Abstract |
Hinokitiol ( beta-thujaplicin), a troplone-related compound found in the heartwood of cupressaceous plants, strongly inhibits the proliferation of a broad range of tumor cell lines. This is the first report to demonstrate that hinokitiol, a metal chelator derived from natural plants, suppresses cell growth and disrupts AR signaling in prostate carcinoma cell lines. Our present studies indicate that hinokitiol suppresses androgen/AR-mediated cell growth and androgen-stimulated DNA synthesis by [(3)H] thymidine incorporation in a dose- and time-dependent manner. Hinokitiol simultaneously suppresses the intracellular and secreted PSA levels, a marker for the progression of prostate cancer. Hinokitiol significantly represses the AR mRNA and protein expression in a dose- and time-dependent manner. Additionally, the ligand-binding assay shows that hinokitiol blocks binding of the synthetic androgen [(3)H] R1881 to AR in LNCaP cells. These findings collectively suggest that hinokitiol is potentially effective against prostate cancer in vitro, and thus it might become a novel chemopreventive or chemotherapeutic agent for prostate cancer.
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Authors | Shicheng Liu, Hitoshi Yamauchi |
Journal | Biochemical and biophysical research communications
(Biochem Biophys Res Commun)
Vol. 351
Issue 1
Pg. 26-32
(Dec 08 2006)
ISSN: 0006-291X [Print] United States |
PMID | 17055455
(Publication Type: Journal Article)
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Chemical References |
- Androgens
- Chelating Agents
- Metals
- Monoterpenes
- Plant Extracts
- Receptors, Androgen
- Tropolone
- Prostate-Specific Antigen
- beta-thujaplicin
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Topics |
- Androgens
(metabolism)
- Apoptosis
(drug effects)
- Cell Line, Tumor
- Cell Proliferation
(drug effects)
- Chelating Agents
(administration & dosage)
- Humans
- Male
- Metals
(administration & dosage)
- Monoterpenes
(administration & dosage)
- Plant Extracts
(administration & dosage)
- Prostate-Specific Antigen
(metabolism)
- Prostatic Neoplasms
(metabolism, pathology)
- Receptors, Androgen
(metabolism)
- Signal Transduction
(drug effects)
- Tropolone
(administration & dosage, analogs & derivatives)
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