TABLE 1

Comparison of phase I and phase II enzyme gene expression between Fa2N-4 cells and cryopreserved human hepatocytes

The gene expression levels were evaluated in human hepatocytes and Fa2N-4 cells after the 24- and 48-h adaptation periods, respectively. Data are expressed as means ± S.E.-fold change in human hepatocytes compared with Fa2N-4 cells determined from three independent experiments, as described under Materials and Methods.

PubMed ID
Gene
mRNA Expression Levels Relative to Fa2N-4
527
455
LHO
DMQ
NM_000499 CYP1A1 23.79 ± 9.88* 11.71 ± 1.90* 62.11 ± 28.75* 15.83 ± 3.88*
NM_000761 CYP1A2 19.26 ± 6.08* >100c,* 97.67 ± 0.74* >100c,*
NM_000762 CYP2A6 4.12 ± 0.18* 0.70 ± 0.34 0.42 ± 0.24 48.11 ± 18.00*
NM_000767 CYP2B6 a 3.95 ± 0.66* 2.87 ± 0.84 2.70 ± 0.57 10.24 ± 0.66*
NM_000769 CYP2C19 b 2.05 ± 0.56 0.38 ± 0.21* 1.03 ± 0.04 2.07 ± 0.33
NM_000770 CYP2C8 2.09 ± 0.86 3.34 ± 0.59* 2.70 ± 1.00* 25.57 ± 6.35*
NM_000771 CYP2C9 a 1.05 ± 0.46 0.66 ± 0.10* 1.07 ± 0.18 2.02 ± 1.12
NM_000106 CYP2D6 5.33 ± 1.01* 3.6 ± 1.9* 6.05 ± 0.14* 32.90 ± 13.53*
NM_000773 CYP2E1 19.81 ± 2.88* 45.78 ± 15.03* 92.66 ± 18.68* >100c,*
NM_017460 CYP3A4 a 0.75 ± 0.39 0.27 ± 0.03* 18.19b 6.61 ± 2.86
NM_022820 CYP3A43 0.64 ± 0.71 32.01 ± 6.22 3.34 ± 4.47 2.60 ± 2.26
NM_000777 CYP3A5 b 0.56 ± 0.15* 2.56 ± 1.12* 3.58d 24.31 ± 6.87*
NM_000765 CYP3A7 34.38 ± 8.84* N.D. 62.0 ± 5.0 25.38d
NM_023944 CYP4F12 1.50 ± 0.05 0.48 ± 0.06* 1.43 ± 0.15 2.28 ± 1.40
NM_000846 GSTA2 a 2.03 ± 0.59* 0.46 ± 0.05* 5.23 ± 0.53* 9.08 ± 2.48*
NM_000847 GSTA3 >100c,* 0.70 ± 0.09 6.12 ± 2.65* 38.91 ± 1.10*
NM_177536 SULT1A1 4.76 ± 3.54 >100c,d 44.37 ± 72.77 0.94 ± 0.17
NM_177528 SULT1A2 1.31 ± 1.11 5.14 ± 0.48* 29.01 ± 23.84 6.63 ± 0.62*
NM_024044 SULT1A3;GIYD2;GIYD1 a 0.21 ± 0.07* 0.11 ± 0.06* 0.30 ± 0.05* 0.64 ± 0.12*
NM_014465 SULT1B1 0.05 ± 0.04 3.26 ± 2.44 0.07 ± 0.03* 0.01 ± 0.00*
NM_005420 SULT1E1 a 0.02 ± 0.01 0.00 ± 0.00* 0.04 ± 0.01* 0.07 ± 0.04*
NM_003167 SULT2A1 0.77 ± 0.21 0.27 ± 0.04* 0.78 ± 0.22 4.06 ± 1.37*
NM_000367 TPMT 0.43 ± 0.18* 0.11 ± 0.04* 0.15 ± 0.02* 0.31 ± 0.08*
NM_000463 UGT1A1 1.25 ± 0.06* 2.68 ± 0.98* 1.38 ± 0.26* 3.96 ± 1.47*
NM_001072 UGT1A6 a , b 26.79 ± 5.61* 5.42 ± 0.97* 19.33 ± 1.98* 18.83 ± 9.60*
NM_019076 UGT1A8 0.78 ± 0.55 0.34 ± 0.22* 0.47 ± 0.19 0.94 ± 0.47
NM_001076 UGT2B15 17.64 ± 5.91* 13.3 ± 7.0* 19.98 ± 6.83* >100c,*
NM_021139 UGT2B4 60.95 ± 31.57* 75.48 ± 13.65* >100c,* >100c,*
NM_001074
UGT2B7
9.96 ± 1.06*
1.42 ± 0.11
1.67 ± 0.57
18.14 ± 2.60*

  • N.D., no data.

  • ↵* P < 0.05, ΔCt value significantly different from that for Fa2N-4 cells.

  • ↵ a Fa2N-4 cells gene expression increased > 10-fold during the 48-h adaptation period.

  • ↵ b Cryopreserved human hepatocyte gene expression increased > 10-fold during the 24-h adaptation period.

  • ↵ c Low gene expression in Fa2N-4 cells (Ct > 34).

  • ↵ d Data are expressed as the average value of experiments performed in duplicate.