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Vol. 26, Issue 2, 91-97, February 1998
-Dipyridyl in Rats Is Not Accompanied
by Induction of Intestinal Enzymes
Department of Pharmacology and Toxicology, University of Utah
The induction of hepatic and intestinal cytochrome P450,
NAD(P)H:quinone oxidoreductase (QOR), glutathione
S-transferase (GST), and UDP-glucuronosyltransferase (UGT)
activities by intragastric administration of 1,7-phenanthroline,
2,2
-dipyridyl, and oltipraz has been investigated in rats. In the
liver, all three compounds induced phase II drug-metabolizing enzymes
without inducing overall cytochrome P450 concentrations and, in a
direct comparison, all agents induced the enzymes to a greater extent
than did the same dose of tert-butyl-4-hydroxyanisole. With
a 75 mg/kg daily, 3-day regimen, UGT, GST, and QOR activities were
induced by all compounds. The changes in hepatic GST, QOR, and UGT
activities induced by N-heterocyclic compounds were
accompanied by increases in the amounts of mRNA for GST Ya
(2-2.4-fold), QOR (1.6-2.8-fold), and the UGTs UGT2B1 (4-6-fold) and
UGT1A6 (4-10-fold). Changes in the amounts of UGT2B1 mRNA and UGT1A6
mRNA were highly correlated (r = 0.9), but there was
no correlation between changes in either UGT2B1 or UGT1A6 mRNA and GST
Ya mRNA. No significant mRNA changes were elicited by
tert-butyl-4-hydroxyanisole. Neither GST nor UGT activities
were induced in the small intestinal mucosa by any agent. QOR activity
was slightly induced by oltipraz. The data suggest that requirements
for induction of phase II enzymes in the intestine are markedly
different from requirements in the liver.
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