title: Effect of flavonoids on androgen and glucocorticoid receptors based on in vitro reporter gene assay.
abstract: 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.
authors: Department of Environmental Bioscience, Meijo University, Nagoya 468-8502, Japan.
authors: Yosuke
authors: Y
authors: Nishizaki
authors: Yoichi
authors: Y
authors: Ishimoto
authors: Yudai
authors: Y
authors: Hotta
authors: Akifumi
authors: A
authors: Hosoda
authors: Hiromichi
authors: H
authors: Yoshikawa
authors: Miki
authors: M
authors: Akamatsu
authors: Hiroto
authors: H
authors: Tamura
mesh_terms: D059002:Androgen Receptor Antagonists; D000728:Androgens; D045744:Cell Line, Tumor; D005419:Flavonoids / Q000737:chemistry / Q000494:pharmacology*; D017930:Genes, Reporter / Q000235:genetics*; D006801:Humans; D011944:Receptors, Androgen / Q000378:metabolism; D011965:Receptors, Glucocorticoid / Q000819:agonists* / Q000037:antagonists & inhibitors* / Q000378:metabolism; D013329:Structure-Activity Relationship
chemical_list: D059002:Androgen Receptor Antagonists; D000728:Androgens; D005419:Flavonoids; D011944:Receptors, Androgen; D011965:Receptors, Glucocorticoid