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Histone acetyltransferase inhibitory activity of Bokbunja (Rubus coreanus Miq.) ethanol extract on androgen receptor-dependent prostate cancer cell growth

Authors
 Mi-Jeong Kim  ;  Ah-Reum Seong  ;  Yoo-Hyun Lee  ;  Young Jun Kim  ;  Masaki Shiota  ;  Akira Yokomizo  ;  Seiji Naito  ;  Jeongmin Lee  ;  Woojin Jun  ;  Ho-Geun Yoon 
Citation
 FOOD SCIENCE AND BIOTECHNOLOGY, Vol.19(6) : 1503-1511, 2010 
Journal Title
 FOOD SCIENCE AND BIOTECHNOLOGY 
ISSN
 1226-7708 
Issue Date
2010
Keywords
bokbunja ; Rubus coreanus ; histone acetyltransferase ; androgen receptor ; prostate cancer
Abstract
In this study, we demonstrate that a bokbunja (Rubus coreanus) ethanol extract (RCE) exhibits the strong histone acetyltransferase (HAT) inhibitory activity, and shows specificity against the p300 HAT enzyme. RCE specifically inhibited p300 acetyltransferase activities with an IC50 of approximately 70 μg/mL, but did not inhibit other epigenetic enzymes. We found that RCE inhibited agonist-dependent androgen receptor (AR) acetylation and suppressed androgen-induced AR transcriptional activity. RCE treatment also decreased the enhancement of AR transcriptional activity caused by p300 overexpression, and combined treatment with RCE potentiated the activity of the AR antagonist flutamide. Finally, RCE treatment reduced the growth of LNCaP human prostate cancer cells via inhibition of cyclin D1 and cyclin E expression, and concomitantly induced apoptosis. Collectively, our results suggest that therapeutic targeting of AR acetylation by HATi could lead to a new class of antagonists for the treatment of prostate cancer
Full Text
http://link.springer.com/article/10.1007%2Fs10068-010-0214-8#
DOI
10.1007/s10068-010-0214-8
Appears in Collections:
1. College of Medicine (의과대학) > Dept. of Biochemistry and Molecular Biology (생화학-분자생물학교실) > 1. Journal Papers
Yonsei Authors
Kim, Mi Jeong(김미정) ORCID logo https://orcid.org/0000-0002-0758-7145
Yoon, Ho Geun(윤호근) ORCID logo https://orcid.org/0000-0003-2718-3372
URI
https://ir.ymlib.yonsei.ac.kr/handle/22282913/102704
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