Chem -Bwl Interactwns, 83 (1992) 155 - 169 155
Elsevier Scmntlfic Pubhshers Ireland Ltd
THE ANTI-CARCINOGENIC PLANT COMPOUND INDOLE-3-CARBINOL
DIFFERENTIALLY MODULATES P450-MEDIATED STEROID
HYDROXYLASE ACTIVITIES IN MICE
WILLIAM S BALDWIN and GERALD A LEBLANC
Department of Toxicology, Box 7633, North Carohna State Unwers~ty, Raleigh, NC 27695 (USA)
(Received March 3rd, 1992)
(Rewsmn received April 14th, 1992)
(Accepted April 14th, 1992)
SUMMARY
Indole-3-carbmol (I3C), a component of cruclferous vegetables, exhibits anti-
carcinogenic activity m a variety of model systems This activity has been
attributed m part to the reduction of cytochrome P450 CYP1A subfamily
members and the resulting mcreased metabohc mactlvatmn of chemmal carcino-
gens The present study was undertaken to assess the effects of I3C on several
constitutive P450 actlvltms that contribute to both carcinogen and stermd hor-
mone metabohsm Mxce were administered I3C m their diet at estimated dally
doses of 250, 500 and 750 mg/kg for 1 week Liver mmrosomes from treated and
untreated mine were subsequently assayed for CYPIA-medmted ethoxy-
resorufin O-deethylase (EROD) actlwty, estradml 2-hydroxylase actavlty and
seven different testosterone hydroxylase act~wtms I3C elevated EROD,
estradlol 2-hydroxylase and testosterone 6a-hydroxylase actwltms m a dose-
dependent manner The other SLX testosterone hydroxylase act~wtms were not
slgmficantly affected by m wvo treatment with I3C In ad&tmn to its effects on
steroid hydroxylase actlwtms, I3C also elevated NADPH-cytochrome P450
reductase actlwty, a necessary component to the P450 monooxygenase system
We next examined the direct m wtro effects of I3C and its acid condensatmn
products, as are generated in the stomach following mgestmn, on the
P450 catalytm actlvxtms Testosterone 6~-hydroxylase, the major testosterone
hydroxylase actlwty m untreated mine, was sxgmficantly inhabited (ICs0 - 12
#g/ml) by the acid condensatmn products of I3C In contrast, all other P450
actlwtms were not appreciably affected by I3C or its acid condensatmn products
These results mdmate that I3C can ehclt both mductwe and suppressive effects
on the constitutive P450s that partxclpate m carcinogen and steroid hormone
metabohsm This plelotropm effect on hepatm catalytm enzymes may contnbute
to the ante-carcinogenic properties of th~s compound
Correspondence to G A LeBlanc, Department of Toxmology, Box 7633, North Carohna State
Umverslty, Raleigh, NC 27695, USA
0009-2797/92/$05 00
© 1992 Elsewer Scmntlfic Pubhshers Ireland Ltd
Pnnted and Pubhshed in Ireland