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Evidence-Based Complementary and Alternative Medicine
Volume 2013, Article ID 635694, 10 pages
http://dx.doi.org/10.1155/2013/635694
Research Article

Synergistic Action of Flavonoids, Baicalein, and Daidzein in Estrogenic and Neuroprotective Effects: A Development of Potential Health Products and Therapeutic Drugs against Alzheimer’s Disease

Division of Life Science and Center for Chinese Medicine, State Key Laboratory of Molecular Neuroscience, The Hong Kong University of Science and Technology, Clear Water Bay Road, Kowloon, Hong Kong

Received 3 December 2012; Revised 15 May 2013; Accepted 10 June 2013

Academic Editor: Mee-Ra Rhyu

Copyright © 2013 Roy C. Y. Choi et al. This is an open access article distributed under the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

Linked References

  1. J. M. Hall and D. P. McDonnell, “Co-regulators in nuclear estrogen receptor action: from concept to therapeutic targeting,” Molecular Interventions, vol. 5, no. 6, pp. 343–357, 2005. View at Publisher · View at Google Scholar · View at Scopus
  2. L. L. Shook, “An update on hormone replacement therapy: health and medicine for women: a multidisciplinary, evidence-based review of mid-life health concerns,” Yale Journal of Biology and Medicine, vol. 84, no. 1, pp. 39–42, 2011. View at Google Scholar · View at Scopus
  3. M. G. Glazier and M. A. Bowman, “A review of the evidence for the use of phytoestrogens as a replacement for traditional estrogen replacement therapy,” Archives of Internal Medicine, vol. 161, no. 9, pp. 1161–1172, 2001. View at Google Scholar · View at Scopus
  4. M. D. Long, C. F. Martin, J. A. Galanko, and R. S. Sandler, “Hormone replacement therapy, oral contraceptive use, and distal large bowel cancer: a population-based case-control study,” The American Journal of Gastroenterology, vol. 105, no. 8, pp. 1843–1850, 2010. View at Publisher · View at Google Scholar · View at Scopus
  5. G. E. Gillies and S. McArthur, “Estrogen actions in the brain and the basis for differential action in men and women: a case for sex-specific medicines,” Pharmacological Reviews, vol. 62, no. 2, pp. 155–198, 2010. View at Publisher · View at Google Scholar · View at Scopus
  6. P. S. Green, K. E. Gridley, and J. W. Simpkins, “Estradiol protects against β-amyloid (25–35)-induced toxicity in SK-N-SH human neuroblastoma cells,” Neuroscience Letters, vol. 218, no. 3, pp. 165–168, 1996. View at Publisher · View at Google Scholar · View at Scopus
  7. S. Goodenough, M. Schäfer, and C. Behl, “Estrogen-induced cell signalling in a cellular model of Alzheimer's disease,” Journal of Steroid Biochemistry and Molecular Biology, vol. 84, no. 2-3, pp. 301–305, 2003. View at Publisher · View at Google Scholar · View at Scopus
  8. L. Fester, J. Prange-Kiel, L. Zhou et al., “Estrogen-regulated synaptogenesis in the hippocampus: sexual dimorphism in vivo but not in vitro,” Journal of Steroid Biochemistry and Molecular Biology, vol. 131, no. 1-2, pp. 24–29, 2012. View at Publisher · View at Google Scholar · View at Scopus
  9. M. E. Bailey, A. C. Wang, J. Hao et al., “Interactive effects of age and estrogen on cortical neurons: implications for cognitive aging,” Neuroscience, vol. 191, pp. 148–158, 2011. View at Publisher · View at Google Scholar · View at Scopus
