Total views : 1632

In vitro Estrogenic Potency of Phytoestrogen-Glycosides and some Plant Flavanoids


  • Animal Physiology & Biochemistry Laboratory, Dept. of Zoology, Gauhati University, Guwahati-781014, Assam, India
  • Biomedical Sciences Division, King’s College London, University of London, United Kingdom


Many plants produce chemicals that mimic or interact with hormonal signals in animals. Their presence in human diet is the object of many studies concerned with prevention of breast and prostate cancer, osteoporosis and other hormone-dependent diseases. Isoflavones, daidzein and genistein occurring either free or bound in glycosides are the main phytoestrogens in soya. The present study investigated the estrogenic activities of two isoflavones, two glucosylated isoflavones, one isoflavandiol, two flavanoids and some other plant-derived phenolic compounds. The bioassay used in this study was an estrogen responsive cell line Ishikawa Var-1. Besides, this study also used the recombinant yeast cells bearing the human estrogen receptor for confirming the actual estrogenic nature of the plant chemicals. There was a marked stimulation of alkaline phosphatase activity in Ishikawa cells and β-galactosidase activity in yeast cells by glucosylated isoflavones, genistin and daidzin. Considering the potency of body's endogenous estrogen (17β-estradiol) as 100, in the Ishikawa assay the relative estrogenic potency of these compounds were found to be genistein (0.11), genistin (0.06), daidzein (0.08) and daidzin (0.07). In the yeast cell assay, the relative estrogenic potencies were genistein (0.1), genistin (0.01), daidzein (0.02) and daidzin (0.002). Estrogenic potency of equol was almost equal (0.18&0.16) in both Ishikawa and yeast cell assays, respectively. While kaempferol and resveratrol were weakly estrogenic, quercetin, rutin, catechin, hesperetin and luteolin did not show any estrogenic activity.


Phytoestrogen, Flavanoids, Estrogenic Activity, Glycosides

Full Text:

 |  (PDF views: 897)


