TABLE 3

Enzyme kinetic parameters for the formation of major metabolites of CYP1A1, CYP1A2, CYP2C6, and CYP2C11

Data are the mean and S.E.E. (standard error of estimate), Vmax (in picomoles per picomoles of P450 per minute), Km and Ksi (in micromolars), and h were determined as per (eq. 4). Clint [intrinsic clearance (in microliters per minute per picomoles P450)] was calculated. as Vmax/Km.

CompoundVmaxKmKsihClintR2
CYP1A116-HETE1.79 ± 0.3641.6 ± 9.32132 ± 152.46 ± 0.610.040.88
17-HETE2.39 ± 0.4551.6 ± 10.5132 ± 152.30 ± 0.440.050.96
18-HETE3.77 ± 0.6048.3 ± 7.32132 ± 152.37 ± 0.320.080.96
19-HETE7.75 ± 1.0439.5 ± 4.77132 ± 152.27 ± 0.220.200.96
CYP1A216-HETE2.18 ± 0.1310.1 ± 0.82121 ± 5.332.71 ± 0.440.220.98
17-HETE0.44 ± 0.1411.3 ± 6.53121 ± 5.332.00 ± 0.550.040.99
18-HETE0.73 ± 0.119.92 ± 2.31121 ± 5.332.71 ± 1.410.070.98
19-HETE1.17 ± 0.119.76 ± 1.26121 ± 5.333.00 ± 1.000.120.98
CYP2C612-HETE2.65 ± 0.2918.3 ± 2.84142 ± 5.912.39 ± 0.550.140.96
15-HETE0.82 ± 0.1313 ± 2.02142 ± 5.915.40 ± 2.330.060.93
11,12-EET1.49 ± 0.4035.9 ± 18.5142 ± 5.911.44 ± 0.540.040.97
14,15-EET2.10 ± 0.3931.9 ± 11.1142 ± 5.911.46 ± 0.380.070.97
CYP2C115,6-EET4.99 ± 1.2690.2 ± 43.782.9 ± 5.051.33 ± 0.420.060.90
8,9-EET8.36 ± 1.2565.6 ± 10.682.9 ± 5.052.13 ± 0.290.130.97
11,12-EET12 ± 1.3860.1 ± 6.7882.9 ± 5.052.18 ± 0.200.200.96
14,15-EET7.77 ± 1.1462.3 ± 11.282.9 ± 5.051.89 ± 0.280.120.98