Substrate | Glucuronide Formation |
---|---|
pmol/min/mg of protein | |
Coumarins | |
Umbelliferone | 152 |
4-Methylumbelliferone | 400 ± 70 |
Esculetin | 225 |
Scopoletin | 1970 ± 300 |
4-Hydroxycoumarin | ND4-a |
Flavonoids | |
Naringenin (0.2 mM) | 612 ± 59 |
Apigenin (0.2 mM) | 508 ± 17 |
Galangin | 610 |
Fisetin | 276 |
7-Hydroxyflavone | 604 |
Genestein | 131 |
Quercetin (0.2 mM) | 550 |
Anthraquinones | |
Anthraflavic acid | 608 |
Emodin | 149 |
Alizarin | 1072 |
Quinalizarin | 749 |
Sapogenins | |
Hecogenin | ND |
Tigogenin | ND |
Diosgenin | ND |
Phenolic compounds | |
4-Nitrophenol | 239 ± 19 |
1-Naphthol | 27 |
Thymol | 69 |
Eugenol | 61 |
2-Hydroxybiphenyl | 94 |
3-Hydroxybiphenyl | 130 |
4-Hydroxybiphenyl | 299 |
Propofol | ND |
Carboxylic acids | |
Ketoprofen | 61 |
(R)-Ibuprofen | 121 |
(S)-Ibuprofen | 83 |
Fenoprofen | 108 |
Naproxen | 39 |
Ciprofibrate | 84 |
Clofibrate | 10 |
Valproic acid | 9 |
Decanoic acid | 80 |
Dodecanoic acid | 114 |
Aliphatic alcohols | |
(±)-Menthol | ND |
Borneol | ND |
Hexafluoro-2-propanol | ND |
Assays were performed in pH 7.5 Tris buffer at 37°C for 0.25–1.0 hr, using whole-cell homogenates of HK293 cells expressing UGT1A3. The concentration of UDP-glucuronic acid was 2.0 mM, and the aglycone concentrations were 0.5 mM, unless otherwise noted. Enzymatic rates are expressed as the mean ± SD of determinations from three transfections or the average determinations using cell homogenates from two transfections.
↵4-a ND, glucuronide formation was not detected (limits of detection, 2.0 pmol/min/mg of protein).