Inhibitors | DM-221 Formed | DM-222 Formed |
---|---|---|
pmol/min/mg | ||
Control | 3.9 ± 0.1 (100) | 3.9 ± 0.1 (100) |
α-Naphthoflavone | 3.8 ± 0.1 (96) | 3.8 ± 0.1 (98) |
Sulfaphenazole | 4.1 ± 0.1 (104) | 4.3 ± 0.1 (111) |
S-Mephenytoin | 3.8 ± 0.1 (98) | 3.4 ± 0.1 (88) |
Quinidine | 1.1 ± 0.0 (28) | 1.2 ± 0.2 (30) |
Diethyldithiocarbamate | 4.2 ± 0.9 (108) | 3.0 ± 0.3 (76) |
Troleandomycin | 3.6 ± 0.0 (90) | 3.8 ± 0.1 (98) |
DM-215 was incubated with the microsomes for 30 min at 37 °C in the presence of various inhibitors. Each inhibitor was added to the incubation mixture at 100 μM, except for α-naphthoflavone (1 μM). Enzyme incubation and metabolite analysis were carried out in triplicate, and the data were expressed as means ± S.D. Numbers in parentheses represent the relative activities.