Table 5.
Summary of apparent kinetic parameters of genistein glucuronidation in different rat microsomes and human UGT isoforms
Kinetic parameters | Sprague-Dawley rats | Human UGT isoforms | |||||||
---|---|---|---|---|---|---|---|---|---|
Duodenum | Jejunum | Ileum | Colon | Liver | UGT1A1 | UGT1A8 | UGT1A9 | UGT1A10 | |
Vmax1 (nmol/min/mg) | 1.445 | 3.171 | 1.423 | 0.435 | 3.713 | NA | 1.24 | 2.09 | 12.34 |
Km1 (μM) | 4.04 | 6.628 | 8.239 | 3.186 | 23.6 | NA | 2.24 | 1.29 | 1.04 |
Vmax1 /Km1 (ml/min/mg) | 0.357 | 0.478 | 0.172 | 0.136 | 0.157 | NA | 1.81 | 0.62 | 0.08 |
Vmax2 (biphasic) (nmol/min/mg) | 0.041 | 1.59E3 | 0.826 | ||||||
Km2 (μM) | 7.994 | 2.74E3 | 0.71E-7 | ||||||
Vmax-0 (autoactivation) (nmol/min/mg) | NA | 0.01 | |||||||
Vmax-d (autoactivation) (nmol/min/mg) | NA | 1.23 | |||||||
R2 | 0.998 | 0.995 | 0.963 | 0.995 | 0.989 | NA | 0.96 | 0.98 | 0.99 |
AIC | −55.67 | −19.13 | −21.85 | −53.61 | −17.9 | NA | −7.98 | −26.91 | −25.23 |