Figure 6.
Time courses of the hydrolysis of raloxifene mono- and disulfate by human placental sulfatase (STS). Expressed human SULT2A1 and SULT1E1 were used to generate the two raloxifene monosulfates and the disulfate radiolabeled with 35S-PAPS. The 35S-labeled raloxifene products were then used as substrates for hydrolysis by STS. The formation and hydrolysis of the raloxifene monosulfates and disulfates were analyzed by HPLC. Panel A; STS hydrolysis of the single raloxifene monosulfate formed by SULT2A1. Panel B; STS hydrolysis of the monosulfates and disulfate of raloxifene formed by SULT1E1 at a raloxifene concentration of 10 μM. SULT1E1 with 10 μM raloxifene forms mostly monosulfates with a ratio of approx. 8:1, and only a relatively low level of the disulfate; Panel C. STS hydrolysis of the monosulfates and disulfate of raloxifene formed by SULT1E1 at a raloxifene concentration of 2.5 μM. SULT1E1 with 2.5 μM raloxifene forms mostly the disulfate.
