ABSTRACT. Toltrazuril (TZR) is a triazine-based antiprotozoal agent. Following a single oral administration of TZR at 10 and 20 mg/kg to male pigs, the mean TZR concentration in plasma peaked at 4.24 and 8.18 g/ml at 15.0 and 12.0 hr post-dose, respectively. TZR absorbed was rapidly converted to the short-lived intermediary metabolite toltrazuril sulfoxide (TZR-SO), and then metabolized to the reactive toltrazuril sulfone (TZR-SO 2 ). TZR-SO 2 was actually more slowly eliminated, with average half-lives of 231 and 245 hr, compared with TZR (48.7 and 68.9 hr) or TZR-SO (51.9 and 53.2 hr) in the 10 and 20 mg/kg groups, respectively. This study demonstrates that TZR metabolizes to TZR-SO 2 having a long-terminal half-life, enabling the persistent clinical efficacy in the treatment of I. suis infection. In contrast, special consideration should be given to the residual of TZR-SO 2 .
Surfactin C, produced by acillus subtilis isolated from Korean soybean paste, was given to Sprague-Dawley rats of both sexes at dose of 500, 1000 or 2000 mg/kg for 28 days. There were no surfactin C-related toxicities in survival, clinical signs, and hematological parameters in the experimental period. The highest dose of surfactin C showed the decrease in body weight gain despite normal food and water consumptions and the increase in relative liver weight. alanine aminotransferase (ALT), aspartate aminotransferase (AST) and alkaline phosphatase (ALP) levels were increased in animals administered with surfactin C of 1000 or 2000 mg/kg. Zonal necrosis of hepatocyte around the hepatic vein was observed after administration of the same doses in a dose-dependent manner. In the present study, the no-observed-adverse-effect level (NOAEL) of surfactin C was 500 mg/kg following oral administration in rats.
The aim of the present study was to evaluate the protective activity of aqueous extract
from Platycodon grandiflorum (BC703) on thioacetamide (TA)-induced
hepatotoxicity in mice. We found that BC703 significantly decreased mortality and the
change in serum transaminase following TA administration. The group treated with BC703 at
doses of 1, 5, and 10 mg/kg produced significant hepatoprotective effects against
TA-induced liver damage by decreasing the activities of serum enzymes, nitric oxide and
lipid peroxidation in dose-dependent manners. Histopathological studies further
substantiated the protective effect of BC703. These results show the hepatoprotective
activity of aqueous extract from Platycodon grandiflorum on
thioacetamide-induced fulminant hepatic failure.
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