Effect of flavonoids on androgen and glucocorticoid receptors based on in vitro reporter gene assay

Bioorg Med Chem Lett. 2009 Aug 15;19(16):4706-10. doi: 10.1016/j.bmcl.2009.06.073. Epub 2009 Jun 23.


The effect of 32 flavonoids on androgen (AR) and glucocorticoid receptors (GR) was investigated using an MDA-kb2 human breast cancer cell line to predict potential AR and GR activities. Among them, 5-hydroxyflavone (7) had the highest AR antagonistic activity with an IC(50) value of 0.3 microM, whereas 6-methoxyflavone (11) had the highest induced luciferase activity with an EC(150) value of 0.7 microM. Genistein (2) and daizein (1) showed a sufficient increase of luciferase activities as their concentrations increased with EC(150) values of 4.4 and 10.1 microM, respectively. These findings provide evidence of a fundamental property of their structure-activity relationship with AR and/or GR.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Androgen Receptor Antagonists*
  • Androgens*
  • Cell Line, Tumor
  • Flavonoids / chemistry
  • Flavonoids / pharmacology*
  • Genes, Reporter / genetics*
  • Humans
  • Receptors, Androgen / metabolism
  • Receptors, Glucocorticoid / agonists*
  • Receptors, Glucocorticoid / antagonists & inhibitors*
  • Receptors, Glucocorticoid / metabolism
  • Structure-Activity Relationship


  • Androgen Receptor Antagonists
  • Androgens
  • Flavonoids
  • Receptors, Androgen
  • Receptors, Glucocorticoid