Xanthohumol from hops prevents hormone-dependent tumourigenesis in vitro and in vivo

Acta Horticulturae

Volumn 848, Issue , 2009, Pages 179-190

  Strathmann, J ^a   Bertl, E ^a   Hussong, R ^a   Klimo, K ^a   Steinle, R ^a   Frank, N ^a   Gerhauser, C ^a  

^a GERMAN CANCER RESEARCH CENTER DKFZ   (Germany)

Author keywords

Anti estrogenic; Antiangiogenic; Cancer chemoprevention; DMBA induced mammary carcinogenesis; Humulus lupulus L.; Rat uterotrophic assay

Indexed keywords

HUMULUS; HUMULUS LUPULUS; MUS; RATTUS;

EID: 75649107252     PISSN: 05677572     EISSN: None     Source Type: Book Series    
DOI: 10.17660/ActaHortic.2009.848.20     Document Type: Conference Paper

References (52)

1. Albini, A., Dell'eva, R., Vene, R., Ferrari, N., Buhler, D. R., Noonan, D. M. and Fassina, G. 2006. Mechanisms of the antiangiogenic activity by the hop flavonoid xanthohumol: NF-κB and Akt as targets. FASEB J. 20:527-529.
2. Bertl, E., Klimo, K., Heiss, E., Klenke, F., Peschke, P., Becker, H., Eicher, T., Herhaus, C., Kapadia, G., Bartsch, H. and Gerhauser, C. 2004. Identification of novel inhibitors of angiogenesis using a human in vitro anti-angiogenesis assay. Int. J. Cancer Prev. 1:47-61.
3. Bertl, E. 2005. Inhibition of angiogenesis by potential cancer chemopreventive agents - Establishment of a human in vitro anti-angiogenesis assay and mechanistic evaluation of potent inhibitors. Ph. D. Thesis, University of Heidelberg.
4. Bertl, E., Bartsch, H. and Gerhauser, C. 2006. Inhibition of angiogenesis and endothelial cell functions are novel sulforaphane-mediated mechanisms in chemoprevention. Mol. Cancer Ther. 5:575-585.
5. Berwanger, S., Frank, N., Knauft, J. and Becker, H. 2005. Biosynthetic (14) C-labelling of xanthohumol in hop cones. Mol. Nutr. Food Res. 49:857-860.
6. Carmeliet, P. and Jain, R. K. 2000. Angiogenesis in cancer and other diseases. Nature 407:249-257.
7. Cavalieri, E., Chakravarti, D., Guttenplan, J., Hart, E., Ingle, J., Jankowiak, R., Muti, P., Rogan, E., Russo, J., Santen, R. and Sutter, T. 2006. Catechol estrogen quinones as initiators of breast and other human cancers: implications for biomarkers of susceptibility and cancer prevention. Biochim. Biophys. Acta. 1766:63-78.
8. Cho, Y. C., Kim, H. J., Kim, Y. J., Lee, K. Y., Choi, H. J., Lee, I. S. and Kang, B. Y. 2008. Differential anti-inflammatory pathway by xanthohumol in IFN-γ and LPS-activated macrophages. Int. Immunopharmacol. 8:567-573.
9. Colgate, E. C., Miranda, C. L., Stevens, J. F., Bray, T. M. and Ho, E. 2007. Xanthohumol, a prenylflavonoid derived from hops induces apoptosis and inhibits NF-κB activation in prostate epithelial cells. Cancer Lett. 246:201-209.
10. De Flora, S. and Ferguson, L. R. 2005. Overview of mechanisms of cancer chemopreventive agents. Mutat. Res. 591:8-15.
11. Dell'Eva, R., Ambrosini, C., Vannini, N., Piaggio, G., Albini, A. and Ferrari, N. 2007. AKT/NF-kappaB inhibitor xanthohumol targets cell growth and angiogenesis in hematologic malignancies. Cancer 110:2007-2011.
12. Delmulle, L., Berghe, T. V., Keukeleire, D. D. and Vandenabeele, P. 2008. Treatment of PC-3 and DU145 prostate cancer cells by prenylflavonoids from hop (Humulus lupulus L.) induces a caspase-independent form of cell death. Phytother. Res. 22:197-203.
13. Diel, P., Schulz, T., Smolnikar, K., Strunck, E., Vollmer, G. and Michna, H. 2000. Ability of xeno-and phytoestrogens to modulate expression of estrogen-sensitive genes in rat uterus: estrogenicity profiles and uterotropic activity. J. Steroid Biochem. Mol. Biol. 73:1-10.
14. Fokialakis, N., Lambrinidis, G., Mitsiou, D. J., Aligiannis, N., Mitakou, S., Skaltsounis, A. L., Pratsinis, H., Mikros, E. and Alexis, M. N. 2004. A new class of phytoestrogens; evaluation of the estrogenic activity of deoxybenzoins. Chem. Biol. 11:397-406.
