Effects of bicyclol on aflatoxin B1 metabolism and hepatotoxicity in rats

AIM: To study the effect of new antihepatitis drug, bicyclol, on the metabolism and hepatotoxicity of aflatoxin B, (AFB(1)) in rats. METHODS: Rats were given bicyclol 300 mg(.)kg(-1.)d(-1.)g for 3 d and then injected ip with AFB(1) 1.5 mg(.)kg(-1). Liver damages were examined 16 h after ip AFB(1). The in vitro metabolism of AFB(1) by bicyclol-pretreated liver microsomes was investigated by HPLC assay. RESULTS: Bicyclol (300 mg(.)kg(-1.)d(-1) for 3 d) pretreatment provided protection against AFB(1) hepatotoxicity as evidenced by the decrease of AFB(1)-elevated serum aminotransferase and hepatic malondialdehyde in rats. Bicyclol pretreatment slightly increased the production of the less toxic metabolite aflatoxin Q(1). Bicyclol increased liver cytochrome P450 content, CYP 2B1-mediated 7-pentoxyresorufin O-dealkylase (PROD) activity, cytosolic glutathione (GSH) level, and GSH S-transferase (GST) activities, Moreover, bicyclol increased CYP 3A-mediated erythromycin-demethylase and CYP 1A-mediated 7-ethoxyresorufin O-deethylase (EROD) activities. CONCLUSION: Bicyclol protected rats against AFB(1) hepatotoxicity by increasing the detoxifying metabolism of AFB(1) in the liver.