Table 2. Reverse Type I spectral changes and inhibition of EROD activities of human P450 1B1 with pyrenes, naphthalenes, phenanthrenes, and biphenyls.
Reverse Type I spectra | inhibition of EROD | |||
---|---|---|---|---|
chemicals | Ks (μM) | ΔAmax | ΔAmax/Ks | IC50 (μM) |
pyrene | 1.3 ± 0.1 | 0.044 ± 0.001 | 0.0338 | 0.025 ± 0.003 |
1EP | 2.9 ± 0.3 | 0.049 ± 0.005 | 0.0169 | 0.036 ± 0.005 |
2EP | 3.4 ± 0.2 | 0.071 ± 0.001 | 0.0209 | 0.038 ± 0.004 |
4EP | 4.0 ± 0.5 | 0.052 ± 0.004 | 0.0130 | 0.17 ± 0.03 |
1VP | 4.4 ± 0.3 | 0.092 ± 0.003 | 0.0209 | 0.15 ± 0.02 |
1PP | 2.7 ± 0.3 | 0.042 ± 0.002 | 0.0156 | 0.045 ± 0.005 |
naphthalene | ND | ND | ND | 26 ± 3.2 |
2EN | 15 ± 0.3 | 0.049 ± 0.002 | 0.0033 | 1.2 ± 0.2 |
1NMPE | 92 ± 10 | 0.074 ± 0.005 | 0.0008 | 1.2 ± 0.3 |
1NEPE | 88 ± 18 | 0.079 ± 0.009 | 0.0009 | 0.92 ± 0.15 |
2NPE | 97 ± 19 | 0.086 ± 0.008 | 0.0009 | 4.3 ± 0.6 |
2NMPE | 100 ± 17 | 0.090 ± 0.009 | 0.0009 | 2.1 ± 0.3 |
2NEPE | 110 ± 3.1 | 0.094 ± 0.016 | 0.0009 | 5.2 ± 0.7 |
Phenanthrene | 14 ± 1.7 | 0.044 ± 0.002 | 0.0031 | 0.51 ± 0.10 |
2EPh | 4.2 ± 0.5 | 0.080 ± 0.004 | 0.0190 | 0.21 ± 0.03 |
3EPh | 3.0 ± 0.3 | 0.071 ± 0.001 | 0.0237 | 0.16 ± 0.02 |
9EPh | 3.6 ± 0.4 | 0.071 ± 0.004 | 0.0197 | 0.12 ± 0.01 |
2PPh | 2.2 ± 0.2 | 0.067 ± 0.005 | 0.0305 | 0.15 ± 0.02 |
3PPh | 3.1 ± 0.4 | 0.060 ± 0.006 | 0.0194 | 0.067 ± 0.008 |
9PPh | 3.2 ± 0.4 | 0.049 ± 0.002 | 0.0153 | 0.16 ± 0.03 |
biphenyl | 140 ± 19 | 0.037 ± 0.008 | 0.0003 | 19 ± 2.3 |
4EB | 7.6 ± 1.2 | 0.023 ± 0.001 | 0.0030 | 2.2 ± 0.3 |
4PB | 12 ± 1.8 | 0.074 ± 0.008 | 0.0062 | 1.8 ± 0.2 |
4BuB | 54 ± 6.2 | 0.092 ± 0.007 | 0.0017 | 1.5 ± 0.3 |
2BPE | 114 ± 16 | 0.110 ± 0.009 | 0.0010 | 15 ± 0.2 |
4BPE | 83 ± 26 | 0.056 ± 0.010 | 0.0007 | 16 ± 0.3 |
2BMPE | 146 ± 15 | 0.130 ± 0.009 | 0.0009 | 12 ± 0.2 |
4BMPE | 13 ± 1.5 | 0.071 ± 0.002 | 0.0055 | 1.2 ± 0.1 |
22BDPE | 30 ± 4.5 | 0.018 ± 0.001 | 0.0006 | 12 ± 1.7 |
44BDPE | 23 ± 4.3 | 0.031 ± 0.002 | 0.0013 | 7.8 ± 1.0 |
ND, not detected at the highest concentration of 100 μM. Ks, ΔAmax, and IC50 values presented are the means ± SEs obtained from the experiments with 5-8 different concentrations of the chemicals.