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. 2018 Apr 19;12:887–899. doi: 10.2147/DDDT.S160314

Table 1.

2-benzylidene-1-indanone derivatives 4a-t inhibited LPS-induced IL-6 and TNF-α secretion in MPM 5′

graphic file with name dddt-12-887Fig10.jpg
Compound R1 (%) Inhibition (10 µM)*
Compound R1 (%) Inhibition (10 µM)*
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.