TABLE 4
Structures of compounds that modulate UGT1A1 enzyme activity in vitro
Compound | Structure | In Vitro IC50a | Reference |
|---|---|---|---|
| Tangeretin |
| 1 | Williams et al. (2002) |
| Silybin |
| 1b | Goosen et al. (2004) |
| Chrysin |
| <10 | Williams et al. (2002) |
| Nobiletin |
| >10 | Williams et al. (2002) |
| Bilirubin |
| <30 | Williams et al. (2002) |
| 17α-Ethinylestradiol |
| Stimulation | Williams et al. (2002) |
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↵ a Pooled human liver microsomes using estradiol 3-glucuronidation as a marker for UGT1A1 activity (Williams et al., 2002) unless indicated
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↵ b Recombinant UGT1A1 using HFC as substrate (Goosen et al., 2004). Ethinylestradiol stimulation of estradiol 3-glucuronidation was maximal (180% of control activity) at the lowest tested ethinylestradiol concentration (5 μM)