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IC50 values and inhibition constants (Ki) for ketoconazole and xenoestrogens on CYP1A- and CYP3A activities assayed in vitro. |
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| Compound(s) |
IC50(μM)1,a |
Ki(μM)1,a |
IC50(μM)2,b |
Ki(μM)2,b |
IC50(μM)3,b |
|
|
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| Ketoconazole (KC) |
0.6 (0.0)c |
0.04 – low [S] |
0.3 (0.1)c |
0.2 |
0.4c |
| 0.2 – high [S] |
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| Nonylphenol (NP) |
5.2 (1.1) |
3.5 |
160 (40) |
Not analysed |
35 |
| Ethynylestradiol |
20 (1.2) |
5.4 – low [S] |
40 (7.1) |
54 – low [S] |
50 |
| 10.3 – high [S] |
95 – high [S] |
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| KC:NP (1:5) |
1.3 (0.2):6.2 (1.0) |
Not analysed |
5.3 (1.1):25.0 (5.3) |
Not analysed |
Not analysed |
|
1 Hepatic Microsomal CYP1A activity; 2 Hepatic Microsomal CYP3A activity; 3 cDNA Expressed Human CYP3A4; a Substrate [S] = 7-Ethoxyresorufin; b [S] = 7-Benzyloxy-4-[trifluoromethyl]-coumarin; c Published in [22]. Each IC50 value represents the mean from 2–4 separate assays, followed by the SD, in brackets. The Ki values are estimated from one representative Dixon plot. | |||||
Hasselberg et al. Comparative Hepatology 2005 4:2 doi:10.1186/1476-5926-4-2 |
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