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Metabolites, Volume 9, Issue 8 (August 2019)
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Cover Story (view full-size image) Enniatins (ENNs) are fungal secondary metabolites that frequently occur in grain in temperate [...] Read more. Enniatins (ENNs) are fungal secondary metabolites that frequently occur in grain in temperate climates. Their toxic potency is connected to their ionophoric character and lipophilicity. The biotransformation of ENNs predominantly takes place via cytochrome P450 3A (CYP 3A)-dependent oxidation reactions. In the present study, we determined the kinetic characteristics and inhibitory potential of ENNB1 in human liver microsomes and CYP3A4-containing nanodiscs. Considering the importance of CYP3A4 in the metabolism of ENNB1 in vitro, the potential for drug–drug interactions was studied using deoxynivalenol (DON), one of the most prevalent Fusarium mycotoxins in grain. Although DON was not metabolized by CYP3A4 or binding to its active site, the metabolite formation rates of ENNB1 and the frequently used drugs progesterone and atorvastatin lactone were noticeably reduced, indicating a certain binding affinity of DON to the enzyme. View this p