  10. R. Norbury, W. J. Cutter, J. Compton et al., “The neuroprotective effects of estrogen on the aging brain,” Experimental Gerontology, vol. 38, no. 1-2, pp. 109–117, 2003. View at Publisher · View at Google Scholar · View at Scopus
  11. X. Zhu, A. K. Raina, H.-G. Lee, G. Casadesus, M. A. Smith, and G. Perry, “Oxidative stress signalling in Alzheimer's disease,” Brain Research, vol. 1000, no. 1-2, pp. 32–39, 2004. View at Publisher · View at Google Scholar · View at Scopus
  12. K. Irie, K. Murakami, Y. Masuda et al., “Structure of β-amyloid fibrils and its relevance to their neurotoxicity: implications for the pathogenesis of Alzheimer's disease,” Journal of Bioscience and Bioengineering, vol. 99, no. 5, pp. 437–447, 2005. View at Publisher · View at Google Scholar · View at Scopus
  13. R. E. Tanzi and L. Bertram, “Twenty years of the Alzheimer's disease amyloid hypothesis: a genetic perspective,” Cell, vol. 120, no. 4, pp. 545–555, 2005. View at Publisher · View at Google Scholar · View at Scopus
  14. R. J. Miksicek, “Commonly occurring plant flavonoids have estrogenic activity,” Molecular Pharmacology, vol. 44, no. 1, pp. 37–43, 1993. View at Google Scholar · View at Scopus
  15. A. L. Murkies, G. Wilcox, and S. R. Davis, “Phytoestrogens,” Journal of Clinical Endocrinology and Metabolism, vol. 83, no. 2, pp. 297–303, 1998. View at Publisher · View at Google Scholar · View at Scopus
  16. P. Mullie, P. Clarys, P. Deriemaeker, and M. Hebbelinck, “Estimation of daily human intake of food flavonoids,” International Journal of Food Sciences and Nutrition, vol. 59, no. 4, pp. 291–298, 2008. View at Publisher · View at Google Scholar · View at Scopus
  17. O. K. Chun, S. J. Chung, and W. O. Song, “Estimated dietary flavonoid intake and major food sources of U.S. adults,” Journal of Nutrition, vol. 137, no. 5, pp. 1244–1252, 2007. View at Google Scholar · View at Scopus
  18. D. Dixon-Shanies and N. Shaikh, “Growth inhibition of human breast cancer cells by herbs and phytoestrogens,” Oncology Reports, vol. 6, no. 6, pp. 1383–1387, 1999. View at Google Scholar · View at Scopus
  19. N. D. Fisher, F. A. Sorond, and N. K. Hollenberg, “Cocoa flavanols and brain perfusion,” Journal of Cardiovascular Pharmacology, vol. 47, no. 2, pp. S210–S214, 2006. View at Publisher · View at Google Scholar · View at Scopus
  20. F. Dajas, F. Rivera-Megret, F. Blasina et al., “Neuroprotection by flavonoids,” Brazilian Journal of Medical and Biological Research, vol. 36, no. 12, pp. 1613–1620, 2003. View at Google Scholar · View at Scopus
  21. O. I. Aruoma, T. Bahorun, and L.-S. Jen, “Neuroprotection by bioactive components in medicinal and food plant extracts,” Mutation Research, vol. 544, no. 2-3, pp. 203–215, 2003. View at Publisher · View at Google Scholar · View at Scopus
  22. M. D'Archivio, C. Filesi, R. Di Benedetto, R. Gargiulo, C. Giovannini, and R. Masella, “Polyphenols, dietary sources and bioavailability,” Annali dell'Istituto Superiore di Sanita, vol. 43, no. 4, pp. 348–361, 2007. View at Google Scholar · View at Scopus
  23. H. Kim, B.-S. Park, K.-G. Lee et al., “Effects of naturally occurring compounds on fibril formation and oxidative stress of β-amyloid,” Journal of Agricultural and Food Chemistry, vol. 53, no. 22, pp. 8537–8541, 2005. View at Publisher · View at Google Scholar · View at Scopus
  24. A. J. Guo, H. Q. Xie, R. C. Choi et al., “Galangin, a flavonol derived from Rhizoma Alpiniae Officinarum, inhibits acetylcholinesterase activity in vitro,” Chemico-Biological Interactions, vol. 187, no. 1–3, pp. 246–248, 2010. View at Publisher · View at Google Scholar · View at Scopus
