| Literature DB >> 19592245 |
Yosuke Nishizaki1, Yoichi Ishimoto, Yudai Hotta, Akifumi Hosoda, Hiromichi Yoshikawa, Miki Akamatsu, Hiroto Tamura.
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.Entities:
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Year: 2009 PMID： 19592245 DOI： 10.1016/j.bmcl.2009.06.073
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823