TABLE 2

Effect of bergamottin, tTEPA, and 17EE on the bupropion hydroxylation and 7-EFC activities of P450s Δ2B6 and Δ2B6 K262R P450s Δ2B6 and Δ2B6 K262R were reconstituted with reductase as described under Materials and Methods. Bergamottin, tTEPA, and 17EE were present in the primary reaction mixture at concentrations of 10 μM, 100 μM, and 100 μM, respectively. NADPH was added to the primary reaction mixture to initiate the reaction.



Percentage of Control Activity Remaining

Bupropion Assay
7-EFC Assay
Δ2B6 Bergamottin 30 ± 1 34 ± 2
Δ2B6 K262R Bergamottin 31 ± 1 40 ± 3
Δ2B6 tTEPA 51 ± 2 55 ± 3
Δ2B6 K262R tTEPA 62 ± 3 81 ± 4
Δ2B6 17EE 61 ± 4 23 ± 3
Δ2B6 K262R 17EE
100 ± 0
100 ± 0