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Xanthohumol, a prenylflavonoid derived from hops induces apoptosis and inhibits NF-κB activation in prostate epithelial cells

Department of Nutrition and Exercise Sciences, Oregon State University, Corvallis, OR 97331, USA.
Cancer Letters (Impact Factor: 5.62). 03/2007; 246(1-2):201-9. DOI: 10.1016/j.canlet.2006.02.015
Source: PubMed

ABSTRACT

There is increasing evidence that certain natural compounds found in plants may be useful as cancer chemopreventive or chemotherapeutic agents. Limited in vitro studies indicate that several prenylated flavonoids present in the hop plant (Humulus lupulus) possess anticarcinogenic properties. The purpose of this study was to investigate the anti-tumorigenic effects of xanthohumol (XN), the major prenylflavonoid in hops, on prostate cancer and benign prostate hyperplasia. BPH-1 and PC3 cell lines were used in our study to represent both non-tumorigenic hyperplasia and malignant prostate cancer. In both BPH-1 and PC3 cells, XN and its oxidation product, XAL, decreased cell viability in a dose dependent manner (2.5-20 microM) as determined by MTT assay and caused an increase in the formation of early and late apoptotic cells as determined by Annexin V staining and multicaspase assays. XN and its oxygenated derivative also induced cell cycle changes in both cells lines, seen in an elevated sub G1 peak at 48h treatment. Western blot analysis was performed to confirm the activation of proapoptotic proteins, Bax and p53. XN and its derivative caused decreased activation of NFkappaB. This work suggests that XN and its oxidation product, XAL, may be potentially useful as a chemopreventive agent during prostate hyperplasia and prostate carcinogenesis, acting via induction of apoptosis and down-regulation of NFkappaB activation in BPH-1 cells.

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    • "Furthermore, the xanthohumol and other prenylflavonoids, such as 8-prenylnaringenin, inhibit selectively the activation of NF-kB. In fact, Colgate and co-workers demonstrated that the xanthohumol inhibits the NF-kB production in prostate epithelial cell line[87]. In particular, the NF-kB activity decreased significantly (42%) by using a xanthohumol concentration of 20 mM[86e88]. "
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    • "Moreover, pro-apoptotic activity of XN has also been observed in human breast cancer [47], prostate cancer [7], B-chronic lymphocytic leukemia [32], and malignant glioblastoma cells [18]. Besides these effects, it has been reported as a strong inhibitor of migration, invasion, and angiogenesis in hematological malignancies [11] [36]. "

    Full-text · Dataset · Aug 2015
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    • "Moreover, pro-apoptotic activity of XN has also been observed in human breast cancer [47], prostate cancer [7], B-chronic lymphocytic leukemia [32], and malignant glioblastoma cells [18]. Besides these effects, it has been reported as a strong inhibitor of migration, invasion, and angiogenesis in hematological malignancies [11] [36]. "
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    ABSTRACT: Xanthohumol (XN), a prenylflavonoid derived from the hop plant (Humulus lupulus L.) has been found to exhibit a broad spectrum of biological properties, including anti-cancer activity. In this study, the mechanisms involved in anti-cancer activity of XN in human RK33 and RK45 larynx cancer cell lines were investigated. The effect of XN on the viability of larynx cancer and normal cells (human skin fibroblasts HSF and rat oligodendroglia-derived cells, OLN-93) was compared. Additionally, the influence of XN on proliferation, cell cycle progression, induction of apoptosis in larynx cancer cells, as well as the molecular mechanisms underlying in these processes were analyzed. XN promoted the reduction of cell viability in cancer cells, but showed low cytotoxicity to normal cells. The decrease in cell viability in the cancer cells was coupled with induction of apoptosis via two pathways. The mechanisms involved in these effects of XN were associated with cell growth inhibition by induction of cell cycle arrest in the G1 phase, increased p53 and p21/WAF1 expression levels, downregulation of cyclin D1 and Bcl-2, and activation of caspases-9, -8, and -3. Moreover, this compound inhibited phosphorylation of ERK1/2, suggesting a key role of the ERKs pathway in the XN-mediated growth suppressing effects against the studied cells. These results indicate that XN could be used as a potential agent for the treatment of patients with larynx cancer. Copyright © 2015. Published by Elsevier Ireland Ltd.
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