TABLE 3.
P450 inhibition of demethyl-IQ formation by liver microsomes from BNF-treated mice
Incubations were conducted for 30 min at 37°C with 0.06 mM IQ. Furafylline was preincubated for 10 min before addition of IQ. For those incubations, the control microsomal activity was 0.25 ± 0.01 nmol, which is not different from the control value above. Data are expressed as mean nanomole of demethyl-IQ ± S.E. with n = 3.
| Test Agents | Type of P450 Inhibitor | Concentration | Activity | % of Total |
|---|---|---|---|---|
| μM | nmol | |||
| Control | 0.26 ± 0.04 | 100 | ||
| Ellipticine | 1A | 10 | 0.03 ± 0.01* | 12 |
| 20 | N.D. | 0 | ||
| Furafylline | 1A2 | 20 | 0.22 ± 0.01 | 85 |
| α-Naphthoflavone | 1A | 20 | 0.20 ± 0.01 | 77 |
| 100 | 0.15 ± 0.02* | 58 | ||
| SKF-525A | Nonspecific | 20 | 0.19 ± 0.04 | 73 |
| 100 | 0.12 ± 0.02* | 46 | ||
| Ketoconazole | 3A | 20 | 0.17 ± 0.02* | 65 |
| 100 | 0.07 ± 0.04* | 27 | ||
| Sulfaphenazole | 2C | 20 | 0.19 ± 0.05 | 73 |
| 100 | 0.20 ± 0.03 | 77 |
N.D., not detected.
p < 0.05 compared with control.