In the present study, we investigated the growth inhibitory effect of 5-acetyloxy-6,7,8,4'-tetramethoxyflavone (5-ATAN), an acetylated derivative of tangeretin (TAN), on human prostate cancer PC-3 cells.  The results showed that 5-ATAN revealed stronger cytotoxic effects than that of TAN on cell viability of PC-3 cells. After 48 h treatment, the IC<sub>50</sub> of 5-ATAN and TAN were determined as 5.2 and 25.9 µM, respectively. Moreover, treatment of 5-ATAN increased the sub-G1 phase population and induced G2/M phase arrest in the cell cycle of PC-3 cells. We also found that 5-ATAN triggered the activation of caspase-8, -9 and -3 and disrupted mitochondrial membrane potential in PC-3 cells, suggesting induction of apoptosis. In cell wound healing test, 5-ATAN decreased the cell migration dose-dependently. Overall, we infer the mechanism of cell growth inhibition of 5-ATAN in human prostate cancer PC-3 cells may due to induction of the cell cycle arrest and apoptosis that can be regarded as a potentially useful agent for the treatment and prevention of human prostate cancer.

5-Acetyloxy-6,7,8,4'-tetramethoxyflavone, a tangeretin derivative, inhibits cell growth in human prostate cancer PC-3 cells

250th National Meeting (2015)

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