Table 2. Effects of esculentin-2CHa and its analogues on insulin- and LDH-release, membrane potential and intracellular calcium concentration in BRIN-BD11 cells.
| Peptide | BRIN-BD11 cells (Threshold concentration) | Mouse islets (Threshold concentration) | LDH release (% of control) | Membrane potential (AUC, x 103 RFU) | Intracellular Ca2+ (AUC, x 102 RFU) |
|---|---|---|---|---|---|
| Control (Glucose 5.6mM) | - | - | 100.0±2.9 | 3.71±1.05 | 4.30±0.40 |
| Esculentin-2CHa | 0.3nM | 10nM | 102.7±1.1 | 8.01±0.28** | 6.44±0.47* |
| [L21K]Esculentin-2CHa | 0.01nM | 10nM | 100.6±2.0 | 7.78±0.31** | 6.14±0.41* |
| [L24K]Esculentin-2CHa | 0.01nM | 10nM | 101.3±3.1 | 7.87±0.19** | 6.28±0.62* |
| [L28K]Esculentin-2CHa | 0.01nM | 1nM | 101.8±1.5 | 7.78±0.22** | 7.28±0.94* |
| [C31K]Esculentin-2CHa | 0.01nM | 0.1nM | 100.2±2.8 | 7.92±0.14** | 6.32±0.72* |
| [C31S, C37S]Esculentin-2CHa | 0.01nM | 1nM | 104.3±3.1 | 7.96±0.24** | 6.55±0.36* |
| [D20K, D27K]Esculentin-2CHa | 0.1nM | 10nM | 102.5±2.6 | 7.85±0.32** | 6.10±0.46* |
LDH release data were obtained at the highest peptide concentration (3 μM). Membrane potential and intracellular Ca2+ experiments were carried out at 1μM concentration. Values are mean ± SEM with n = 8.
*P < 0.05
**P < 0.01 compared with 5.6mM glucose.