Document Detail

Guggulsterone suppresses bile acid-induced and constitutive caudal-related homeobox 2 expression in gut-derived adenocarcinoma cells.
MedLine Citation:
PMID:  20651339     Owner:  NLM     Status:  MEDLINE    
BACKGROUND: Guggulsterone, a plant polyphenol guggulipid, has several antitumour effects and acts as an antagonist for the farnesoid X receptor. Although bile acids induce caudal-related homeobox 2 (CdX2), a transcription factor essential for intestinal development and gut tumourigenesis, the effects of guggulsterone on regulation of CdX2 in the gut are unknown. MATERIALS AND METHODS: Regulation of CdX2 expression by treatment with bile acids and/or guggulsterone was analysed by immunoblot analysis in human gut-derived adenocarcinoma, Bic-1 cells. Nuclear factor-kappaB (NF-kappaB) activity and the cell cycle distribution were also examined. RESULTS: Chenodeoxycholic acid and deoxycholic acid increased CdX2 expression in Bic-1 cells. Guggulsterone reduced bile acid-induced and constitutive CdX2 expression at 5 microM. Guggulsterone (up to 5 microM) did not affect cell viability or the cell cycle and did not attenuate bile acid-induced or constitutive NF-kappaB activation. CONCLUSION: Guggulsterone may be used as a novel drug to target CdX2 expression in certain gut adenocarcinomas.
Takanori Yamada; Satoshi Osawa; Yasushi Hamaya; Takahisa Furuta; Akira Hishida; Masayoshi Kajimura; Mutsuhiro Ikuma
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Publication Detail:
Type:  Journal Article; Research Support, Non-U.S. Gov't    
Journal Detail:
Title:  Anticancer research     Volume:  30     ISSN:  1791-7530     ISO Abbreviation:  Anticancer Res.     Publication Date:  2010 Jun 
Date Detail:
Created Date:  2010-07-23     Completed Date:  2010-08-24     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  8102988     Medline TA:  Anticancer Res     Country:  Greece    
Other Details:
Languages:  eng     Pagination:  1953-60     Citation Subset:  IM    
First Department of Medicine, Hamamatsu University School of Medicine, 1-20-1 Handayama, Higashi-ku, Hamamatsu 431-3192, Japan.
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MeSH Terms
Adenocarcinoma / drug therapy*,  pathology
Antineoplastic Agents, Phytogenic / pharmacology*
Apoptosis / drug effects
Bile Acids and Salts / antagonists & inhibitors*
Cell Cycle / drug effects
Cell Line, Tumor
Cell Survival / drug effects
Homeodomain Proteins / antagonists & inhibitors*
Intestinal Neoplasms / drug therapy*,  pathology
NF-kappa B / antagonists & inhibitors,  metabolism
Pregnenediones / pharmacology*
Receptors, Cytoplasmic and Nuclear / antagonists & inhibitors*
Reg. No./Substance:
0/Antineoplastic Agents, Phytogenic; 0/Bile Acids and Salts; 0/CDX2 protein, human; 0/Homeodomain Proteins; 0/NF-kappa B; 0/Pregnenediones; 0/Receptors, Cytoplasmic and Nuclear; 0/farnesoid X-activated receptor; 95975-55-6/pregna-4,17-diene-3,16-dione

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