TABLE 6

Regioselectivity of UGT1A3 enzymes to quercetin (n = 3)

Vmax and Vmax/Km are normalized by expression levels of recombinant UGT1A3s. Relative catalytic efficiency of each UGT1A3 enzyme is indicated as percentage of 7-glucuronide.


Monoglucuronide

UGT1A3.1a

UGT1A3.2

UGT1A3.3

UGT1A3.4

UGT1A3.5
Vmax/Km
Percentage of 7-Glucuronide
Vmax/Km
Percentage of 7-Glucuronide
Vmax/Km
Percentage of 7-Glucuronide
Vmax/Km
Percentage of 7-Glucuronide
Vmax/Km
Percentage of 7-Glucuronide
μl/mg/min μl/mg/min μl/mg/min μl/mg/min μl/mg/min
7-Glucuronide 8.310 ± 0.87 100 2.574 ± 0.17 100 1.214 ± 0.13 100 66.60 ± 5.87 100 20.32 ± 0.42 100
3-Glucuronide 10.51 ± 0.61 126 2.073 ± 0.17 84 1.327 ± 0.05 110 158.7 ± 10.8 238 16.26 ± 0.90 80
4′-Glucuronide 9.216 ± 0.14 111 0.423 ± 0.04 16 1.908 ± 0.10 158 5.866 ± 0.27 9 1.330 ± 0.02 7
3′-Glucuronide
22.01 ± 0.90
265
0.461 ± 0.02
18
6.929 ± 0.34
573
1.067 ± 0.10
2
0.787 ± 0.07
4