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. 2020 Feb 26;27(5):1208–1216. doi: 10.1016/j.sjbs.2020.02.010

Table 1.

Results of percentage of inhibition of COX-1, and COX-2, IC50, selectivity COX-1/CO-2; percentage of inhibition of IL-6 (pg/ml), and TNF-α of the synthesized spirooxindoles based on benzo[b]furan scaffold 5a-r.

# Compound COX-1% COX-2% COX-1
 COX-2
 Selectivityb
IC50 COX-1/IC50 COX-2		 IL-6 (pg/ml)% TNF-α
(pg/ml)%
IC50 (μM ± SD)a
1 graphic file with name fx1.gif 57.38 11.24 20.42 ± 0.55 88.09 ± 1.78 23% 57.38 51.24
2 graphic file with name fx2.gif 27.36 9.81 NDc ND ND 27.36 9.81
3 graphic file with name fx3.gif 40.81 8.33 37 ± 1.54 76.17 ± 1.46 49% 59.81 48.33
4 graphic file with name fx4.gif 19.81 7.77 ND ND ND 76.81 67.77
5 graphic file with name fx5.gif 9.43 1.8 ND ND ND 82.43 71.8
6 graphic file with name fx6.gif 32.08 5.92 ND ND ND 63.08 55.92
7 graphic file with name fx7.gif 19.81 2.76 ND ND ND 81.81 78.76
8 graphic file with name fx8.gif 41.70 9.8 35.70 ± 0.51 84.66 ± 1.16 42% 38.70 49.8
9 graphic file with name fx9.gif 44.53 17.85 29.55 ± 0.19 71.25 ± 1.29 41% 62.53 57.85
10 graphic file with name fx10.gif 21.70 7.89 ND ND ND 77.70 67.89
11 graphic file with name fx11.gif 12.26 4.45 ND ND ND 87.26 74.45
12 graphic file with name fx12.gif 47.74 19.78 31.25 ± 0.24 58.75 ± 1.58 36% 42.74 39.78
13 graphic file with name fx13.gif 20.75 5.78 ND ND ND 79.54 75.78
14 graphic file with name fx14.gif 9.43 1.11 ND ND ND 82.12 77.11
15 graphic file with name fx15.gif 29.25 6.11 ND ND ND 76.81 66.11
16 graphic file with name fx16.gif 52.75 9.98 38.24 ± 0.96 85.70 ± 1.51 45% 47.18 39.98
17 graphic file with name fx17.gif 32.08 10.1 ND ND ND 67.43 60.1
18 graphic file with name fx18.gif 32.08 6.91 ND ND ND 64.81 62.91
STD Indomethacin 87.31 18.76 0.24 ± 0.05 3.28 ± 0.09 7% 7.7 8.1
Acetyl-keto boswellic acid 71.42 19.87 7.84 ± 0.13 82.52 ± 0.62 10% 7.31 18.76
Acetyl-β-boswellic acid 75.73 14.87 8.16 ± 0.10 72.52 ± 0.51 11% 11.42 19.87
Acetyl-α-boswellic acid 69.81 7.98 10.13 ± 0.17 >100 10% 15.73 14.87
β-Boswellic acid 64.77 7.66 18.14 ± 0.42 >100 18% 19.81 27.98
Celecoxib 8.7 92 29.19 ± 0.33 0.08 ± 0.44 365% 24.77 25.16
Lipopolysaccharide (LPS) – – – – – 100 100
a

COX-1, and COX-2 inhibitory activity is expressed as the mean ± SD of triplicate experiments. bSelectivity is defined as IC50 COX-1/IC50 COX-2. cND: not determined.