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 enzyme | Substrate | Substrate conc. (µM) | Marker metabolite | Mean | S.E.M. |
---|---|---|---|---|---|
CYP1A1 | 7-Ethoxyresozufin | 20 | Resozufin | 0.26 | 0.13 |
CYP1A2 | Phenacetin | 100 | Acetaminophen | 3.34 | 0.89 |
CYP2A6 | Coumarin | 50 | 7-HC, 7-HC-sulfate, 7-HC-glucuronide | NA | NA |
CYP2B6 | Buproprion | 500 | Hydroxybuproprion | 0.69 | 0.11 |
CYP2C8 | Paclitaxel (taxol) | 20 | 6α-Hydroxypaclitaxel | 0.12 | 0.02 |
CYP2C9 | Diclofenac | 25 | 4-OH diclofenac | 0.39 | 0.05 |
CYP2C19 | S-mephenytoin | 250 | 4-OH S-mephenytoin | 0.86 | 0.26 |
CYP2D6 | Dextromethorphan | 15 | Dextrophan | 0.04 | 0.02 |
CYP2E1 | Chlorzoxazone | 250 | 6-OH chlorzoxazone | 0.04 | 0.01 |
CYP2J2 | Astemizole | 50 | O-demethyl astemizole | 2.27 | 0.31 |
CYP3A4-1 | Midazolam | 20 | 1-Hydroxymidazolam | 1.83 | 0.65 |
CYP3A4-2 | Testosterone | 200 | 6β-Hydroxytestosterone | 24.82 | 5.47 |
ECOD | 7-Ethoxycoumarin | 100 | 7-HC, 7-HC-sulfate, 7-HC-glucuronide | 0.81 | 0.24 |
UGT | 7-Hydroxycoumarin | 100 | 7-Hydroxycoumarin glucuronide | 0.71 | 0.26 |
SULT | 7-Hydroxycoumarin | 100 | 7-Hydroxycoumarin sulfate | 1.85 | 0.44 |
GST | Acetaminophen | 10 mM | Acetaminophen glutathione | 0.26 | 0.09 |
UGT | Acetaminophen | 10 mM | Acetaminophen glucuronide | 1.04 | 0.51 |
SULT | Acetaminophen | 10 mM | Acetaminophen sulfate | 4.52 | 0.84 |
FMO | Benzydamine HCl | 250 | Benzydamine-N-oxide | 8.11 | 0.99 |
MAO | Kynuramine HBr | 160 | 4-Hydroxyquinoline | 317.09 | 80.12 |
AO | Cabazeran | 20 | 4-Hydroxycabazeran | 0.02 | 0.00 |
NAT1 | 4-Aminobenzoic acid | 200 | N-acetyl-p-aminobenzoic acid | 2.17 | 0.58 |
NAT2 | Sulfamethazine | 100 | N-acetyl-sulfamethazine | 1.46 | 0.16 |
CES2 | Irinotecan | 50 | SN38 | 1.21 | 0.13 |
ECOD, 7-ethoxycoumarin O-deethylase; NA, no activity.