Table 1

The inhibition of UGT1A1 glucuronidation

AglyconeInhibitor
ControlEtonitazenyl (100 μM)Buprenorphine (100 μM)
pmol/min/mg protein
Anthraflavic acid (20 μM)222  ± 4204  ± 21234  ± 6
2-Hydroxyestrone (25 μM)197  ± 10133  ± 13178  ± 8

Assays were performed at 37°C, at optimal pH and incubation times using membrane preparations from cells expressing UGT1A1. The concentration of UDP-glucuronic acid was 2.0 mM and the aglycone concentrations are indicated. The enzyme rates are expressed as the mean ± S.D. of three experiments.