Screening analysis of exogenous compounds glucuronidated by the UGT2B17 enzyme
| Substrates | Screening | Substrates | Screening |
|---|---|---|---|
| Coumarins | Monoterpenoid | ||
| 4-Methylumbelliferone | + | Borneol | + |
| Umbelliferone | + | Menthol | + |
| Scopoletin | + | Harmol | − |
| Esculetin | − | Opioids | |
| 4-OH-coumarin | − | Codeine | − |
| NSAID | Morphine | − | |
| Acetyl salicylic acid | − | Naltrexone | − |
| Ibuprofen | + | Other | |
| Indomethacin | − | Chloramphenicol | − |
| Salicylic acid | − | 17β-Ethynylestradiol | − |
| Anthraquinones | Hydroxyflutamide | − | |
| Anthraflavic acid | + | Furosemide | − |
| Quinizarin | − | 6-Hydroxyquinoline | − |
| Emodin | + | 8-Hydroxyquinoline | − |
| Alizarin | + | Hecogenin | − |
| Benzodiazepins | Phenolic compounds | ||
| Chlordiazepoxide (Librium) | − | 4-Ethyl phenol | + |
| Diazepam (Valium) | − | 4-Propyl phenol | + |
| Lorazepam (Ativan) | − | 4-T-buthyl phenol | − |
| Oxazepam (Serax) | − | Eugenol | + |
| Flavonoids | 1-Naphthol | + | |
| 7-Hydroxyflavone | + | p-Nitrophenol | + |
| Naringenin | − | Phenol red | + |
| Chrysin | + | Acetaminophen | − |
| Galangin | + | Caffeic acid | − |
| Apigenin | − | Ferrulic acid | − |
| Baicalein | − | Pyrogallol | − |
| Fisetin | − | Carvacrol | − |
| Quercetin | − | Thymol | − |
| Genistein | − | Amines | |
| Biochenin A | − | α-Naphtylamine | − |
| Naringin | + |
To screen for substrates that react with the UGT2B17 enzyme, 200 μM of each compound was incubated in the presence of 15 μM [14C]UDPGA, 100 μM unlabeled UDPGA for 16 h at 37oC, and 11 μg of microsomal proteins from HK293 cells stably expressing UGT2B17 enzyme. +, glucuronidation activity was observed; −, no conjugation was observed.