Table 2.
Kinetic parameters derived for corylifol A-related glucuronides (M4) by HLM, expressed UGTs enzymes, RLM, MLM, DLM, MkLM and RaLM (Mean ± SD).
| Meta. | Vmax (pmol/min/mg) | Km (μM) | Ki (μM) | CLint (μL/min/mg) | Model | |
|---|---|---|---|---|---|---|
| HLM | M4 | 4837 ± 595.9 | 2.64 ± 0.58 | 18.15 ± 4.51 | 1829 ± 464.3 | SI |
| M5 | + | + | + | + | ||
| UGT1A1 | M4 | 148.0 ± 4.30 | 0.52 ± 0.06 | 53.70 ± 8.03 | 284.07 ± 26.67 | SI |
| UGT1A3 | M4 | + | + | + | + | |
| UGT1A4 | M4 | + | + | + | + | |
| UGT1A7 | M4 | 440.8 ± 8.78 | 5.19 ± 0.32 | N.A. | 85.01 ± 0.06 | MM |
| UGT1A8 | M4 | 3044 ± 902.7 | 22.45 ± 7.94 | 6.98 ± 2.59 | 135.59 ± 62.56 | SI |
| UGT1A9 | M4 | 776.4 ± 23.24 | 4.05 ± 0.26 | 75.26 ± 6.26 | 191.94 ± 13.40 | SI |
| M5 | ++ | ++ | ++ | ++ | ||
| UGT2B4 | M4 | ++ | ++ | ++ | ++ | |
| UGT2B7 | M4 | ++ | ++ | ++ | ++ | |
| RLM | M4 | 2563 ± 333.6 | 2.81 ± 0.58 | 8.82 ± 1.91 | 911.1 ± 223.6 | SI |
| MLM | M4 | 6119 ± 531.3 | 4.56 ± 0.62 | 15.44 ± 2.35 | 1340 ± 218.3 | SI |
| DLM | M4 | 3054 ± 283.5 | 3.47 ± 0.62 | 51.38 ± 13.84 | 879.1 ± 177.8 | SI |
| MkLM | M4 | 6812 ± 1366 | 8.00 ± 2.08 | 5.50 ± 1.47 | 851.5 ± 279.6 | SI |
| RaLM | M4 | 2859 ± 249.4 | 3.08 ± 0.43 | 11.13 ± 1.67 | 927.6 ± 154.5 | SI |
All experiments were performed in triplicate.
HLM: human liver microsomes; Meta.: metabolites; MM: Michaelis–Menten model; N.A.: not available; +: under the limit of quantification; ++: unable to determine the kinetic parameters in the absence of a full kinetic profile; SI: substrate inhibition model.