TABLE 1

Enzyme activities of biological samples and effects of typical inhibitors

Each value represents the mean ± S.D. (n = 3).

Marker EnzymeEnzyme SourceProbe SubstrateInhibitorEnzyme Activity
CYP2A6 (pmol/min/pmol of P450)cDNA-expressedCoumarin7.1 ± 0.1
+TCP (10 μM)0.7 ± 0.2
CYP2A6 (pmol/min/mg)MicrosomesCoumarin424.0 ± 30.3
+TCP (10 μM)12.0 ± 1.6
CYP2A6 (pmol/min/mg)S9Coumarin262.7 ± 9.7
+TCP (10 μM)11.4 ± 0.3
TPase (nmol/min)Purified TPaseThymidine6.6 ± 0.3
+TPI (10 μM)N.D.
TPase (nmol/min/mg)CytosolThymidine9.0 ± 0.3
+TPI (10 μM)N.D.
TPase (nmol/min/mg)S9Thymidine5.5 ± 0.7
+TPI (10 μM)N.D.
ALDH (nmol/min/mg)CytosolAcetaldehyde5.8 ± 0.8
+Disulfiram (100 μM)0.4 ± 0.4
ALH (nmol/min/mg)CytosolEthanol18.0 ± 1.5
+4-Methylpyrazole (100 μM)3.1 ± 0.7
ALO (nmol/min/mg)CytosolPhenanthridine2.8 ± 0.2
+Menadione (100 μM)0.2 ± 0.1
  • ALDH, aldehyde dehydrogenase; ALH, alcohol dehydrogenase; ALO, aldehyde oxidase; cDNA-expressed, cDNA-expressed CYP2A6; microsomes, human liver microsomes; S9, human liver S9; cytosol, human liver cytosol; N.D., not detected.