AI Article Synopsis
- Taxifolin, a flavonoid found in food plants, was studied for its effects on the enzyme 11β-hydroxysteroid dehydrogenase 2 (11β-HSD2) in both rat and human kidneys, which converts active cortisol into inactive forms.
- Taxifolin was found to noncompetitively inhibit 11β-HSD2, with inhibition values of 33.08 μM for rats and 13.14 μM for humans.
- Administration of taxifolin in rats significantly reduced cortisol metabolism, suggesting it is a strong 11β-HSD2 inhibitor, which could lead to potential side effects.
Article Abstract
Taxifolin is a flavonoid in food plants. Kidney 11β-hydroxysteroid dehydrogenase 2 (11β-HSD2) is an NAD-dependent oxidase that inactivates glucocorticoid cortisol (human) or corticosterone (rodents) into biologically inert 11 keto glucocorticoids. The present study investigated the effects of taxifolin on rat and human kidney microsomal 11β-HSD2. Taxifolin noncompetitively inhibited rat and human 11β-HSD2 against steroid substrates, with IC values of 33.08 and 13.14μM, respectively. Administration of 5 and 10mg/kg taxifolin for 30min ex vivo inhibited 11β-HSD2 significantly and also in vivo decreased cortisol metabolism, as shown in the significant increase of area under curve (AUC). This result shows that taxifolin is a potent 11β-HSD2 inhibitor, possibly causing side effects.
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| http://dx.doi.org/10.1016/j.fitote.2017.07.004 | DOI Listing |
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