Fig. 3: TLR4 agonist and antagonist activity of the compounds.
From: Adjuvant activity of a small molecule TLR4 agonist discovered via structure-based virtual screening
A TLR4 agonist activity of compounds. WT and TLR4−/− mouse macrophage cell lines were stimulated with 2 µg/mL MPLA (1.13 µM), or 2 µM of NSF-418 (0.679 µg/mL) or NSF-501(0.649 µg/mL) or NSF-951 (0.873 µg/mL) for 24hrs at 37 °C/5%CO2 and production of proinflammatory cytokines (IL-6 and TNF-α) was analysed in the culture supernatant by sandwich ELISA as described in methodology. B TLR4 antagonist activity of compounds. RAW 264.7 cells were treated with the compounds as described above, followed by treatment with MPLA (2 µg/mL) for 24 hrs at 37 °C/ 5%CO2 and production of proinflammatory cytokines (IL-6 and TNF-α) was analysed in the culture supernatant by sandwich ELISA as described in methodology. All data represent the mean ± SD of triplicates (n = 3) and are representative of three independent biological experiments. Significant differences were analysed using one-way analysis of variance (ANOVA), followed by the Dunnett post hoc test. The value of p < 0.05 was considered statistically significant and noted as ****p < 0.0001 and “ns” as not significant.
