TABLE 1.
CYP-dependent catalytic activitiesa | |||||||||||||
No. | pmol CYP per mg protein |
Sudan I oxidation in presence of ketoconazole (CYP1A1)b |
Phenacetin O-deethy-lation (CYP1A2) |
Coumarin 7-hydroxylation (CYP2A6) |
(S)-Mephenytoin N-demthy-lation (CYP2B6) |
Paclitaxel 6α-hydroxy-lation (CYP2C8) |
Diclofenac 4′-hydroxy-lation (CYP2C9) |
(S)-Mephenytoin 4′-hydroxy-lation (CYP2C19) |
Burfuralol 1′-hydroxy-lation (CYP2D6) |
Chloroxazone 6-hydroxy-lation (CYP2E1) |
Testosterone 6β-hydroxy-lation (CYP3A4) |
Lauric acid 12-hydroxy-lation (CYP4A) |
AAIs Peak area |
HG93 | 290 | 1.1 | 750 | 340 | 25 | 180 | 2100 | 41 | 56 | 1800 | 2400 | 1600 | 6.0 |
HG03 | 290 | 0.9 | 170 | 2000 | 51 | 200 | 1700 | 44 | 110 | 1800 | 6100 | 1600 | 2.0 |
HG74 | 220 | 1.2 | 520 | 360 | 13 | 130 | 2100 | 55 | 120 | 1400 | 2700 | 1300 | 7.8 |
HG06 | 300 | 0.9 | 770 | 580 | 3.0 | 130 | 2650 | 36 | ND | 1200 | 2990 | 740 | 5.8 |
HK27 | 300 | 1.6 | 1320 | 1320 | 31 | 180 | 480 | 460 | 130 | 3000 | 4910 | 1110 | 10 |
HG42 | 670 | 0.9 | 700 | 2200 | 150 | 480 | 1600 | 7.0 | 95 | 1600 | 15,000 | 1400 | 4.0 |
HG112 | 560 | 0.5 | 320 | 490 | 150 | 180 | 4000 | 380 | 32 | 2400 | 25,000 | 1800 | 2.7 |
HG56 | 550 | 3.0 | 2400 | 1500 | 48 | 180 | 3100 | 480 | 120 | 1900 | 5300 | 3000 | 18 |
HG43 | 270 | 1.2 | 630 | 850 | 34 | 60 | 1400 | 700 | 20 | 1100 | 5600 | 2100 | 3.8 |
HG89 | 400 | 1.6 | 1500 | 650 | 60 | 160 | 2100 | 190 | 13 | 1700 | 12,000 | 2200 | 16 |
HG32 | 170 | 1.3 | 730 | 520 | 1.0 | 20 | 450 | 5.0 | 46 | 1200 | 2000 | 680 | 4.8 |
HK31 | 580 | 2.5 | 1220 | 2160 | 8.0 | 130 | 1690 | 170 | 3.0 | 1660 | 8210 | 2010 | 17.5 |
HK23 | 380 | 1.6 | 960 | 1100 | 24 | 160 | 2100 | 110 | 140 | 2100 | 6800 | 780 | 7.2 |
HK34 | 500 | 1.6 | 1000 | 1500 | 39 | 220 | 1900 | 45 | 100 | 6000 | 5200 | 1100 | 6.15 |
Meansc | 390 (150) | 1.4 (0.6) | 930 (540) | 1110 (650) | 46 (46) | 170 (100) | 1960 (890) | 200 (210) | 76 (47) | 2060 (1200) | 7440 (6010) | 1530 (630) | 8.0 (5.2) |
CYP activities in picomoles per minute per milligram protein. CYP1A2, CYP2A6, CYP2B6, CYP2C8, CYP2C9, CYP2C19, CYP2D6, CYP2E1, CYP3A4, and CYP4A determined by Gentest.
Picomole total C-hydroxylated metabolites per minute per milligram protein.
Arithmetic means for hepatic microsomal samples of 14 human donors and (SD), representing interindividual variability.