Table 1. Comparison of the inhibitory effects of meleagrin (1) and its derivatives against Staphylococcus aureus and E. coli FabI, bacterial growth, and [14C] acetate and [14C] leucine incorporation into membrane fatty acids.
Compounds | IC50 (μM) | MIC (μg/mL) | IC50 (μM) | |||||
saFabI | ecFabI | spFabK | S. aureus a | E. coli b | S. pneumoniae c | [14C] acetate incorporation | [14C] leucine incorporation | |
1 | 40.1 | 33.2 | >200 | 64 | 32 | 64 | 40.3 | >200 |
2 | 54.6 | 49.7 | >200 | 64 | 64 | 64 | - | - |
3 | 38.7 | 38.8 | >200 | 64 | 32 | 64 | 33.5 | >200 |
4 | 48.0 | 33.1 | >200 | 64 | 32 | 64 | 35.7 | >200 |
5 | 13.5 | 15.6 | >200 | 16 | 8 | 16 | 16.3 | >200 |
6 | 13.1 | 15.4 | >200 | 16 | 8 | 16 | 19.8 | >200 |
7 | >200 | >200 | >200 | >128 | >128 | >128 | >200 | >200 |
Triclosan | 0.66 | 0.98 | >200 | 0.01 | 0.01 | 64 | 0.04 | >10 |
S. aureus RN4220; b E. coli KCTC 1924; c S. pneumoniae KCTC 3932.