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  • EGCG suppresses prostate cancer cell growth modulating acetylation of androgen receptor by anti-histone acetyltransferase activity.

EGCG suppresses prostate cancer cell growth modulating acetylation of androgen receptor by anti-histone acetyltransferase activity.

International journal of molecular medicine (2012-04-17)
Yoo-Hyun Lee, Jieun Kwak, Hyo-Kyoung Choi, Kyung-Chul Choi, Sunoh Kim, Jeongmin Lee, Woojin Jun, Hyun-Jin Park, Ho-Geun Yoon
ABSTRACT

Manipulating acetylation status of key gene targets is likely to be crucial for effective cancer therapy. In this study, we utilized green tea catechins, epicatechin (EC), epigallocatechin (EGC) and epigallocatechin-3-gallate (EGCG) to examine the regulation of androgen receptor acetylation in androgen-dependent prostate cancer cells by histone acetyl-transferase (HAT) activity. EC, EGC and EGCG induced prostate cancer cell death, suppressed agonist-dependent androgen receptor (AR) activation and AR-regulated gene transcription. These results demonstrated a similar tendency to HAT inhibitory activities; EGCG>EGC>EC. The strongest HAT inhibitor among them, EGCG (50 µM), downregulated AR acetylation and finally, AR protein translocation to nucleus from the cytoplasmic compartment was effectively inhibited in the presence of the agonist. These results suggest another mechanism to develop effective therapeutics based on green tea catechins.

MATERIALS
Product Number
Brand
Product Description

Sigma-Aldrich
(−)-Gallocatechin, ≥98% (HPLC)
Supelco
(−)-Gallocatechin, analytical standard
Sigma-Aldrich
(−)-Epigallocatechin, ≥95% (HPLC), from green tea
Epigallocatechin, primary reference standard
Supelco
(−)-Epigallocatechin, analytical standard