Table 3.
Kinetic parameters derived for the corylin glucuronides (M7) of corylin by HLM, HIM, expressed UGT enzymes, MkLM, RLM, MLM, DLM, GpLM and RaLM (Mean ± SD). All experiments were performed in triplicate.
| Enzyme | Meta. | Vmax (pmol/min/mg) | Km (mM) | Ki(μM) | CLint (μL/min/mg) | Model |
|---|---|---|---|---|---|---|
| HLM | M7 | 660.1 ± 31.75 | 5.27 ±0.46 | 54.97 ± 6.85 | 125.33 ± 12.58 | SI |
| HIM | M7 | 353.2 ± 9.71 | 3.25 ±0.33 | N.A. | 108.74± 11.30 | MM |
| UGT1A1 | M7 | 390.8 ± 29.15 | 3.20 ±0.50 | 62.12 ±13.98 | 122.32 ± 21.07 | SI |
| UGT1A3 | M7 | 76.99 ±3.80 | 3.83 ±0.37 | 41.63 ± 4.95 | 20.11 ± 2.16 | SI |
| UGT1A8 | M7 | 83.76 ±3.06 | 25.59 ±1.94 | N.A. | 3.27 ± 0.28 | MM |
| MkLM | M7 | 1477.0± 94.32 | 9.80 ±0.90 | 17.32 ± 1.7 | 150.78 ±16.83 | SI |
| RLM | M7 | 211.1 ± 17.75 | 4.20 ±0.57 | 13.71 ± 1.95 | 50.24 ± 8.00 | SI |
| MLM | M7 | 929.9 ± 124.3 | 8.22 ±1.65 | 20.07 ± 4.50 | 113.07 ± 27.24 | SI |
| DLM | M7 | 534.2 ± 8.68 | 5.84 ±0.30 | N.A. | 91.52 ± 4.00 | MM |
| GpLM | M7 | 1424.0 ±27.57 | 7.73 ±0.44 | N.A. | 184.24 ±11.13 | MM |
| RaLM | M7 | 654.7 ± 40.13 | 7.34 ±0.73 | 33.93 ±4.17 | 89.26 ±10.43 | SI |
Note: Meta., metabolites; N.A., not available; HLM, human liver microsomes; HIM, human intestine microsomes; MkLM, monkey liver microsomes; RLM, rat liver microsomes; DLM, dog liver microsomes; GpLM, guinea pig liver microsomes; RaLM, rabbit liver microsomes; SI, substrate inhibition model; MM, Michaelis-Menten model.