Effect of flavonoids on androgen and glucocorticoid receptors based on in vitro reporter gene assay.
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.
Nishizaki
Yosuke
Y
Department of Environmental Bioscience, Meijo University, Nagoya 468-8502, Japan.
Ishimoto
Yoichi
Y
Hotta
Yudai
Y
Hosoda
Akifumi
A
Yoshikawa
Hiromichi
H
Akamatsu
Miki
M
Tamura
Hiroto
H
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
D059002:Androgen Receptor Antagonists; D000728:Androgens; D005419:Flavonoids; D011944:Receptors, Androgen; D011965:Receptors, Glucocorticoid