Dmd #8094 1 in Vitro Metabolic Activation of Thiabendazole via 5- Hydroxythiabendazole: Identification of a Glutathione Conjugate of 5- Hydroxythiabendazole
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In vitro metabolic activation of thiabendazole via 5-hydroxythiabendazole: identification of a glutathione conjugate of 5-hydroxythiabendazole.
Thiabendazole (TBZ) is a broad-spectrum antihelmintic used for treatment of parasitic infections in animals and humans and as an agricultural fungicide for postharvest treatment of fruits and vegetables. It is teratogenic and nephrotoxic in mice, and cases of hepatotoxicity have been observed in humans. Recent reports have demonstrated a correlation between 5-hydroxythiabendazole (5-OHTBZ) form...
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Thiabendazole (TBZ) and its major metabolite 5-hydroxythiabendazole (5OH-TBZ) were screened for potential time-dependent inhibition (TDI) against CYP1A2. Screen assays were carried out in the absence and presence of NADPH. TDI was observed with both compounds, with k(inact) and K(I) values of 0.08 and 0.02 min(-1) and 1.4 and 63.3 microM for TBZ and 5OH-TBZ, respectively. Enzyme inactivation wa...
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