Table 3

Effect of selected flavone derivatives on luciferase induction in stably transfected Hepa cells

Compound designationInhibition of TCDD-induced luciferase3-aInductionof luciferase3-bRelative plating efficiency3-c
IC50 % of 1 nM TCDD % of control
I451  ± 635090
II11  ± 1195
III6  ± 0.30.4100
VIII396  ± 814100
IX46  ± 11100
XI53  ± 1099
  • 3-a Antagonism of TCDD-induced luciferase was determined at 150 pM TCDD plus 1 nM – 1 μM of each compound. Cells were harvested after 4 h of exposure (see Materials and Methods). Values shown are mean ± standard error from nonlinear fit to data from triplicate measurements.

  • 3-b Luciferase induction by each compound alone at 1 μM as a percent of induction by 1 nM TCDD (tested concurrently for each experiment).

  • 3-c Cells were exposed to 1 μM of each compound for 4 h, trypsinized, and aliquots of cells transferred to fresh plates; after 7 days, cells were fixed to the plates (methanol), stained with crystal violet, and colonies counted. Expressed as percent of solvent control plates, average of 3 plates.