Table 1

Kinetic analysis of substrate glucuronidation in alamethicin-pretreated mixture of human liver microsomes

MetaboliteKmappVmaxappn1-aModel
mM nmol/mg protein/min
E3G0.017  ± 0.0010.40  ± 0.021.79  ± 0.11Hill
E17G0.006  ± 0.0010.32  ± 0.02n/a1-b Michaelis-Menten
APAPG4.1  ± 0.91.50  ± 0.231.37  ± 0.09Hill
M3G5.2  ± 0.82.48  ± 0.28n/a1-b Michaelis-Menten

Microsomes from a mixture of four human livers were pretreated with alamethicin (50 μg/mg protein) and incubated with various concentrations of substrates as described in Materials and Methods. Incubations were analyzed as described, and the data was fit where appropriate to either Michaelis-Menten or Hill kinetics. Kinetic plots are presented in Fig. 4.

  • 1-a n = Hill constant.

  • 1-b n/a = not applicable.