TABLE 2

Summary of enzyme activity data for seven UGT enzymes in human liver microsomal samples (n = 59)

EnzymeProbe SubstrateMonitored MetaboliteUGT Activity Rates
Mean ± S.D. (%CV)Range (fold difference)
nmol min−1 mg−1 HLM protein
UGT1A1β-estradiolβ-estradiol-3-glucuronide0.895 ± 0.648 (72%)0.166– 4.173 (25)
UGT1A3Chenodeoxycholic acid (CDCA)CDCA-24-glucuronide14.980 ± 5.978 (40%)4.480–34.222 (8)
UGT1A4TrifluoperazineTrifluoperazine-N-glucuronide0.414 ± 0.155 (37%)0.175–0.856 (5)
UGT1A65-hydroxytryptophol5-hydroxytryptophol-O-glucuronide19.830 ± 5.924 (30%)8.860–38.200 (4)
UGT1A9PropofolPropofol-O-glucuronide2.296 ± 0.825 (36%)0.779–5.013 (6)
UGT2B7Zidovudinezidovudine-5′-glucuronide1.130 ± 0.344 (30%)0.559–2.307 (4)
UGT2B15S-oxazepamS-oxazepam glucuronide0.143 ± 0.072 (50%)0.057–0.395 (7)