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Inhibition of aromatase (estrogen synthase) activity by several flavonoids
Author(s) -
Monteiro Rosário,
Azevedo Isabel,
Calhau Conceição
Publication year - 2006
Publication title -
the faseb journal
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.709
H-Index - 277
eISSN - 1530-6860
pISSN - 0892-6638
DOI - 10.1096/fasebj.20.4.a355-b
Subject(s) - aromatase , estrogen , chemistry , medicine , endocrinology , genistein , daidzein , androstenedione , naringenin , biology , biochemistry , flavonoid , androgen , hormone , cancer , breast cancer , antioxidant
Besides their functions in reproduction, estrogens are involved in physiological phenomena such as regulation of body weight and fat distribution, maintenance of bone mass and preservation of cognitive skills. Estrogens are also involved in the development of estrogen‐dependent cancers. Polyphenols are food components known to modulate biochemical processes. For this reason, we decided to test the effect of daidzein, genistein, kampferol, naringenin and 8‐prenylnaringenin on the activity and expression of aromatase. Choriocarcinoma derived JAR cells, which express high levels of aromatase, were preincubated with different concentrations of compounds for 2 h and aromatase activity was determined by tritiated water release assay, by incubating cells with compounds and 3H‐androstenedione for 1 h. All tested compounds dose‐dependently inhibited aromatase except daidzein which had no effect on aromatase activity. 8‐Prenylnaringenin was the most potent compound. The effect of the same compounds on aromatase expression was also assessed by western blotting and RT‐PCR after treatment of the cells with 100 μM of the compounds for 24 h. No effect was observed. The results showed that these food components are able to inhibit aromatase and that this occurs independently of aromatase synthesis. So, the ingestion of certain foodstuffs potentially decreases estrogen synthesis, what may therefore be of interest in the management of estrogen‐dependent diseases. Supported by FCT (POCTI, Feder, Programa Comunitário de Apoio, and SFRH/BD/12622/2003).