TABLE 3

Inhibition of estradiol-3-glucronidation (UGT1A1) or zidovudine (AZT) glucuronidation by structurally diverse compounds in human liver microsomes Experiments were performed according to the previously described methodology (Court et al., 2003). HMF and valproic acid concentrations were taken to the limits of solubility. Data are means of triplicate incubations of three separate experiments for each compound. Stimulation of estradiol 3-glucuronidation increased with increasing AZT concentration to a maximal 174% of control activity at the highest AZT concentration tested (3 mM).


Compound

Structure

UGT1A1 IC50

UGT2B7 IC50
μM μM
S-Flurbiprofen Embedded Image 349 186
Propofol Embedded Image 626 314
Estradiol Embedded Image N/A 300
3′,4′,5,5′,6,7-Hexamethoxyflavone (HMF) Embedded Image 0.84 >1000
Valproic acid Embedded Image 4100 >4100
Zidovudine (AZT)
Embedded Image
Stimulation
N/A