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. 2011 Nov 15;125(2):345–358. doi: 10.1093/toxsci/kfr306

TABLE 1.

CYP-Mediated Formation of AAIa Form AAI in Human Hepatic Microsomes

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)
a

CYP activities in picomoles per minute per milligram protein. CYP1A2, CYP2A6, CYP2B6, CYP2C8, CYP2C9, CYP2C19, CYP2D6, CYP2E1, CYP3A4, and CYP4A determined by Gentest.

b

Picomole total C-hydroxylated metabolites per minute per milligram protein.

c

Arithmetic means for hepatic microsomal samples of 14 human donors and (SD), representing interindividual variability.