ArticleInternational journal of cancer2010
Flavokawain B, a kava chalcone, induces apoptosis via up-regulation of death-receptor 5 and Bim expression in androgen receptor negative, hormonal refractory prostate cancer cell lines and reduces tumor growth.
Article in International journal of cancer, 2010. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 42 papers.
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Who cites it
42 citing papers in PubMed, 91 citations in OpenAlex.
- Review
- The Role of Natural Chalcones and Their Derivatives in Targeting Prostate Cancer: Recent Updates.International journal of molecular sciences · 2025Review
- Searching for Natural Aurora a Kinase Inhibitors from Peppers Using Molecular Docking and Molecular Dynamics.Pharmaceuticals (Basel, Switzerland) · 2023Article
- Anticancer Potential of Natural Chalcones: In Vitro and In Vivo Evidence.International journal of molecular sciences · 2023Review
- Core Structure-Activity Relationship Studies of 5,7,20-Pharmaceuticals (Basel, Switzerland) · 2023Article
- Pharmacological Small Molecules against Prostate Cancer by Enhancing Function of Death Receptor 5.Pharmaceuticals (Basel, Switzerland) · 2022Review
- Flavokawain A Reduces Tumor-Initiating Properties and Stemness of Prostate Cancer.Frontiers in oncology · 2022Article
- Peppers: A "Hot" Natural Source for Antitumor Compounds.Molecules (Basel, Switzerland) · 2021Review
- Molecular Basis of Prostate Cancer and Natural Products as Potential Chemotherapeutic and Chemopreventive Agents.Frontiers in pharmacology · 2021Review
- Kava constituents exert selective anticancer effects in oral squamous cell carcinoma cells in vitro.Scientific reports · 2020Article
- Review
- Flavokawain B targets protein neddylation for enhancing the anti-prostate cancer effect of Bortezomib via Skp2 degradation.Cell communication and signaling : CCS · 2019Article
- Down-regulation of Skp2 expression inhibits invasion and lung metastasis in osteosarcoma.Scientific reports · 2018Article
- (-)-Gochnatiolide B, synthesized from dehydrocostuslactone, exhibits potent anti-bladder cancer activity in vitro and in vivo.Scientific reports · 2018Article
- Restoring TRAIL Induced Apoptosis Using Naturopathy. Hercules Joins Hand with Nature to Triumph Over Lernaean Hydra.Current genomics · 2017Review
- Physapubescin selectively induces apoptosis in VHL-null renal cell carcinoma cells through down-regulation of HIF-2α and inhibits tumor growth.Scientific reports · 2016Article
- Flavokawains A and B from kava (Piper methysticum) activate heat shock and antioxidant responses and protect against hydrogen peroxide-induced cell death in HepG2 hepatocytes.Pharmaceutical biology · 2016Article
- Flavokawain B induced cytotoxicity in two breast cancer cell lines, MCF-7 and MDA-MB231 and inhibited the metastatic potential of MDA-MB231 via the regulation of several tyrosine kinases In vitro.BMC complementary and alternative medicine · 2016Article
- New withanolides with TRAIL-sensitizing effect fromRSC advances · 2016Article
- In vivo antitumor and antimetastatic effects of flavokawain B in 4T1 breast cancer cell-challenged mice.Drug design, development and therapy · 2015Article
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Authors and funding
6 authors at 2 institutions in 1 country.
Funding
Abstract
Limited success has been achieved in extending the survival of patients with metastatic and hormone-refractory prostate cancer (HRPC). There is a strong need for novel agents in the treatment and prevention of HRPC. We have shown that flavokawain B (FKB), a kava chalcone, is about 4- to 12-fold more effective in reducing the cell viabilities of androgen receptor (AR)-negative, HRPC cell lines DU145 and PC-3 than AR-positive, hormone-sensitive prostate cancer cell lines LAPC4 and LNCaP, with minimal effect on normal prostatic epithelial and stromal cells. FKB induces apoptosis with an associated increased expression of proapoptotic proteins: death receptor-5, Bim and Puma and a decreased expression of inhibitors of apoptosis protein: XIAP and survivin. Among them, Bim expression was significantly induced by FKB as early as 4 hr of the treatment. Knockdown of Bim expression by short-hairpin RNAs attenuates the inhibitory effect on anchorage-dependent and -independent growth and caspase cleavages induced by FKB. These findings suggest that the effect of FKB, at least in part, requires Bim expression. In addition, FKB synergizes with TRAIL for markedly enhanced induction of apoptosis. Furthermore, FKB treatment of mice bearing DU145 xenograft tumors results in tumor growth inhibition and increases Bim expression in tumor tissues. Together, these results suggest robust mechanisms for FKB induction of apoptosis preferentially for HRPC and the potential usefulness of FKB for prevention and treatment of HRPC in an adjuvant setting.
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