Table 1

Comparison of in vivo and in vitro induction of rat liver CYP enzymes by prototypical inducers

P-450 Enzyme1-aIn Vivo Induction in Male Rats1-bIn Vitro Induction in Hepatocytes1-c
Control Activity1-dInduced ActivityControl ActivityInduced Activity
CYP1A152  ± 273,320  ± 18324.0  ± 15.3513  ± 12.0
CYP2B23.8  ± 4.21,460  ± 1802.25  ± 2.1615  ± 101
CYP3A2,460  ± 78012,693  ± 2,255208  ± 602,670  ± 410
CYP4A489  ± 5210,693  ± 620430  ± 802,700  ± 600
  • 1-a The enzyme activities of CYP1A, CYP2B, CYP3A, and CYP4A enzymes were determined as 7-ethoxyresorufinO-dealkylation, 7-pentoxyresorufinO-dealkylation, testosterone 6β-hydroxylation, and lauric acid 12-hydroxylation, respectively (Pearce et al., 1996).

  • 1-b Liver microsomes from male Sprague-Dawley rats treated with P-450 enzyme inducers. Rats were dosed once per day for 4 days with isotonic saline, β-naphthoflavone, phenobarbital, dexamethasone, or clofibric acid at a dosage of 5, 100, 80, 50, and 200 mg/kg, respectively. Data on the activity of P-450 enzymes were provided by XenoTech, LLC (Kansas City, KS).

  • 1-c Liver microsomes from cultured rat hepatocytes were treated with P-450 enzyme inducers and activity of P-450 enzymes was determined as described in Experimental Procedures. Data are the means ± S.E. from three separate experiments (Fig. 8).

  • 1-d Activities are reported as pmol/min/mg protein and are averages of duplicate determinations from three to five experiments.