Table I.
Half-maximal inhibitory concentration of N-arylacyl O-sulfonated aminoglycosides for inhibition of each NSP
| Compound | Human neutrophil elastasea, IC50 (μM) | Cathepsin Gb, IC50 (μM) | Proteinase 3a, IC50 (μM) |
|---|---|---|---|
| NeoCbz | 8.13 ± 3.49 | 0.42 ± 0.03 | >300 |
| NeoPhA | >300 | 1.29 ± 0.21 | 97.72 ± 22.75 |
| NeoBz | >300 | 1.55 ± 0.36 | >300 |
| KanCbz | 16.60 ± 7.55 | 3.72 ± 0.17 | 16.98 ± 5.18* |
| KanPhA | 229.09 ± 58.99 | 12.3 ± 1.42 | 165.96 ± 58.75 |
| KanBz | >300 | 26.92 ± 5.63 | >300 |
| AprCbz | 20.42 ± 11.45 | 2.14 ± 0.2 | 26.92 ± 18.52 |
| AprPhA | 263.03 ± 30.37 | 123.03 ± 11.35 | NI |
| AprBz | NI | 208.93 ± 24.68 | ND |
NI, no inhibition; ND, not determined.
IC50 values derived from nonlinear regression curve fitting to log(inhibitor) vs. normalized response. Data are shown as mean ± SE (n = 3 or *n = 2).
aSubstrates: N-methoxysuccinyl-Ala-Ala-Pro-Val-p-nitroanilide.
bN-succinyl-Ala-Ala-Pro-Phe-p-nitroanilide.