Table 1.
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Compound | R1 | (%) Inhibition (10 µM)*
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Compound | R1 | (%) Inhibition (10 µM)*
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IL-6 | TNF-α | IL-6 | TNF-α | ||||
4a | 4′-OMe | 61.61±6.21 | 48.26±1.14 | 4l | 2′-Cl | 45.77±1.79 | 26.36±4.99 |
4b | 4′-OEt | 35.54±1.21 | 14.42±6.14 | 4m | 2′-Br | 63.04±2.13 | NA |
4c | 3′,4′-OH | 70.32±3.27 | 45.59±3.59 | 4n | 3′-Br | 47.37±6.65 | 17.87±1.89 |
4d | 3′-OMe, 4′-OH | 69.28±1.58 | 83.73±4.05 | 4o | 4′-Br | 53.71±3.29 | 29.40±0.61 |
4e | 2′,3′-OMe | 41.35±1.70 | 34.13±3.19 | 4p | 4′-F | 59.99±1.32 | 41.99±1.44 |
4f | 2′,4′-OMe | 52.29±2.09 | 44.52±3.61 | 4q | 4′-CF3 | 52.24±5.33 | 36.07±2.03 |
4g | 3′,4′,5′-OMe | 55.69±1.63 | 67.94±1.21 | 4r | 3′,4′-F | 17.39±1.51 | 18.93±1.19 |
4h | 2′,3′,4′-OMe | 55.33±9.97 | 67.92±3.85 | 4s | 3′,4′-Cl | 54.08±1.13 | 33.89±5.37 |
4i | 2′,4′,6′-OMe | 54.21±1.02 | 44.16±3.58 | 4t | 3′-NO2, 4′-Cl | 47.37±3.16 | 36.51±2.91 |
4j | 2′,4′,5′-OMe | 54.78±2.28 | 28.40±1.82 | XAN | 62.45±1.83 | 53.27±1.65 | |
4k | 2′-F | 41.28±1.98 | 15.68±3.64 |
Notes: Macrophages were plated at a density of 5.0×105/plate at 37°C and 5% CO2 overnight. Cells were pretreated with vehicle and compounds (10 µM) for 30 min, and subsequently treated with LPS (0.5 µg/mL) for 24 h. The culture media were collected and the inflammatory cytokines, TNF-α and IL-6, in media were detected by ELISA and normalized by total protein concentration.
Values are the mean of at least n=3 independent experiments±SEM.
Abbreviations: IL-6, interleukin-6; LPS, lipopolysaccharide; TNF-α, tumor necrosis factor-α; MPM, murine primary macrophage; ELISA, enzyme-linked immunosorbent assay; NA, no activity; XAN, xanthohumol; SEM, standard error of the mean.