TABLE 1

Sulfating activities toward various amine drugs of human recombinant SULTs

Sulfating activities were determined using [35S]PAPS as a sulfate donor. Reactions were performed at pH 7.4 (for ciprofloxacin, moxifloxacin, and garenoxacin) or pH 10.0 (for desipramine and metoclopramide) in the presence of 100 μM concentrations of substrates and 50 ng of recombinant enzymes (His6-SULT). After a 20-min incubation, reaction mixtures were separated on thin-layer plates. The radioactive spots were quantified with an FLA-3000 image analyzer. The data are expressed as the mean ± S.D. of three determinations from one experiment.


SULT

Sulfating Activity
Ciprofloxacin
Moxifloxacin
Garenoxacin
Desipramine
Metoclopramide
nmol/min/mg protein
hSULT1A1 N.D. N.D. 1.9 ± 0.03 N.D. N.D.
hSULT1A3 N.D. N.D. N.D. N.D. N.D.
hSULT1B1 N.D. N.D. N.D. N.D. N.D.
hSULT1C2 N.D. N.D. N.D. N.D. N.D.
hSULT1E1 N.D. N.D. N.D. N.D. N.D.
hSULT2A1
3.8 ± 0.3
6.3 ± 0.1
4.3 ± 0.2
3.4 ± 0.2
0.29 ± 0.04
  • N.D., not detected (activity below the detection limit: 0.1 nmol/min/mg protein).