S. Hegstad et al., Characterization of metabolites of benz(j)aceanthrylene in faeces, urine and bile from rat, XENOBIOTICA, 29(12), 1999, pp. 1257-1272
1. The excretion of benz[j]aceanthrylene (B[j]A) and the biotransformation
products found in faeces, urine and bile of rat exposed to [H-3]-labelled B
[j]A have been studied.
2. About 95% of the administered radioactivity was excreted within 7 days,
79% via faeces and 16% via urine, and most of the radioactivity in urine an
d faeces was excreted within 2 days.
3. The B[j]A metabolites excreted between days 1 and 2, including those exc
reted in bile during the first 5.5 h in a separate experiment, were further
characterized by HPLC, UV and electrospray/atmospheric pressure chemical i
onization mass spectrometry.
4. In faeces, bile and urine, hydroxylated B[j]A metabolites predominated.
The major metabolites in faeces were B[j]A-1,2-dihydrodiol-8-hydroxy and B[
j]A-1,2-dihydrodiol-10-hydroxy. These metabolites were found as conjugated
metabolites in the bile. The glucuronide conjugate of B[j]A-1,2-dihydrodiol
-10-hydroxy was also a major metabolite in urine. Two sulphate conjugates o
f oxidized B[j]A were detected in bile, a sulphate conjugate of a B[j]A-dih
ydrodiol-phenol and B[j]A-1,2-dihydrodiol-10-sulphate. Trans-B[j]A-1,2-dihy
drodiol was detected in urine, faeces and bile.
5. These findings support the hypothesis that epoxidation at the cyclopenta
ring is an important biotransformation pathway for B[j]A in vivo. In addit
ion to the characterized metabolites, a large fraction of polar compounds,
possibly glutathione conjugates, was also excreted in urine and bile.