Table 3.
Enzymes | Substrate /Product(s) |
Vmax | Km | Ks | Vmax/Km (CLint) |
---|---|---|---|---|---|
nmol/mg/min | µM | µM | ml/min/mg | ||
UGT1A7 | 3,7DHF | ||||
3-O-glucuronide | 2.04 ± 0.07 | 1.61 ± 0.14 | 309.17 ± 127.39 | 1.27 | |
7-O-glucuronide | 0.44 ± 0.07 | 23.17 ± 6.96 | N/A | 0.02 | |
3,5,7THF | |||||
3-O-glucuronide | 3.35 ± 0.11 | 0.82 ± 0.08 | 55.75 ± 7.27 | 4.09 | |
7-O-glucuronide | 2.46 ± 0.34 | 21.43 ± 6.09 | N/A | 0.11 | |
3,5,7,4’QHF | |||||
3-O-glucuronide | 0.77 ± 0.04 | 1.46 ± 0.32 | N/A | 0.53 | |
7-O-glucuronide | 1.10 ± 0.11 | 11.56 ± 2.91 | N/A | 0.10 | |
UGT1A8 | 3,7DHF | ||||
3-O-glucuronide | 0.76 ± 0.04 | 8.68 ± 1.21 | N/A | 0.09 | |
7-O-glucuronide | 0.65 ± 0.10 | 27.32 ± 7.50 | N/A | 0.02 | |
3,5,7THF | |||||
3-O-glucuronide | 3.89 ± 0.47 | 6.44 ± 1.28 | 37.28 ± 10.12 | 0.60 | |
7-O-glucuronide | 0.79 ± 0.57 | 4.88 ± 1.14 | N/A | 0.16 | |
3,5,7,4’QHF | |||||
3-O-glucuronide | 0.74 ± 0.04 | 2.39 ± 0.47 | N/A | 0.31 | |
7-O-glucuronide | 1.01 ± 0.09 | 6.77 ± 1.78 | N/A | 0.15 | |
UGT1A9 | 3,7DHF | ||||
3-O-glucuronide | 4.60 ± 0.28 | 0.22 ± 0.04 | 30.13 ± 7.11 | 20.91 | |
7-O-glucuronide | 2.04 ± 0.09 | 1.50 ± 0.26 | N/A | 1.36 | |
3,5,7THF | |||||
3-O-glucuronide | 7.41 ± 0.89 | 0.68 ± 0.16 | 7.43 ± 2.12 | 10.90 | |
7-O-glucuronide | 2.56 ± 0.10 | 0.54 ± 0.08 | N/A | 4.74 | |
3,7,4’THF | |||||
3-O-glucuronide | 2.62 ± 0.05 | 0.36 ± 0.03 | N/A | 7.28 | |
7-O-glucuronide | 1.15 ± 0.08 | 2.67 ± 0.56 | N/A | 0.43 | |
3,5,7,4’QHF | |||||
3-O-glucuronide | 1.92 ± 0.03 | 0.32 ± 0.03 | N/A | 6.00 | |
7-O-glucuronide | 0.87 ± 0.05 | 3.87 ± 0.59 | N/A | 0.22 | |
UGT1A10 | 3,7DHF | ||||
3-O-glucuronide | 0.19 ± 0.01 | 6.66 ± 0.66 | N/A | 0.03 | |
7-O-glucuronide | 0.26 ± 0.02 | 8.74 ± 1.37 | N/A | 0.03 | |
3,5,7THF | |||||
3-O-glucuronide | 2.01 ± 0.14 | 4.49 ± 0.61 | 73.48 ± 17.82 | 0.45 | |
7-O-glucuronide | 0.77 ± 0.04 | 3.96 ± 0.58 | N/A | 0.19 | |
3,5,7,4’QHF | |||||
3-O-glucuronide | 1.46 ± 0.16 | 2.44 ± 0.55 | 30.01 ± 8.00 | 0.60 | |
7-O-glucuronide | 1.10 ± 0.20 | 3.34 ± 1.21 | 51.37 ± 27.15 | 0.33 |
Data are means ± S.E. of three determinations. N/A means that parameter Ks was not available; this was for the cases in which data fitted better to Michaelis-Menten equation