Synthetic isoflavones and doping: A novel class of aromatase inhibitors?

Synthetic isoflavones and doping : A novel class of aromatase inhibitors? / Michele Iannone, Francesco Botrè, Nicoletta Cardillo, Xavier de la Torre. - (Drug Testing and Analysis 11 (2019) 2 (February); p. 208-214)

  • PMID: 30118172.
  • DOI: 10.1002/dta.2482


Anectodical information suggests that flavonoids may be widely used among athletes for their multiple biochemical and pharmacological effects. We have evaluated in vitro the effects of two synthetic isoflavones, methoxyisoflavone and ipriflavone, on the catalytic activity of human aromatase (CYP19), the enzyme catalyzing the conversion of androgens (ie, testosterone or androstenedione) to estrogens (ie, estradiol and estrone). The potential inhibitory effect was evaluated by measuring the rate of aromatization of testosterone, monitored by gas chromatography-mass spectrometry (GC-MS), both in the presence and in the absence of methoxyisoflavone or ipriflavone, comparing their effects with those of synthetic aromatase inhibitors (formestane, anastrozole, and aminoglutethimide) presently included in the list of prohibited substances and methods, and of natural flavonoids (chrysin, quercetin, and daidzein), that are known inhibitors of CYP19. The preliminary results of our in vitro study show that methoxyisoflavone and ipriflavone act as competitive inhibitors of aromatase, the degree of inhibition measured in vitro being of the same order of magnitude of that of the aromatase inhibitors commonly used in anti-estrogenic therapies. Our preliminary in vitro results indicate that, in principle, a sufficiently large intake of isoflavones could alter the kinetics of the dynamic equilibria between androgens and estrogens, suggesting their monitoring in doping control routine analysis.

Original document


Research / Study
17 August 2018
Botrè, Francesco
Cardillo, Nicoletta
de la Torre, Xavier
Iannone, Michele
Other organisations
Sapienza Università di Roma - Sapienza University of Rome
Roma, Italia: Laboratorio Antidoping FMSI
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Mass spectrometry analysis
Medical terms
Endogenous production
Gym/fitness environment
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Pdf file
Date generated
27 March 2019
Date of last modification
7 September 2020
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