TABLE 3

NC-Induced inhibition of E2 hydroxylation activity of CYP1A1, CYP1B1, and CYP1A2

Data represent the mean ± S.D. (n = 3).

CYP1 EnzymeE2 Hydroxylation SiteKmVmaxVmax/KmActivity Ratio (2-/4-)IC50IC50 Ratio (2-/4-)
μMnmol/min per nanomoles P450ml/min per nanomoles P450μM
1A12-OHE23.38 ± 0.696.91 ± 0.332.042550.16 ± 0.0040.64
4-OHE228.9 ± 11.50.22 ± 0.040.0080.25 ± 0.04
1B12-OHE22.26 ± 0.300.45 ± 0.040.200.1435.0 ± 6.444.23
4-OHE20.87 ± 0.161.21 ± 0.121.398.27 ± 2.40
1A22-OHE223.7 ± 4.0650.6 ± 4.932.145513.2 ± 5.562.47
4-OHE224.8 ± 4.780.97 ± 0.140.045.35 ± 0.62
  • 2-/4-, 2-/4-hydroxylation.