Table 1.
In vitro and bacterial cell–based assays for β-glucuronidase activity and inhibitor efficacy. kcat, catalytic rate; Km, Michaelis constant; N/A, not applicable. N.E., not effective. Errors represent standard deviation, where N = 3.
E. coli β-glucuronidase in vitro
|
E. coli cell–based
|
|||
---|---|---|---|---|
IC50 (nM) | kcat/Km (s−1 μM−1) | Ki (nM) | EC50 (nM) | |
No inhibitor | N/A | 0.134 ± 0.0123 | N/A | N/A |
Glucaro-δ-lactam | 26400 ± 483 | N/A | 7750 ± 475 | N.E. |
Inhibitor 1 | 283 ± 26.1 | 0.0987 ± 0.00621 | 164 ± 13.0 | 17.7 ± 7.42 |
Inhibitor 2 | 369 ± 2.51 | 0.119 ± 0.00473 | 208 ± 25.4 | 28.3 ± 2.11 |
Inhibitor 3 | 586 ± 31.1 | 0.136 ± 0.00633 | 684 ± 81.6 | 233.2 ± 2.99 |
Inhibitor 4 | 1060 ± 3.54 | 0.122 ± 0.0205 | 1380 ± 166 | 1322.8 ± 1.15 |