Table 1.
Activities of 10-substituted 1,8-diazaphenothiazines in selected immunological assays
| No. | Cytotoxicity against PBMC | Inhibition of PHA-induced PBMC proliferation | TNF-α inhibition | |||
|---|---|---|---|---|---|---|
| 10 µg/ml | 50 µg/ml | 1 µg/ml | 10 µg/ml | 50 µg/ml | 5 µg/ml | |
| 4 | 6.7 | 21.4 | 5.0 | 74.4 | 78.6 | 50.4 |
| 7 | 0.8 | 1.7 | 9.6 | 22.9 | 45.6 | 76.4 |
| 8 | −0.3 | −6.0 | 19.0 | 26.0 | 55.6 | 89.3 |
| 9 | −1.1 | 8.8 | 9.3 | 24.4 | 41.2 | 87.4 |
| 10 | 2.0 | 2.6 | 13.6 | 26.8 | 45.5 | 85.9 |
| 12 | 6.6 | 8.1 | 4.1 | 5.2 | 26.2 | 54.8 |
| 13 | −3.6 | 15.0 | 5.7 | 20.9 | 81.1 | 86.7 |
| 14 | −0.7 | 11.9 | 1.4 | 19.2 | 59.4 | 89.1 |
| 15 | 1.3 | 12.1 | −6.8 | −5.4 | 59.6 | 75.0 |
| 16 | 0.9 | 10.0 | −0.9 | −2.9 | 47.0 | 85.6 |
| 17 | 1.5 | 7.3 | −0.9 | −0.5 | 18.0 | 47.6 |
| 18 | −1.4 | 18.7 | −3.4 | 5.1 | 67.4 | 73.1 |
| 19 | −4.5 | 4.8 | −0.9 | 7.0 | 18.2 | 46.1 |
| 20 | −2.0 | −0.1 | 3.6 | 12.5 | 42.2 | 76.0 |
| 22 | −5.0 | 6.7 | 8.9 | 16.2 | 62.5 | 5.8 |
| 23 | −0.9 | 12.5 | 9.4 | 19.3 | 50.2 | 48.6 |
| 24 | −1.6 | 4.5 | 8.4 | 12.4 | 46.8 | 7.3 |
The table shows the degree of cytotoxicity against PBMC, effects on PHA-induced proliferative response of human PBMC and LPS-induced TNF-α production by these cells. The results are given in percentage inhibition as compared with appropriate DMSO controls. Positive values denote inhibition, negative stimulation