Kinetic parameters for the formation of acyl glucuronides of BVM with recombinant human UGTs and pooled human liver and intestinal microsomes
Data were measured by LC-ESI-MS and are expressed as the means of duplicates.
Enzyme Source and Glucuronide | Vmax | Km | Vmax/Km |
|---|---|---|---|
| pmol/min/mg protein | μM | μl/min/mg protein | |
| UGT1A3 | |||
| Mono-BVMG (I) | 65 | 13 | 5.0 |
| Mono-BVMG (II) | N.D. | N.D. | N.D. |
| UGT1A4 | |||
| Mono-BVMG (I) | 1.8 | 5.6 | 0.32 |
| Mono-BVMG (II) | N.D. | N.D. | N.D. |
| UGT2B7 | |||
| Mono-BVMG (I) | 6.1 | 6.0 | 1.0 |
| Mono-BVMG (II) | 6.5 | 7.8 | 0.83 |
| HLMs | |||
| Mono-BVMG (I) | 61 | 27 | 2.3 |
| Mono-BVMG (II) | 48 | 16 | 3.1 |
| HIMs | |||
| Mono-BVMG (I) | N.D. | N.D. | N.D. |
| Mono-BVMG (II) | 90 | 8.3 | 11 |
N.D., not detected.