Table 1.
Antimicrobial and hemolytic activities of KR12 derived lipopeptides 1
| Peptide | Amino acid sequence |
Acyl chain |
MIC (μM) | HC50 (μM) |
CSI 2 | |||
|---|---|---|---|---|---|---|---|---|
| EC | KP | PA | SA | |||||
| LL-37 | See legend 3 | None | 3.1-6.2 | 6.2 | >50 | >50 | 170 | ND |
| KR12 | KRIWQRIKDFLR | None | >50 | >50 | 25 | >50 | >340 | ND |
| C14-KR10 | KRIWQRIKDF | C14 | 50 | 6.2 | 12.5 | 3.1 | <25 | <8 |
| C14-KR8 | KRIWQRIK | C14 | 12.5 | >50 | 6.2 | <1.5 | <25 | <16 |
| C14-KR6 | KRIWQR | C14 | 12.5 | >50 | 6.2 | 3.1 | <25 | <8 |
| C14-KR4 | KRIW | C14 | 12.5-50 | 12.5 | 6.2 | 3.1 | <25 | <8 |
| C12-KR12 | KRIWQRIKDFLR | C12 | >50 | 12.5 | >50 | 6.2 | <25 | <4 |
| C12-KR10 | KRIWQRIKDF | C12 | 6.2 | 3.1 | 3.1 | 1.5 | <25 | <16 |
| C12-KR8 | KRIWQRIK | C12 | 6.2 | >50 | 3.1 | 1.5 | 35 | 24 |
| C12-KR6 | KRIWQR | C12 | 12.5 | >50 | 6.2 | 3.1 | 75 | 24 |
| C12-KR4 | KRIW | C12 | 12.5 | >50 | 6.2 | 3.1 | 30 | 10 |
| C10-KR12 | KRIWQRIKDFLR | C10 | >50 | 6.2-12.5 | 25 | 3.1 | <25 | <8 |
| C10-KR10 | KRIWQRIKDF | C10 | 3.1 | 6.2 | 6.2 | 1.5 | 50 | 33 |
| C10-KR8 | KRIWQRIK | C10 | 12.5 | 50 | 6.2 | 1.5-3.1 | 300 | 200 |
| C10-KR8d | KRIWQRIK | C10 | 12.5 | 25 | 6.2 | 1.5-3.1 | 300 | 200 |
| C10-KR6 | KRIWQR | C10 | 50 | >50 | 25 | 12.5 | >340 | >27 |
| C10-KR4 | KRIW | C10 | 50 | >50 | 12.5 | 12.5 | 150 | 12 |
| C8-KR12 | KRIWQRIKDFLR | C8 | 6.2 | <6.2 | 6.2 | 3.1 | <25 | <8 |
| C8-KR10 | KRIWQRIKDF | C8 | 6.2 | 25 | 6.2 | 3.1-6.2 | 250 | 40-80 |
| C8-KR10d | KRIWQRIKDF | C8 | 6.2 | 12.5 | 12.5 | 3.1 | 150 | 48 |
| C8-KR8 | KRIWQRIK | C8 | 25 | >50 | 12.5 | 6.2 | >200 | 32 |
| C8-KR6 | KRIWQR | C8 | 50 | >50 | >50 | >50 | >200 | ND |
| C8-KR4 | KRIW | C8 | >50 | >50 | >50 | >50 | >200 | ND |
| C6-KR12 | KRIWQRIKDFLR | C6 | 3.1 | 6.2 | 12.5 | <1.5 | 25 | 16 |
| C6-KR10 | KRIWQRIKDF | C6 | 50 | >50 | 50 | 25 | >200 | >8 |
| C6-KR8 | KRIWQRIK | C6 | >50 | >50 | >50 | >50 | >200 | ND |
| C6-KR6 | KRIWQR | C6 | >50 | >50 | >50 | >50 | >200 | ND |
| C6-KR4 | KRIW | C6 | >50 | >50 | >50 | >50 | >200 | ND |
1
All peptides are C-terminally amidated. MIC, the minimal inhibitory concentration; EC, E. coli ATCC25922; KP, Klebsiella pneumonia ATCC 13883; PA, P. aeruginosa PAO1; SA, S. aureus USA300 LAC. ND = not determined.
2
CSI = HC50/MICSA where HC50 is the peptide concentration that causes 50% hemolysis and MICSA is MIC against S. aureus.
3
The amino acid sequence of LL-37 is LLGDFFRKSKEKIGKEFKRIVQRIKDFLRNLVPRTES, where KR12 is underlined. MIC and HC50 of LL-37 were taken from ref. [36].