Anti‐Histone Acetyltransferase Activity from Ampelopsis Radix Extracts Inhibits Androgen Receptor‐Dependent Prostate Cancer Cell Growth

Histone acetylation depends on the activity of two enzyme families, histone acetyltransferase (HAT) and deacetylase (HDAC). In this study, we screened various plant extracts to find potent HAT inhibitors. Hot water extracts of Ampelopsis Radix inhibited HAT activity, especially p300 and CBP (40% at 100 μg/ml). The mRNA levels of two androgen receptor (AR) regulated genes, PSA and TSC22, decreased with Ampelopsis Radix treatment (100 μg/ml). Importantly, in IP western analysis, AR acetylation was dramatically decreased by Ampelopsis Radix treatment. Furthermore, chromatin immunoprecipitation indicated that the acetylation of histone H3 in the PSA and B2M promoter regions was also repressed. Finally, Ampelopsis Radix treatment reduced the growth of human prostate cancer cells, LNCaP (50% growth inhibition at 200 μg/ml). Taken together, our data indicate that the potent HAT inhibitory activity of allspice reduced AR and histone acetylation and led to decreased transcription of AR target genes, resulting in inhibition of prostate cancer cell growth. This work was supported by the Korea Science and Engineering Foundation (KOSEF) grant funded by the Korea gorvenment (MOST) (No. R13‐2002‐054‐04002‐0); a grant (code #20070301034007) from BioGreen 21 program, Rural Development Administration, Republic of Korea.