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Synthetic isoflavones and doping: A novel class of aromatase inhibitors?
- Source :
- Drug testing and analysis. 11(2)
- Publication Year :
- 2018
-
Abstract
- 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.
- Subjects :
- gas chromatography
Pharmaceutical Science
Estrone
doping
Pharmacology
In Vitro Techniques
01 natural sciences
Formestane
Analytical Chemistry
03 medical and health sciences
chemistry.chemical_compound
0302 clinical medicine
medicine
Environmental Chemistry
metabolic pathways
Humans
Testosterone
030216 legal & forensic medicine
Chrysin
Aromatase
Spectroscopy
mass spectrometry
Doping in Sports
Flavonoids
biology
Aromatase Inhibitors
010401 analytical chemistry
Daidzein
Isoflavones
0104 chemical sciences
chemistry
biology.protein
Ipriflavone
Aminoglutethimide
medicine.drug
Subjects
Details
- ISSN :
- 19427611
- Volume :
- 11
- Issue :
- 2
- Database :
- OpenAIRE
- Journal :
- Drug testing and analysis
- Accession number :
- edsair.doi.dedup.....3be1704ab3de98485a7605c45e663ca3