  • Anderson JJ, Anthony MS, Jordan VC and VergoteI (1999): Health potentials of soy isoflavones for menopausal women. Public Health Nutr. 2, 489-504.
  • Arvidson NG (1977) Early oestrogen-induced changes in uterine albumin exchange in mice. Acta Physiol. Scand. 100, 325-331.
  • Barrett J (1996) Phytoestrogens: Friends or foes? Environ. Health Perspectives. 104, 478-482.
  • Benson GK, Cowie AT and Hosking ZD (1961) Mammogenic activity of miroestrol. J. Endocrinol. 21, 401-409.
  • Bickoff EM, Livingston AL, Hendrickson AP and Booth (1962) Relative potencies of several estrogen-like compounds found in forages. J. Agric. Food. Chem. 10, 410-412.
  • Bitter GA (2007) Regulation of human estrogen receptor alpha-mediated gene transactivation in Saccharomyces cerevisiae by human co-activator and corepressor proteins. J. Steroid Biochem. Mol. Biol. 103, 189-195.
  • Boonchird C, Mahapanichkul T and Cherdshewasart W (2010) Differential binding with ERa and ERß of the phytoestrogen-rich plant Pueraria mirifica. Braz. J. Med. Biol. Res. 43(2), 195-200.
  • Cheng EW, Yoder L, Story CD and Burroughs W (1954) Estrogenic activity of some isoflavanoid derivatives. Science.120, 575-576.
  • Cherdshewasart W, Sriwatcharakul S and Malaivijitnond S (2008) Variance of estrogenic activity of the phytoestrogen-rich plant. Maturitas. 61, 350- 357.
  • Colborn T, Dumanski D and Myers JP (1996) Our stolen future. New York: Penguin Books, Inc.
  • Coldham NG, Darby C, Hows M, King LJ, Zhang AQ and Sauer MJ (2001) Comparative metabolism of genistin by human and rat gut microflora: Detection and identification of the end-products of metabolism. Xenobiotica. 22(10), 45–62.
  • Cushnie TPT and Lamb AJ (2005) Antimicrobial activity of flavonoids. Int. J. Antimicrob. Agents. 26(5), 343–356.
  • Davis SR, Dalais FS, Simpson ER and Murkies AL (1999) Phytoestrogens in health and disease. Recent Prog. Horm. Res. 54,185-210.
  • De Sousa RR, Queiroz KC, Souza AC, Gurgueira SA, Augusto AC, Miranda MA, Peppelenbosch MP, Ferreira CV and Aoyama H (2007) Phosphoprotein levels, MAPK activities and NFkappaB expression are affected by fisetin. J. Enzyme Inhib. Med. Chem. 22(4), 439–444.
  • Farmakalidis E, Hatchcock IN and Murphy PA (1985) Oestrogenic potency of genistin and daidzin in mice. Food Chem. Toxicol. 23, 741-744.
  • Farnsworth NR, Bingel AS, Cordell GA, Crane FA and Fong HS (1975a) Potential value of plants as sources of new antifertility agents I. J. Pharm. Sci. 64, 535- 598.
  • Farnsworth NR, Bingel AS, Cordell GA, Crane FA and Fong HS (1975b) Potential value of plants as sources of new antifertility agents II. J. Pharm. Sci. 64, 717- 753.
  • Galeotti F, Barile E, Curir P, Dolci, M and Lanzotti V (2008) Flavonoids from carnation (Dianthus caryophyllus) and their antifungal activity. Phytochem. Letts. 1, 44.
  • Harmsen S, Meijerman I, Beijnen JH and Schellens JH (2007) The role of nuclear receptors in harmacokinetic drug-drug interactions in oncology. Cancer Treat Rev. 33, 369-380.
  • Kalita JC (1998) Studies of plant oestrogens with special reference to hops (Humulus lupulus L.) Ph. D Thesis, King’s College, University of London.
  • Kalita JC, Sharma DK and Milligan SR (2006) Oestrogenic potency of certain established dietary phytoestrogens in cell culture bioassay. Adv. Reproductive Toxicol. Pointer publishers, Jaipur, India. Eds. pp: 273-293.
  • Keung WM and Vallee BL (1998) Kudzu root: An ancient Chinese source of modern antidipsotropic agents. Phytochem. 47(4), 499–506.
  • Littlefield BA, Gurpide E, Markiewicz L, McKinley B and Hochberg RB (1990) A Simple and sensitive microtiter plate estrogen bioassay based on Stimulation of alkaline phosphatase in Ishikawa cells: Estrogen action of adrenal steroids. Endocrinol. 127, 2757-2761.
  • Malaivijitnond S, Chansri K, Kijkuokul P, Urasopon N and Cherd-shewasart W (2006) Using vaginal cytology to assess the estro-genic activity of phytoestrogen-rich herb. J. Ethnopharmacol. 107, 354-360.
  • Markiewicz L, Garey J, Adlercreutz H and Gurpide E (1993) In vitro bioassays of non-steroidal phytoestrogens. J. Steroid Biochem. Mol. Biol. 45, 399-405.
  • Mayr U, Butsch A and Schneider S (1992) Validation of two in vitro test systems for estrogenic activities with zearalenone, phytoestrogens and cereal extracts. Toxicol. 74, 135-149.
  • McLachlan et al. (1997) Synergistic effects of environmental estrogens: Report withdrawn. Science. 277, 459.
  • Miksicek RJ (1993) Commonly occurring plant flavonoids have estrogenic activity. Mol. Pharmacol. 44, 37-43.
  • Miksicek RJ (1994) Interaction of naturally occurring nonsteroidal estrogens with expressed recombinant human estrogen receptor. J. Steroid Biochem. Molec. Biol. 49, 153-160. 30.Milligan SR, Balasubramanian AV and Kalita JC (1998) Relative potency of xenobiotic estrogens in an acute in vivo mammalian assay. Environ. Health Perspec. 106, 23-26.
  • Osman S and Fett W (1983) Isoflavone glucoside stress metabolites of soybean leaves. Phytochem. 22, 1921.
  • Ramsey LA, Ross BS and Fischer RG (1999) Phytoestrogens and the management of menopause. Adv. Nurse Practitioners. 7, 26-30.
  • Rezvani A (2003) Plant derivatives in the treatment of alcohol dependency. Pharmacol. Biochem. Behavior. 75, 593.
  • Routledge EJ and Sumpter JP (1996) Estrogenic activity of surfactants and some of their degradation products assessed using a recombinant yeast screen. Environ. Toxicol. Chem. 15, 241-248.
  • Russell L, Swink Hicks G, Low AK, Sheperd JM and Brown CA (2002) Phytoestrogens: A viable option? Am. J. Med. Sci. 324(4), 185-188.
  • Spencer and Jeremy PE (2008) Flavonoids: Modulators of brain function? British J. Nutrition. 99, 60–77.
  • Whitten PL, Russell E and Naftolin F (1992) Effects of a normal, human-concentration, phytoestrogen diet on rat uterine growth. Steroids. 57, 99-106.
  • Yamamoto Y and Richard B Gaynor (2001) Therapeutic potential of inhibition of the NF-?B pathway in the treatment of inflammation and cancer. J. Clin. Invest. 107(2), 135–142.
  • Zava DT and Duwe G (1997) Estrogenic and antiproliferative properties of genistein and other flavonoids in human breast cancer cells in vitro. Nutr. Cancer. 27, 31-40.


  • There are currently no refbacks.

Creative Commons License
This work is licensed under a Creative Commons Attribution 3.0 License.