15. Folkman, J. 1971. Tumor angiogenesis: therapeutic implications. N. Engl. J. Med. 285:1182-1186.
16. Gerhauser, C., Alt, A., Heiss, E., Gamal-Eldeen, A., Klimo, K., Knauft, J., Neumann, I., Scherf, H. R., Frank, N., Bartsch, H. and Becker, H. 2002a. Cancer chemopreventive activity of Xanthohumol, a natural product derived from hop. Mol. Cancer Ther. 1:959-969.
17. Gerhauser, C., Alt, A. P., Klimo, K., Knauft, J., Frank, N. and Becker, H. 2002b. Isolation and potential cancer chemopreventive activities of phenolic compounds of beer. Phytochem. Rev. 1:369-377.
18. Gerhauser, C., Klimo, K., Heiss, E., Neumann, I., Gamal-Eldeen, A., Knauft, J., Liu, G. Y., Sitthimonchai, S. and Frank, N. 2003. Mechanism-based in vitro screening of potential cancer chemopreventive agents. Mutat. Res. 523-524:163-172.
19. Gerhauser, C. 2005a. Beer constituents as potential cancer chemopreventive agents. Eur. J. Cancer 41:1941-1954.
20. Gerhauser, C. 2005b. Broad spectrum anti-infective potential of xanthohumol from hop (Humulus lupulus L.) in comparison with activities of other hop constituents and xanthohumol metabolites. Mol. Nutr. Food Res. 49:827-831.
21. Griekspoor, A., Zwart, W., Neefjes, J. and Michalides, R. 2007. Visualizing the action of steroid hormone receptors in living cells. Nucl. Recept. Signal. 5:e003.
22. Guerreiro, S., Monteiro, R., Martins, M. J., Calhau, C, Azevedo, I. and Soares, R. 2007. Distinct modulation of alkaline phosphatase isoenzymes by 17β-estradiol and xanthohumol in breast cancer MCF-7 cells. Clin. Biochem. 40:268-273.
23. Hanske, L., Hussong, R., Frank, N., Gerhauser, C, Blaut, M. and Braune, A. 2005. Xanthohumol does not affect the composition of rat intestinal microbiota. Mol. Nutr. Food Res. 49:868-873.
24. Harikumar, K. B., Kunnumakkara, A. B., Ahn, K. S., Anand, P., Krishnan, S., Guha, S. and Aggarwal, B. B. 2008. Modification of the cysteine residues in IκB α kinase and NF-κB (p65) by xanthohumol leads to suppression of NF-κB-regulated gene products and potentiation of apoptosis in leukemia cells. Blood (doi:10.1182/blood-2008-04-151944).
25. Ho, Y. C., Liu, C. H., Chen, C. N., Duan, K. J. and Lin, M. T. 2008. Inhibitory effects of xanthohumol from hops (Humulus lupulus L.) on human hepatocellular carcinoma cell lines. Phytother. Res. 22:1465-1468.
26. Hussong, R., Frank, N., Knauft, J., Ittrich, C, Owen, R., Becker, H. and Gerhauser, C. 2005. A safety study of oral xanthohumol administration and its influence on fertility in Sprague Dawley rats. Mol. Nutr. Food Res. 49:861-867.
27. Kac, J., Plazar, J., Mlinaric, A., Zegura, B., Lah, T. T. and Filipic, M. 2008. Antimutagenicity of hops (Humulus lupulus L.) : bioassay-directed fractionation and isolation of xanthohumol. Phytomedicine 15:216-220.
28. Khupse, R. S. and Erhardt, P. W. 2007. Total synthesis of xanthohumol. J. Nat. Prod. 70:1507-1509.
29. Klenke, F. M., Merkle, T., Fellenberg, J., Abdollahi, A., Huber, P. E., Gebhard, M. M., Ewerbeck, V. and Sckell, A. 2005. A novel model for the investigation of orthotopically growing primary and secondary bone tumours using intravital microscopy. Lab. Anim. 39:377-383.
30. Lee, S. H., Kim, H. J., Lee, J. S., Lee, IS. and Kang, B. Y. 2007. Inhibition of topoisomerase I activity and efflux drug transporters' expression by xanthohumol. From hops. Arch. Pharm. Res. 30:1435-1439.
31. Lust, S., Vanhoecke, B., Janssens, A., Philippe, J., Bracke, M. and Offner, F. 2005. Xanthohumol kills B-chronic lymphocytic leukemia cells by an apoptotic mechanism. Mol. Nutr. Food Res. 49:844-850.
32. Mendes, V., Monteiro, R., Pestana, D., Teixeira, D., Calhau, C. and Azevedo, I. 2008. Xanthohumol influences preadipocyte differentiation: implication of antiproliferative and apoptotic effects. J. Agric. Food Chem. 56:11631-11637.
