Table 2. Anti-inflammatory properties of compounds 5a–t.
Compound | R | IC50 nitrite reduction (μM) | IC50 ROS reduction (μM) |
---|---|---|---|
Sulforaphane | — | 1.4 ± 0.3 | 2.84 ± 0.55 |
5a | Ph | >60 | >60 |
5b | 2-OCH3Ph | 43.6 ± 6.45 | >60 |
5c | 3-OCH3Ph | 12.9 ± 0.86 | 18.1 ± 5.36 |
5d | 4-OCH3Ph | 35.4 ± 2.57 | 19.9 ± 4.89 |
5e | 2-CH3Ph | 34.3 ± 3.84 | 60.0 ± 0.29 |
5f | 3-CH3Ph | 13.4 ± 1.44 | 32.6 ± 6.79 |
5g | 4-CH3Ph | 22.3 ± 3.82 | 45.1 ± 5.33 |
5h | 4-FPh | 11.3 ± 1.15 | 37.0 ± 4.32 |
5i | 2-ClPh | >60 | >60 |
5j | 3-ClPh | 5.11 ± 0.65 | 24.0 ± 2.58 |
5k | 4-ClPh | 26.0 ± 2.74 | >60 |
5l | 2-BrPh | 26.7 ± 1.95 | 38.6 ± 7.16 |
5m | 4-BrPh | 11.4 ± 2.27 | 33.2 ± 7.36 |
5n | 2-NO2Ph | 15.8 ± 5.23 | 19.9 ± 4.89 |
5o | 3-NO2Ph | 40.8 ± 2.23 | 30.8 ± 4.99 |
5p | 4-NO2Ph | 26.7 ± 4.86 | >60 |
5q | 2-Furyl | 17.5 ± 2.45 | 22.5 ± 7.78 |
5r | 2-Thienyl | >60 | >60 |
5s | 3-Pyridyl | 7.23 ± 1.10 | 15.2 ± 3.73 |
5t | 4-Pyridyl | 28.8 ± 3.61 | 37.8 ± 1.17 |
IC50 values of nitrite production reduction and ROS production reduction elicited by compounds 5a–t in primary glial cultures treated with LPS (1 μg/mL) during 18 h (nitrite production) and 3 h (NOX activity derived ROS production). Primary glial cultures were treated with increasing concentrations of the corresponding compound for 24 h. Then, treatments were removed and glial cells were co-incubated with the corresponding compound at increasing concentrations and LPS (1 μg/mL) for 18 h. ROS production was measured after 24 h pre-incubation with increasing concentrations of the corresponding compound followed by 18 h of co-incubation with LPS and 3 h with the fluorescent dye. Data are expressed as the concentration required to inhibit 50% the liberation of nitrites induced by LPS (IC50). Data are means ± SEM of four different experiments in duplicate.