TABLE 3

Inhibitory effect of genistein and apigenin on glucuronidation of raloxifene by human and rat jejunal microsomes and Caco-2 cell lysate Raloxifene (4.34 μM) and inhibitor (0∼100 μM genistein or apigenin) were added to the microsomes with cofactors as described under Materials and Methods. Apparent 50% inhibitory concentration (IC50) values were obtained by nonlinear regression of the data presented in Fig. 7 using SigmaPlot.


Compound

Microsome

Glucuronide

Apparent IC50
μM
Genistein Human jejunum M1 51.57
M2 44.90
Rat jejunum M1 4.66
M2 9.42
Caco-2 cell lysate M1 7.78
M2 8.19
Apigenin Human jejunum M1 14.80
M2 16.70
Rat jejunum M1 5.02
M2 3.39
Caco-2 cell lysate M1 1.87


M2
2.14