Effects of flavonoids on aromatase activity, an in vitro study.
In the study, the inhibitory effect of flavonoids, including isoflavonic phytoestrogens, on the ovarian aromatase enzyme complex from the rainbow trout, Oncorhynchus mykiss, was assessed in vitro. Some of the compounds tested on fish were also tested on human placental aromatase activity as a comparison between the two sources of enzyme. It was found that flavone, dl-aminoglutethimide, apigenin, quercetin, 7,4'- dihydroxyflavone, alpha-naphthoflavone and equol were potent inhibitors of the ovarian aromatase activity in rainbow trout. Relative potencies (RP) of these compounds compared to flavone (assigned an effect of 1) were, respectively, 19.0, 8.7, 5.3, 3.7, 3.2 and 0.9. Two other phytoestrogens, namely biochanin A and genistein, slightly inhibited aromatase activity. Finally, 7-hydroxyflavone, formononetin, daidzein, coumestrol, chrysin, flavanone and estradiol-17beta did not inhibit ovarian aromatase activity at doses up to 1000 microM. Experiments on human placental aromatase showed inhibitory effects of dl-aminoglutethimide, flavone, flavanone and equol with RP values of 2.8. 1, 1.5 and 0.4, respectively. These results are in accordance with previous studies. The influence of the experimental procedure on IC50 values and RP is discussed.
Pelissero
C
C
ENITA Bordeaux, Ave Général de Gaulle, Gradignan, France.
Lenczowski
M J
MJ
Chinzi
D
D
Davail-Cuisset
B
B
Sumpter
J P
JP
Fostier
A
A
D000616:Aminoglutethimide / Q000494:pharmacology; D000818:Animals; D047072:Aromatase Inhibitors; D002839:Chromans / Q000494:pharmacology; D004791:Enzyme Inhibitors / Q000494:pharmacology*; D060754:Equol; D004968:Estrogens, Non-Steroidal / Q000494:pharmacology*; D005260:Female; D005419:Flavonoids / Q000494:pharmacology*; D006801:Humans; D007529:Isoflavones; D008861:Microsomes / Q000201:enzymology; D017686:Oncorhynchus mykiss; D010053:Ovary / Q000201:enzymology; D048789:Phytoestrogens; D010920:Placenta / Q000201:enzymology; D028321:Plant Preparations
C007610:4',7-dihydroxy-3,4-dihydroisoflavone; D047072:Aromatase Inhibitors; D002839:Chromans; D004791:Enzyme Inhibitors; D004968:Estrogens, Non-Steroidal; D005419:Flavonoids; D007529:Isoflavones; D048789:Phytoestrogens; D028321:Plant Preparations; D000616:Aminoglutethimide; D060754:Equol