  25. A. J. Guo, R. C. Choi, A. W. Cheung et al., “Baicalin, a flavone, induces the differentiation of cultured osteoblasts: an action via the Wnt/β-catenin signaling pathway,” The Journal of Biological Chemistry, vol. 286, pp. 27882–27893, 2012. View at Publisher · View at Google Scholar · View at Scopus
  26. K. Y. Zheng, R. C. Choi, A. W. Cheung et al., “Flavonoids from radix astragali induce the expression of erythropoietin in cultured cells: a signaling mediated via the accumulation of hypoxia-inducible factor-1α,” Journal of Agricultural and Food Chemistry, vol. 59, no. 5, pp. 1697–1704, 2011. View at Publisher · View at Google Scholar · View at Scopus
  27. A. J. Guo, R. C. Choi, K. Y. Zheng et al., “Kaempferol as a flavonoid induces osteoblastic differentiation via estrogen receptor signaling,” Chinese Medicine, vol. 7, p. 10, 2012. View at Publisher · View at Google Scholar
  28. J. T. Zhu, R. C. Choi, G. K. Chu et al., “Flavonoids possess neuroprotective effects on cultured pheochromocytoma PC12 cells: a comparison of different flavonoids in activating estrogenic effect and in preventing β-amyloid-induced cell death,” Journal of Agricultural and Food Chemistry, vol. 55, no. 6, pp. 2438–2445, 2007. View at Publisher · View at Google Scholar · View at Scopus
  29. J. T. Zhu, R. C. Choi, H. Q. Xie et al., “Hibifolin, a flavonol glycoside, prevents β-amyloid-induced neurotoxicity in cultured cortical neurons,” Neuroscience Letters, vol. 461, no. 2, pp. 172–176, 2009. View at Publisher · View at Google Scholar · View at Scopus
  30. J. T. Zhu, R. C. Choi, J. Li et al., “Estrogenic and neuroprotective properties of scutellarin from erigeron breviscapus: a drug against postmenopausal symptoms and Alzheimer's disease,” Planta Medica, vol. 75, no. 14, pp. 1489–1493, 2009. View at Publisher · View at Google Scholar · View at Scopus
  31. S. L. Xu, R. C. Choi, K. Y. Zhu et al., “Isorhamnetin, a flavonol aglycone from Ginkgo biloba L., induces neuronal differentiation of cultured PC12 cells: potentiating the effect of nerve growth factor,” Evidence-Based Complementary and Alternative Medicine, vol. 2012, 11 pages, 2012. View at Publisher · View at Google Scholar
  32. Q. T. Gao, R. C. Choi, A. W. Cheung et al., “Danggui buxue tang—a Chinese herbal decoction activates the phosphorylations of extracellular signal-regulated kinase and estrogen receptor α in cultured MCF-7 cells,” FEBS Letters, vol. 581, no. 2, pp. 233–240, 2007. View at Publisher · View at Google Scholar · View at Scopus
  33. T. C. Chou, R. J. Motzer, Y. Tong, and G. J. Bosl, “Computerized quantitation of synergism and antagonism of taxol, topotecan, and cisplatin against human teratocarcinoma cell growth: a rational approach to clinical protocol design,” Journal of the National Cancer Institute, vol. 88, no. 20, pp. 1517–1524, 1994. View at Google Scholar · View at Scopus
  34. T. C. Chou and M. Hayball, Calcusyn for Windows, Multiple-Drug Dose-Effect Analyser and Manual, Biosoft, Cambridge, UK, 1996.
  35. T.-C. Chou, “Drug combination studies and their synergy quantification using the chou-talalay method,” Cancer Research, vol. 70, no. 2, pp. 440–446, 2010. View at Publisher · View at Google Scholar · View at Scopus
  36. L. N. Zhao, H. Long, Y. Mu, and L. Y. Chew, “The toxicity of amyloid β oligomers,” International Journal of Molecular Sciences, vol. 13, pp. 7303–7327, 2012. View at Google Scholar
