Toxicokinetic profile of fusarenon-X and its metabolite nivalenol in the goat(Capra hircus)

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The main aim of this research was to evaluate the toxicokinetic characteristics of fusarenon-X (FX) and its metabolite, nivalenol (NIV), in goats. The amounts of FX and NIV in post-mitochondrial (S-9), microsomal and cytosolic fractions of diverse tissues of the goat were also investigated. FX was intravenously (iv) or orally (po) administered to goats at dosages of 0.25 and 1mg/kg bw, respectively. The concentrations of FX and NIV in plasma, feces and urine were quantified by liquid chromatography tandem-mass spectrometry (LC-ESI-MS/MS). The concentrations of FX in plasma were quantified up to 8h with both routes of administration. A large amount of NIV (metabolite) was quantifiable in plasma, urine and feces after both administrations. The Cmax value of FX was 413.39±206.84ng/ml after po administration. The elimination half-life values were 1.64±0.32h and 4.69±1.25h after iv and po administration, respectively. In vitro experiments showed that the conversion FX-to-NIV mainly occurs in the liver microsomal fraction. This is the first study that evaluates the fate and metabolism of FX in ruminant species.HIGHLIGHTSThis is the first study that evaluates the fate and metabolism of FX in ruminant species.FX is absorbed from the gastrointestinal tract with a relatively low bioavailability in goats.The liver is the organ responsible for the FX-to-NIV biotransformation in goats.FX is excreted mainly as NIV in the feces of goats after p.o. administration of FX.

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