FMO1 | Donor 1 | Donor 2 | Donor 3 | Donor 4 | Donor 5 | |
---|---|---|---|---|---|---|
pmol/min/mg microsomal protein | ||||||
MeDDC Sulfine Formation | ||||||
MeDDC, 5 μM | ||||||
Control | 2870 ± 60 (100) | 200 ± 20 (100) | 160 ± 0 (100) | 270 ± 10 (100) | 260 ± 30 (100) | 170 ± 10 (100) |
Methimazole | <410 (<14) | <30 (<15) | <30 (<19) | 30 ± 10 (11) | <30 (<12) | <30 (<18) |
Heat | 1640 ± 90 (57) | 30 ± 10 (15) | 40 ± 0 (25) | 40 ± 10 (15) | 40 ± 0 (15) | 30 ± 0 (18) |
NBI, 1 mM | 2470 ± 160 (86) | 190 ± 10 (95) | 130 ± 0 (81) | 250 ± 20 (93) | N.D. | 150 ± 10 (88) |
NBI, 4 mM | 1810 ± 50 (63) | 140 ± 0 (70) | 100 ± 0 (63) | 180 ± 10 (67) | 170 ± 10 (65) | 100 ± 10 (59) |
No NADPH | <410 (<14) | <30 (<15) | <30 (<19) | 30 ± 10 (11) | <30 (<12) | <30 (<18) |
Control serum | 2850 ± 170 (100) | 200 ± 10 (100) | 150 ± 10 (100) | 270 ± 20 (100) | 220 ± 10 (100) | 150 ± 10 (100) |
Anti-reductase | 3050 ± 130 (107) | 210 ± 10 (105) | 130 ± 10 (87) | 250 ± 10 (93) | 220 ± 20 (100) | 150 ± 10 (100) |
MeDDC, 50 μM | ||||||
Control | 7320 ± 230 (100) | 530 ± 20 (100) | 390 ± 20 (100) | 770 ± 30 (100) | 660 ± 40 (100) | 480 ± 10 (100) |
Methimazole | 1340 ± 190 (18) | 120 ± 0 (23) | 100 ± 0 (26) | 190 ± 20 (25) | 140 ± 10 (21) | 140 ± 0 (29) |
Heat | 4270 ± 200 (58) | 160 ± 10 (30) | 140 ± 0 (36) | 210 ± 20 (27) | 170 ± 0 (26) | 150 ± 10 (31) |
NBI, 1 mM | 7210 ± 230 (99) | 510 ± 10 (96) | 380 ± 10 (97) | 730 ± 50 (95) | N.D. | 450 ± 20 (94) |
NBI, 4 mM | 6550 ± 340 (90) | 480 ± 10 (91) | 360 ± 20 (92) | 680 ± 10 (88) | 590 ± 20 (89) | 420 ± 10 (88) |
No NADPH | 1610 ± 150 (22) | 120 ± 10 (23) | 100 ± 0 (26) | 190 ± 10 (25) | 160 ± 20 (24) | 120 ± 10 (25) |
Control serum | 7750 ± 70 (100) | 530 ± 0 (100) | 380 ± 10 (100) | 770 ± 20 (100) | 600 ± 0 (100) | 440 ± 20 (100) |
Anti-reductase | 7950 ± 420 (103) | 520 ± 20 (98) | 370 ± 20 (97) | 710 ± 30 (92) | 610 ± 20 (102) | 460 ± 10 (105) |
Benzydamine N-oxide Formation | ||||||
Benzydamine, 0.5 mM | ||||||
Control | 15,600 ± 210 | 660 ± 10 | 460 ± 10 | 780 ± 10 | 870 ± 20 | 550 ± 0 |
No NADPH | <540 | <40 | <40 | <40 | <40 | <40 |
7-Hydroxycoumarin Formation | ||||||
7-Ethoxycoumarin, 1 mM | ||||||
Control | <4 | <4 | <4 | <4 | <4 | <4 |
MeDDC (5 or 50 μM) was incubated for 5 min, benzydamine (0.5 mM) for 10 min, or 7-ethoxycoumarin (1 mM) for 30 min, with 0.8 mg/ml human renal microsomes or 0.056 mg/ml FMO1 Supersomes. Values are the mean ± S.D. (percentage of control), n = 3.
N.D., not determined.