Table 1.
Antibacterial activity and cytotoxicity of AMPD sr-X22, sr-X18, and analogs
| E. coli W3110 | MIC at pH 5.0/7.4/8.0a |
MHCb | IC50 HEK293c | ||||
|---|---|---|---|---|---|---|---|
| A. baumannii ATCC 19606 | P. aeruginosa PAO1 | K. pneumoniae NCTC 418 | S aureus COL | ||||
| sr-T25 | 8/4/2 | 8/8/2 | 8/8/2 | >64/64/8 | >64/>64/4 | 1,000 | 197 ± 27 |
| L-T25 | 32/8/8 | 16/4/4 | 32/8/8 | >64/32/16 | >64/>64/32 | 62.5 | 92 ± 3 |
| D-T25 | 32/8/4 | 32/8/4 | 32/8/8 | >64/16/16 | >64/>64/32 | 125 | 33 ± 3 |
| sr-aT25 | 2/2–4/2 | 2/2/2 | 8/8/2 | >64/32/4 | >64/>64/2 | 1,000 | 5.8 ± 0.3 |
| sr-X18 | 32/4/2 | 2/2/2 | 16/4/2 | >64/32/8 | >64/>64/2 | >2,000 | 117 ± 12 |
| L-X18 | 16/16/16 | 16/32/16 | 16/32/16 | >64/>64/32 | >64/>64/16 | 7.8 | 52 ± 4 |
| D-X18 | 32/64/32 | 32/64/32 | 32/64/32 | >64/>64/>64 | >64/>64/32 | 7.8 | 47 ± 12 |
| sr-aX18 | 4/4/2 | 2/2/2 | 16/8/4 | >64/16/8 | >64/16/2 | >2,000 | 18 ± 1 |
| L- aX18 | 32/>64/32 | 32/64/32 | 64/>64/64 | >64/>64/>64 | >64/>64/32 | <3.9 | 14 ± 0.6 |
| D- aX18 | 32/>64/32 | 32/>64/16 | 64/>64/64 | >64/>64/>64 | >64/>64/16 | <3.9 | 21 ± 2 |
| sr-X22 | 32/4/2 | 32/4/2 | 16/2/2 | >64/64/8 | >64/>64/16 | >2,000 | 575 ± 30 |
| L-X22 | 8/4/2 | 8/4/2 | 8/4/4 | >64/>64/8 | >64/>64/8 | >2,000 | 575 ± 23 |
| D-X22 | 8/4/4 | 16/8/4 | 16/4/4 | >64/>64/16 | >64/>64/4 | 2,000 | 514 ± 21 |
| sr-aX22 | 2/2/2 | 2/2/2 | 64/8/4 | >64/64/8 | 64/16/2 | >2,000 | 21 ± 3 |
| L- aX22 | 2/4/4 | 2/4/4 | 16/8/16 | 64/8/8 | 64/16/4 | >2,000 | 24 ± 3 |
| D- aX22 | 4/8/4 | 4/4/4 | 32/8/16 | 64/16/16 | >64/16/4 | >2,000 | 17 ± 2 |
| L-G3KL | 32/8/1–2 | 8/8/1 | 16/4/1 | >64/>64/4 | >64/>64/2 | >2,000 | 460 ± 17 |
| L-T7 | 16/4/2 | 16/8/2–4 | 16/8/2–4 | >64/32/8 | >64/>64/4 | >2,000 | 70 ± 6 |
| PMB | 0.02/0.25/0.13 | 1/0.25/0.25 | 0.03/0.5/0.5 | 8/0.25/0.25 | >64/>64/4 | >2,000 | 346 ± 20 |
a
MIC in μg/mL was measured in Müller-Hinton (MH) medium after incubation for 16–20 h at 37°C. Each result represents two independent experiments performed in duplicate.
b
MHC (minimum hemolytic concentration) in μg/mL was measured on human red blood cells in PBS (pH 7.4) at room temperature after incubation for 4 h at 37°C. Each result represents two independent experiments performed in duplicate.
c
IC50 (mean ± SD, μg/mL) was measured on HEK293 cell line after incubation for 48 h at 37°C. Data present results from three independent experiments in triplicates.