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 B1 (AFB1) in rats.
METHODS: Rats were given bicyclol 300 mg/kg/d ig for 3 d and then injected ip
with AFB1 1.5 mg/kg. Liver damages were examined 16 h after ip AFB1. The in vitro
metabolism of AFB1 by bicyclol-pretreated liver microsomes was investigated by
HPLC assay.
RESULTS: Bicyclol (300 mg/kg/d for 3 d) pretreatment provided protection against
AFB1 hepatotoxicity as evidenced by the decrease of AFB1-elevated serum
aminotransferase and hepatic malondialdehyde in rats. Bicyclol pretreatment
slightly increased the production of the less toxic metabolite aflatoxin Q1.
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 AFB1 hepatotoxicity by increasing the
detoxifying metabolism of AFB1 in the liver.