Figure 2. Glucuronide conjugation of bicalutamide enantiomers by microsomes from human liver, kidney and intestine.
Human liver, kidney or intestine microsomes (10 μg) were incubated in the presence of 100 μM of the racemic (R/S) mixture of bicalutamide (R/S, A and B), or of the pure (R)- (R, C) or (S)-enantiomers (S, D), and UDPGA (1 mM) for 18 hours at 37°C. The formation of (R)bicalutamide-glucuronide (R-G, A and C) and (S)bicalutamide-glucuronide (S-G, B and D) was analyzed by LC-MS/MS. Data represent the mean ± S.D. of two independent experiments performed in triplicate.
G: glucuronide.