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Effect of anti-histone acetyltransferase activity from Rosa rugosa Thunb. (Rosaceae) extracts on androgen receptor-mediated transcriptional regulation

 Yoo-Hyun Lee  ;  Myung Gu Jung  ;  Hee Bum Kang  ;  Kyung-Chul Choi  ;  Seungjoo Haam  ;  Woojin Jun  ;  Young-Jun Kim  ;  Hong Yon Cho  ;  Ho-Geun Yoon 
 JOURNAL OF ETHNOPHARMACOLOGY, Vol.118(3) : 412-417, 2008 
Journal Title
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Apoptosis/drug effects ; Cell Line, Tumor ; Enzyme Inhibitors/pharmacology* ; Female ; Histone Acetyltransferases/antagonists & inhibitors* ; Humans ; Male ; Plant Extracts/pharmacology* ; Prostatic Neoplasms/drug therapy ; Prostatic Neoplasms/pathology ; Receptors, Androgen/physiology* ; Rosa*/chemistry ; Transcription, Genetic
Rosa rugosa Thunb. ; Histone acetyltransferase ; Androgen receptor ; Prostate cancer
ETHNOPHARMACOLOGICAL RELEVANCE: Rosa rugosa Thunb. (Rosaceae) has been traditionally used for treatments of diabetes, chronic inflammatory diseases, pain, and anticancer in Korea. AIM OF STUDY: We investigate the inhibitory effect of histone acetyltransferase activity from the methanol extract of stems of Rosa rugosa on androgen receptor-mediated transcriptional regulation. MATERIALS AND METHODS: For the present study, Rosa rugosa methanol extract (RRME) was obtained from stem part of Rosa rugosa using methanol extraction. Histone acetyltransferase assay were performed to measure the inhibitory effect on acetylation, reporter assay, real-time PCR and ChIP assay were performed to measure androgen receptor-mediated transcriptional regulation, and MTT test were performed to measure cell viability. RESULTS: RRME inhibited both p300 and CBP (60-70% at 100 microg/ml) activity. We show RRME mediates agonist-dependent androgen receptor (AR) activation and suppresses antagonist-dependent inhibition. RRME treatment also decreased transcription of AR regulated genes and also reduced histone H3 and AR acetylation in the promoters of prostate-specific antigen (PSA) and beta-2-microglobulin (B2M). Finally, RRME treatment reduced the growth of LNCaP, a human prostate cancer cell line. CONCLUSION: These results demonstrate RRME is a potent HAT inhibitor, which reduced AR and histone acetylation leading to decreased AR-mediated transcription and reduced LNCaP cell growth.
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1. College of Medicine (의과대학) > Dept. of Biochemistry and Molecular Biology (생화학-분자생물학교실) > 1. Journal Papers
1. College of Medicine (의과대학) > Medical Research Center (임상의학연구센터) > 1. Journal Papers
Yonsei Authors
Kang, Hee Bum(강희범)
Yoon, Ho Geun(윤호근) ORCID logo https://orcid.org/0000-0003-2718-3372
Jun, Woo Jin(전우진)
Choi, Kyung Chul(최경철)
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