Phruksawan Wanchalerm, Poapolathep Saranya, Giorgi Mario, Imsilp Kanjana, Sakulthaew Chainarong, Owen Helen, Poapolathep Amnart
Department of Pharmacology, Faculty of Veterinary Medicine, Kasetsart University, Bangkok, 10900, Thailand.
Department of Veterinary Sciences, University of Pisa, Via Livornese (lato monte), San Piero a Grado, 56122, Pisa, Italy.
Toxicon. 2018 Oct;153:78-84. doi: 10.1016/j.toxicon.2018.08.015. Epub 2018 Aug 30.
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 1 mg/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 8 h with both routes of administration. A large amount of NIV (metabolite) was quantifiable in plasma, urine and feces after both administrations. The C value of FX was 413.39 ± 206.84 ng/ml after po administration. The elimination half-life values were 1.64 ± 0.32 h and 4.69 ± 1.25 h 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.
