Table 2

Inhibition of SSAO activity by different compounds in control and TNF-α-exposed cells

InhibitorKi(nM)
ControlTNF-α
Semicarbazide5720  ± 3904510  ± 240
Aminoguanidine5200  ± 3404440  ± 490
Phenelzine0.6  ± 0.10.5  ± 0.2
Hydrazine2.4  ± 0.21.7  ± 0.3
Hydralazine58.3  ± 6.647.9  ± 8.2
Benserazide64.4  ± 5.249.1  ± 6.2

Cell extracts were prepared from mature 3T3-L1 adipocytes cultured in the absence or presence of 0.3 nM TNF-α for 48 h. 3T3-L1 cell homogenates were preincubated for 30 min at 37°C in the presence of various concentrations of each inhibitor. Pargyline at 1 mM was also added in the assay to inhibit monoamine oxidase activity. Benzylamine (30 μM) was then added as substrate for 1 h. IC50 values were obtained by computer analysis with the ENZFITTER program. ApparentKi values of SSAO towards the different SSAO inhibitors were then calculated by the equation of Cheng and Prusoff. Results represent the mean ± S.E. of four separate experiments.