TABLE 1

Glucuronidating activities of rat UGT1A7 and UGT1A8 towards 40 substrates

Glucuronidation activity was measured using crude membrane fractions prepared from either untransfected HEK control cells or HEK cells transfected with rat UGT1A7 or UGT1A8. The substrate concentration was 0.1 mM. Values are expressed as nanomoles of substrate converted per milligram per minute for three determinations performed with the same membrane preparation at different times. Substrates that were highly glucuronidated (>20% substrate conversion) are indicated by +++.


No.

Compound Name

Control (HEK Cells)

Mean UGT1A7

Mean UGT1A8
activity ± S.E.
1 10-OH BaP N.D. +++ +++
2 5-OH BaP N.D. +++ +++
3 12-OH BaP 0.04, 0.01 +++ +++
4 7-OH BaP N.D. +++ 2.08 ± 0.15
5 11-OH BaP N.D. +++ 1.33 ± 0.08
6 1-Naphthol 0.07, 0.004, 0.006 +++ 1.28 ± 0.12
7 1-OH BaP N.D. +++ 1.00 ± 0.04
8 4-OH BaP N.D. +++ 0.90 ± 0.23
9 6-OH BaP N.D. 0.45 ± 0.03 0.79 ± 0.26
10 4-Methylumbelliferone N.D. +++ 0.64 ± 0.01
11 7-OH coumarin N.D. +++ 0.64 ± 0.01
12 Chrysin N.D. +++ 0.40 ± 0.03
13 4-Nitrophenol N.D. +++ 0.33 ± 0.17
14 BaP-4,5 (±) diol N.D. +++ 0.28 ± 0.01
15 Quercetin 0.005, 0.03, 0.02 +++ 0.22 ± 0.05
16 9-OH BaP N.D. +++ 0.17 ± 0.07
17 Estriol 0.010, 0.03 +++ 0.15 ± 0.05
18 4-OH-biphenyl 0.01, 0.002, 0.008 +++ 0.07 ± 0.04
19 3-OH BaP 0.02, 0.02, 0.005 0.62 ± 0.01 0.06 ± 0.03
20 17β-Estradiol 0.002, 0.005 0.66 ± 0.01 0.05 ± 0.03
21 16α-OH pregnenolone 0.001, 0.004 0.02 ± 0.01 0.05 ± 0.03
22 8-OH BaP N.D. 0.22 ± 0.04 0.03 ± 0.02
23 2-OH BaP N.D. +++ 0.03 ± 0.00
24 17β-Ethynylestradiol 0.009, N.D., 0.006 +++ 0.03 ± 0.01
25 Phenol red 0.001, 0.006 0.07 ± 0.01 N.D.
26 Dinitrocatechol N.D. 0.52 ± 0.03 N.D.
27 Estrone N.D. 0.17 ± 0.01 N.D.
28 4-OH estradiol 0.003, N.D. 0.05 ± 0.01 N.D.
29 Propofol 0.002, 0.001 +++ N.D.
30 BaP-7,8 (+) diol N.D. 0.52 ± 0.01 N.D.
31 BaP-7,8 (-) diol N.D. 0.57 ± 0.08 N.D.
32 Mycophenolic acid N.D. 0.05 ± 0.03 N.D.
33 Serotonin N.D. 0.15 ± 0.03 N.D.
34 Acetaminophen N.D. 0.03 ± 0.01 N.D.
35 Bisphenol A N.D. +++ N.D.
36 Bilirubin N.D. N.D. N.D.
37 Butylated hydroxytoluene N.D. 0.04 ± 0.00 N.D.
38 Butylated Hydroxyquinone N.D. 0.03 ± 0.00 N.D.
39 Buprenorphine N.D. 0.04 ± 0.00 N.D.
40
Epicatechin
N.D.
0.65 ± 0.19
N.D.
  • N.D., not detectable (<0.01 nmol/min/mg protein).