33. Michel, S. 2005. Azoxymethane induced colon carcinogenesis in rats: influence of xanthohumol on early biomarkers for chemoprevention. Diploma thesis, University of Hohenheim.
34. Monteghirfo, S., Tosetti, F., Ambrosini, C., Stigliani, S., Pozzi, S., Frassoni, F., Fassina, G., Soverini, S., Albini, A. and Ferrari, N. 2008. Antileukemia effects of xanthohumol in Bcr/Abl-transformed cells involve nuclear factor-κB and p53 modulation. Mol. Cancer Ther. 7:2692-2702.
35. Monteiro, R., Becker, H., Azevedo, I. and Calhau, C. 2006. Effect of hop (Humulus lupulus L.) flavonoids on aromatase (estrogen synthase) activity. J. Agric. Food Chem. 54:2938-2943.
36. Monteiro, R., Calhau, C, Silva, A. O., Pinheiro-Silva, S., Guerreiro, S., Gartner, F., Azevedo, I. and Soares, R. 2008. Xanthohumol inhibits inflammatory factor production and angiogenesis in breast cancer xenografts. J. Cell. Biochem. 104:1699-1707.
37. Monteiro, R., Faria, A., Azevedo, I. and Calhau, C. 2007. Modulation of breast cancer cell survival by aromatase inhibiting hop (Humulus lupulus L.) flavonoids. J. Steroid Biochem. Mol. Biol. 105:124-130.
38. Nookandeh, A., Frank, N., Steiner, F., Ellinger, R., Schneider, B., Gerhauser, C. and Becker, H. 2004. Xanthohumol metabolites in faeces of rats. Phytochemistry 65:561-570.
39. Nozawa, H. 2005. Xanthohumol, the chalcone from beer hops (Humulus lupulus L.), is the ligand for farnesoid X receptor and ameliorates lipid and glucose metabolism in KK-A (y) mice. Biochem. Biophys. Res. Commun. 336:754-761.
40. Pan, L., Becker, H. and Gerhauser, C. 2005. Xanthohumol induces apoptosis in cultured 40-16 human colon cancer cells by activation of the death receptor-and mitochondrial pathway. Mol. Nutr. Food Res. 49:837-843.
41. Plazar, J., Filipic, M. and Groothuis, G. M. 2008. Antigenotoxic effect of Xanthohumol in rat liver slices. Toxicol. In Vitro 22:318-327.
42. Plazar, J., Zegura, B., Lah, T. T. and Filipic, M. 2007. Protective effects of xanthohumol against the genotoxicity of benzo (a) pyrene (BaP), 2-amino-3-methylimidazo[4, 5-f]quinoline (IQ) and tert-butyl hydroperoxide (t-BOOH) in HepG2 human hepatoma cells. Mutat. Res. 632:1-8.
43. Sckell, A. and Leunig, M. 1999. Dorsal skinfold chamber preparation in mice. Meth. Mol. Med. 46:95-105.
44. Sporn, M. B. and Newton, D. L. 1979. Chemoprevention of cancer with retinoids. Fed. Proc. 38:2528-2534.
45. Stresser, D. M., Turner, S. D., McNamara, J., Stocker, P., Miller, V. P., Crespi, C. L. and Patten, C. J. 2000. A high-throughput screen to identify inhibitors of aromatase (CYP19). Anal. Biochem. 284:427-430.
46. Vogel, S. and Heilmann, J. 2008. Synthesis, cytotoxicity, and antioxidative activity of minor prenylated chalcones from Humulus lupulus. J. Nat. Prod. 71:1237-1241.
47. Vogel, S., Ohmayer, S., Brunner, G. and Heilmann, J. 2008. Natural and non-natural prenylated chalcones: synthesis, cytotoxicity and anti-oxidative activity. Bioorg. Med. Chem. 16:4286-4293.
48. Vollmer, G. and Zierau, O. 2004. [What are phytoestrogens and phyto-SERMS]. Pharm. Unserer Zeit 33:378-383.
49. Wernert, N., Stanjek, A., Kiriakidis, S., Hugel, A., Jha, H. C., Mazitschek, R. and Giannis, A. 1999. Inhibition of angiogenesis in vivo by ets-1 antisense oligonucleotidesinhibition of Ets-1 transcription factor expression by the antibiotic fumagillin. Angew. Chem. Int. Ed. Engl. 38:3228-3231.
50. Yager, J. D. and Davidson, N. E. 2006. Estrogen carcinogenesis in breast cancer. N. Engl. J. Med. 354:270-282.
51. Yang, J. Y., Della-Fera, M. A., Rayalam, S. and Baile, C. A. 2007. Effect of xanthohumol and isoxanthohumol on 3T3-L1 cell apoptosis and adipogenesis. Apoptosis 12:1953-1963.
52. Yang, J. Y., Della-Fera, M. A., Rayalam, S. and Baile, C. A. 2008. Enhanced effects of xanthohumol plus honokiol on apoptosis in 3T3-L1 adipocytes. Obesity (Silver Spring). 16:1232-1238.