Growth Inhibitory and Apoptosis-inducing Effects of Xanthohumol, a Prenylated Chalone Present in Hops, in Human Prostate Cancer Cells

Promotion of apoptosis in cancer cells could potentially lead to the regression and improved prognosis of hormone-refractory prostate cancer. Xanthohumol (XN), a prenylated chalcone-derived from hops, has shown strong antitumorigenic activity towards diverse types of cancer cells. In the present stu...

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Bibliographic Details
Published in:Anticancer research 2010-09, Vol.30 (9), p.3333-3339
Main Authors: DEEB, D, GAO, X, JIANG, H, ARBAB, A. S, DULCHAVSKY, S. A, GAUTAM, S. C
Format: Article
Language:English
Subjects:
Antineoplastic Agents - pharmacology
Apoptosis - drug effects
Biological and medical sciences
Blotting, Western
Cell Line, Tumor
Cell Proliferation - drug effects
Flavonoids - pharmacology
Humans
Humulus - chemistry
Male
Medical sciences
Membrane Potential, Mitochondrial - drug effects
Nephrology. Urinary tract diseases
Phytotherapy - methods
Plant Extracts - pharmacology
Propiophenones - pharmacology
Prostatic Neoplasms - metabolism
Signal Transduction - drug effects
Tumors
Tumors of the urinary system
Urinary tract. Prostate gland
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Summary:Promotion of apoptosis in cancer cells could potentially lead to the regression and improved prognosis of hormone-refractory prostate cancer. Xanthohumol (XN), a prenylated chalcone-derived from hops, has shown strong antitumorigenic activity towards diverse types of cancer cells. In the present study, the growth-inhibitory and apoptosis-inducing activity of XN was tested in hormone-sensitive and hormone-refractory human prostate cancer cells lines. Cell growth/viability assay (MTS) demonstrated that prostate cancer cells are highly sensitive to XN at a concentration range of 20-40 μM. The primary mode of tumor cell destruction was apoptosis as demonstrated by the binding of annexin V-FITC, cleavage of PARP-1, activation of procaspases -3, -8, and -9, mitochondrial depolarization and release of cytochrome c from mitochondria. Induction of apoptosis by XN was associated with the inhibition of prosurvival Akt, NF-κB and mTOR signaling proteins and NF-κB-regulated anti-apoptotic Bcl-2 and survivin. These studies provide a rationale for clinical evaluation of XN for the treatment of hormone-refractory metastatic prostate cancer.
ISSN:0250-7005
1791-7530