Table 4.
Effect of the compounds on LPS-induced NF-κB/AP-1 transcriptional activity in THP1-Blue cells, LPS-induced production of IL-6 in MonoMac-6 cells, and cytotoxicity.
| Compound | THP-1Blue Cell Cytotoxicity | MonoMac-6 Cell Cytotoxicity | THP-1Blue Cell NF-κB/AP-1 | MonoMac-6 Cell IL-6 |
|---|---|---|---|---|
| IC50 (μM) | ||||
| IQ-1 | N.T | N.T | 2.3 ± 0.8 | 3.4 ± 0.8 |
| 4a | N.T. | N.T. | 0.3 ± 0.1 | 3.0 ± 0.6 |
| 4b | N.T. | N.T. | 0.9 ± 0.3 | 1.2 ± 0.4 |
| 4c | 37.5 ± 1.7 | 14.6 ± 1.2 | n.d. | n.d. |
| 4d | N.T. | N.T. | 0.4 ± 0.1 | 1.0 ± 0.2 |
| 4e | N.T. | N.T. | 0.4 ± 0.1 | 2.2 ± 0.2 |
| 4f | N.T. | N.T. | 1.1 ± 0.4 | 14.0 ± 2.8 |
| 4g | N.T. | 32.0 ± 2.2 | 2.1 ± 0.4 | n.d. |
| 4h | N.T. | 29.0 ± 2.5 | 2.5 ± 0.6 | n.d. |
| 4i | N.T. | N.T. | 2.9 ± 0.9 | 6.2 ± 0.2 |
| 4j | 36.5 ± 1.9 | N.T. | n.d. | 4.8 ± 0.5 |
| 4k | N.T. | N.T. | 0.6 ± 0.2 | 2.3 ± 0.4 |
| 4l | 26.1 ± 5.3 | N.T. | n.d. | N.A. |
| 4m | N.T. | N.T. | 0.1 ± 0.05 | 0.8 ± 0.1 |
N.A., no inhibition at concentrations < 50 μM; N.T., non-cytotoxic at concentrations < 50 μM; n.d., no data (activity was not evaluated because of compound cytotoxicity). Data for IQ-1 are from [35].