  37. A. O. Mueck, “Postmenopausal hormone replacement therapy and cardiovascular disease: the value of transdermal estradiol and micronized progesterone,” Climacteric, vol. 15, supplement 1, pp. 11–17, 2012. View at Publisher · View at Google Scholar · View at Scopus
  38. R. C. Choi, J. T. Zhu, K. W. Leung et al., “A flavonol glycoside, isolated from roots of panax notoginseng, reduces amyloid-β-induced neurotoxicity in cultured neurons: signaling transduction and drug development for Alzheimer's disease,” Journal of Alzheimer's Disease, vol. 19, no. 3, pp. 795–811, 2010. View at Publisher · View at Google Scholar · View at Scopus
  39. H. Faus and B. Haendler, “Post-translational modifications of steroid receptors,” Biomedicine and Pharmacotherapy, vol. 60, no. 9, pp. 520–528, 2006. View at Publisher · View at Google Scholar · View at Scopus
  40. Y. Mérot, F. Ferrière, E. Debroas, G. Flouriot, D. Duval, and C. Saligaut, “Estrogen receptor alpha mediates neuronal differentiation and neuroprotection in PC12 cells: critical role of the A/B domain of the receptor,” Journal of Molecular Endocrinology, vol. 35, no. 2, pp. 257–267, 2005. View at Publisher · View at Google Scholar · View at Scopus
  41. N. Linford, C. Wade, and D. Dorsa, “The rapid effects of estrogen are implicated in estrogen-mediated neuroprotection,” Journal of Neurocytology, vol. 29, no. 5-6, pp. 367–374, 2000. View at Publisher · View at Google Scholar · View at Scopus
  42. M. Fotuhi, P. P. Zandi, K. M. Hayden et al., “Better cognitive performance in elderly taking antioxidant vitamins E and C supplements in combination with nonsteroidal anti-inflammatory drugs: the Cache County Study,” Alzheimer's and Dementia, vol. 4, no. 3, pp. 223–227, 2008. View at Publisher · View at Google Scholar · View at Scopus
  43. A. Lebeau, F. Esclaire, W. Rostène, and D. Pélaprat, “Baicalein protects cortical neurons from β-amyloid (25–35) induced toxicity,” NeuroReport, vol. 12, no. 10, pp. 2199–2202, 2001. View at Google Scholar · View at Scopus
  44. Y. Z. Shang, H. Miao, J. J. Cheng, and J. M. Qi, “Effects of amelioration of total flavonoids from stems and leaves of Scutellaria baicalensis Georgi on cognitive deficits, neuronal damage and free radicals disorder induced by cerebral ischemia in rats,” Biological and Pharmaceutical Bulletin, vol. 29, no. 4, pp. 805–810, 2006. View at Publisher · View at Google Scholar · View at Scopus
  45. L. Prokai and J. W. Simpkins, “Structure-nongenomic neuroprotection relationship of estrogens and estrogen-derived compounds,” Pharmacology and Therapeutics, vol. 114, no. 1, pp. 1–12, 2007. View at Publisher · View at Google Scholar · View at Scopus
  46. H. Y. Chen, K. D. Dykstra, E. T. Birzin et al., “Estrogen receptor ligands—part 1: the discovery of flavanoids with subtype selectivity,” Bioorganic and Medicinal Chemistry Letters, vol. 14, no. 6, pp. 1417–1421, 2004. View at Publisher · View at Google Scholar · View at Scopus
  47. M. E. Schutte, M. G. Boersma, D. A. Verhallen, J. P. Groten, and I. M. C. Rietjens, “Effects of flavonoid mixtures on the transport of 2-amino-1-methyl-6-phenylimidazo[4,5-b]pyridine (PhIP) through Caco-2 monolayers: an in vitro and kinetic modeling approach to predict the combined effects on transporter inhibition,” Food and Chemical Toxicology, vol. 46, no. 2, pp. 557–566, 2008. View at Publisher · View at Google Scholar · View at Scopus