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Grape seed extract regulates androgen receptor-mediated transcription in prostate cancer cells through potent anti-histone acetyltransferase activity.

Authors
 Si Yong Park  ;  Yoo-Hyun Lee  ;  Kyung-Chul Choi  ;  Ah-Reum Seong  ;  Hyo-Kyoung Choi  ;  Ok-Hee Lee  ;  Han-Joon Hwang  ;  Ho-Geun Yoon 
Citation
 Journal of Medicinal Food, Vol.14(1-2) : 9-16, 2011 
Journal Title
 Journal of Medicinal Food 
ISSN
 1096-620X 
Issue Date
2011
Abstract
Histone acetylation, which is regulated by histone acetyltransferases (HATs) and deacetylases, is an epigenetic mechanism that influences eukaryotic transcription. Significant changes in histone acetylation are associated with cancer; therefore, manipulating the acetylation status of key gene targets is likely crucial for effective cancer therapy. Grape seed extract (GSE) has a known protective effect against prostate cancer. Here, we showed that GSE significantly inhibited HAT activity by 30-80% in vitro (P < .05). Furthermore, we demonstrated significant repression of androgen receptor (AR)-mediated transcription by GSE in prostate cancer cells by measuring luciferase activity using a pGL3-PSA construct bearing the AR element in the human prostate cancer cell line LNCaP (P < .05). GSE treatment also decreased the mRNA level of the AR-regulated genes PSA and NKX 3.1. Finally, GSE inhibited growth of LNCaP cells. These results indicate that GSE potently inhibits HAT, leading to decreased AR-mediated transcription and cancer cell growth, and implicate GSE as a novel candidate for therapeutic activity against prostate cancer.
URI
https://ir.ymlib.yonsei.ac.kr/handle/22282913/92851
DOI
10.1089/jmf.2010.1264
Appears in Collections:
1. Journal Papers (연구논문) > 1. College of Medicine (의과대학) > Dept. of Biochemistry and Molecular Biology (생화학-분자생물학교실)
1. Journal Papers (연구논문) > 1. College of Medicine (의과대학) > BioMedical Science Institute (의생명과학부)
1. Journal Papers (연구논문) > 5. Research Institutes (연구소) > Yonsei Integrative Research Institute for Cerebral & Cardiovascular Disease (뇌심혈관질환융합연구사업단)
Yonsei Authors
윤호근(Yoon, Ho Geun) ; 이옥희(Lee, Ok Hee) ; 최경철(Choi, Kyung Chul)
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Full Text
http://online.liebertpub.com/doi/abs/10.1089/jmf.2010.1264
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