Table 1. Comparative Antibacterial Activity and Inhibition of Translation in Eukaryotic and Prokaryotic Systemsa.
translation inhibitionb |
antibacterial activity MIC (μM)c |
|||
---|---|---|---|---|
compd | IC50Euk (μM) | IC50Pro (μM) | E. coli R477/100 | B. subtilis ATCC6633 |
Genta. | 62 ± 9 | 0.03 ± 0.00 | 6 | <0.75 |
G418 | 2.0 ± 0.3 | 0.01 ± 0.00 | 9 | <1.25 |
1 | 347.1 ± 34.3 | 6.0 ± 1.0 | ||
(R)-4 | 120.5 ± 14.5 | 11.0 ± 1.2 | >311 | 311 |
(S)-5 | 515.8 ± 15 | 91.9 ± 8.4 | >375 | >375 |
2 | 13.9 ± 1.2 | 1.0 ± 0.1 | 680 | 42 |
6 | 7.5 ± 0.5 | 0.7 ± 0.1 | >273 | 34 |
3 | 1.5 ± 0.1 | 1.1 ± 0.2 | 1267 | 156 |
7 | 1.2 ± 0.1 | 1.2 ± 0.1 | >257 | 64 |
In all biological tests, all AGs were in their sulfate salt forms, and the concentrations refer to the free amine form of each AG.
The eukaryotic and prokaryotic half-maximal-inhibition values (IC50Euk and IC50) were quantified in coupled transcription/translation assays by using active luciferase detection as previously described by us.5
Minimal inhibitory concentration (MIC) values were determined by using the double-microdilution method.