Table 1.
Kinetic parameters of isoliquiritigenin glucuronidation by human liver microsomes (HLM) and recombinant UGT enzymes.
Enzyme | Metabolite | Km or S50 | Vmax | CLint | Ksi | |
---|---|---|---|---|---|---|
(µM) | (nmol/min/mg protein) | (µL/min/mg protein) | (µM) | |||
HLM | MG4 a | 2.84 ± 0.42 | 0.25 ± 0.01 | 88.0 | 168.34 ± 39.52 | |
MG5 a | 8.42 ± 1.21 | 1.47 ± 0.11 | 174.6 | 143.53 ± 31.36 | ||
UGT1A1 | MG4 a | 2.98 ± 0.80 | 1.01 ± 0.16 | 338.9 | 10.89 ± 2.92 | |
MG5 a | 4.30 ± 0.47 | 1.77 ± 0.08 | 411.6 | 189.1 ± 36.0 | ||
UGT1A9 | MG4 b | 8.59 ± 1.43 | 0.14 ± 0.01 | 16.3 | ||
MG5 c | 3.15 ± 0.24 | 0.86 ± 0.02 | 273.0 | |||
UGT1A10 | MG4 b | 25.75 ± 1.28 | 2.13 ± 0.04 | 89.3 | ||
MG5 b | 26.15 ± 2.25 | 0.57 ± 0.02 | 21.8 |
Each value represents Mean ± Std. Error (N = 3)
Substrate inhibition
Michaelis-Menten
Hill equation (n = 1.20 ± 0.08)