of
prostate cancer.