TABLE 1

Kinetic parameters of esculetin (ET) and 4-methylesculetin (4-ME) glucuronidation obtained from recombinant UGT1A6 and UGT1A9 and human liver and intestinal microsomes (HLM and HIM)

Kinetic parameters were obtained using simple Michaelis-Menten models as described in Materials and Methods.

CompoundsKinetic ParametersUGT1A6UGT1A9HLMHIM
ETKm (µM)185.59134.75134.19189.33
Vmax (nmol/min/mg)127.4019.2372.6130.45
CL(Vmax/Km, ml/min/mg)0.690.140.540.16
R20.98230.97750.98330.9738
AIC40.9814.0529.5326.69
4-MEKm (µM)172.5125.20117.81129.12
Vmax (nmol/min/mg)24.700.9969.913.88
CL(Vmax/Km, ml/min/mg)0.140.040.590.03
R20.98240.97930.98790.9918
AIC15.21−41.4934.75−26.16
  • AIC, Akaike’s information criterion.