TABLE 2

Drug metabolizing enzyme activities (picomoles per minute per milligram protein) in CHIM

Means and S.E.s (S.E.M.) of CHIM from four donors are shown. The results are derived from those previously published (Li et al., 2018a).

Drug metabolizing enzymeSubstrateSubstrate conc. (µM)Marker metaboliteMeanS.E.M.
CYP1A17-Ethoxyresozufin20Resozufin0.260.13
CYP1A2Phenacetin100Acetaminophen3.340.89
CYP2A6Coumarin507-HC, 7-HC-sulfate, 7-HC-glucuronideNANA
CYP2B6Buproprion500Hydroxybuproprion0.690.11
CYP2C8Paclitaxel (taxol)206α-Hydroxypaclitaxel0.120.02
CYP2C9Diclofenac254-OH diclofenac0.390.05
CYP2C19S-mephenytoin2504-OH S-mephenytoin0.860.26
CYP2D6Dextromethorphan15Dextrophan0.040.02
CYP2E1Chlorzoxazone2506-OH chlorzoxazone0.040.01
CYP2J2Astemizole50O-demethyl astemizole2.270.31
CYP3A4-1Midazolam201-Hydroxymidazolam1.830.65
CYP3A4-2Testosterone2006β-Hydroxytestosterone24.825.47
ECOD7-Ethoxycoumarin1007-HC, 7-HC-sulfate, 7-HC-glucuronide0.810.24
UGT7-Hydroxycoumarin1007-Hydroxycoumarin glucuronide0.710.26
SULT7-Hydroxycoumarin1007-Hydroxycoumarin sulfate1.850.44
GSTAcetaminophen10 mMAcetaminophen glutathione0.260.09
UGTAcetaminophen10 mMAcetaminophen glucuronide1.040.51
SULTAcetaminophen10 mMAcetaminophen sulfate4.520.84
FMOBenzydamine HCl250Benzydamine-N-oxide8.110.99
MAOKynuramine HBr1604-Hydroxyquinoline317.0980.12
AOCabazeran204-Hydroxycabazeran0.020.00
NAT14-Aminobenzoic acid200N-acetyl-p-aminobenzoic acid2.170.58
NAT2Sulfamethazine100N-acetyl-sulfamethazine1.460.16
CES2Irinotecan50SN381.210.13
  • ECOD, 7-ethoxycoumarin O-deethylase; NA, no activity.