FIG. 2.
Modulation of catalytic activity of CYP1A1, CYP1A2, and CYP3A4 by DIM and 8PN in vitro. EROD (B), MROD (A), and BROD (C) activities were determined using microsomes from recombinant yeast strains expressing human CYP1A1, CYP1A2, and Supersomes (Gentest) expressing human CYP3A4, respectively, after adding increasing concentrations of DIM or 8PN. Values are expressed as % inhibition relative to solvent controls. Means and corresponding SDs are derived from two independent inhibition experiments (with six measurements per experiment). All inhibition mean values at phytochemical concentrations at 1.5μM and higher were statistically significant (p < 0.01), as well as 8PN at 0.15 and 0.5μM in MROD and DIM and 8PN both at 0.5μM in EROD. IC50 values for 8PN were approximately 4.5, 1.7, and 8.4μM for CYP1A2, CYP1A1, and CYP3A4, respectively. IC50 values for DIM were 40.9, 21.4, and 14.5μM for CYP1A2, CYP1A1, and CYP3A4, respectively.
