Anti-inflammatory agent 33

Anti-inflammatory agent 33 is a potent p38α inhibitor. Anti-inflammatory agent 33 inhibits NO production. Anti-inflammatory agent 33 inhibits LPS-induced iNOS, COX-2, p-p38α, p-MK2 protein expression. Anti-inflammatory agent 33 shows anti-inflammatory activity[1].

Signaling Pathways >> MAPK/ERK Pathway >> p38 MAPK

Research Areas >> Inflammation/Immunology

Anti-inflammatory agent 33 (compound 8j) (10, 5, 2.5, 1.25, 0.675 μM; 1+24 h) 在 LPS 诱导的 RAW264.7 细胞中显着抑制 NO 的产生，抑制率为93.97%，IC50 值为 1.25 µM[1]。 Anti-inflammatory agent 33 (1.25, 2.5, 5, 10, 20 µM; 1+24 h) 抑制 TNF-α 和 IL-1β 的产生，IC50 值分别为 11.5, 8.48 μM[1]。 Anti-inflammatory agent 33 (1, 3, 5 µM; 1+24 h) 在 RAW264.7 细胞中呈剂量依赖性抑制 LPS 诱导的 iNOS、COX-2、p-p38α、p-MK2 蛋白的表达[1]。 Western Blot Analysis[1] Cell Line: RAW264.7 cells Concentration: 1, 3, 5 µM Incubation Time: 1+24 h Result: Inhibited the LPS-induced expression of pro-inflammatory mediators iNOS, COX-2, p-p38α; p-MK2 in the RAW264.7 cells.

Anti-inflammatory agent 33 (10, 30 mg/kg; once a day for 14 days) 在大鼠体内表现出剂量依赖性的抗炎活性[1]。 Animal Model: 160-180 g, female Sprague–Dawley rats (AIA model)[1] Dosage: 10, 30 mg/kg Administration: Once a day for 14 days Result: Significantly reduced the swelling of the feet of the rats in a dose-dependent manner.

[1]. Du J, et al. Novel tryptanthrin derivatives with benzenesulfonamide substituents: Design, synthesis, and anti-inflammatory evaluation. Eur J Med Chem. 2022 Nov 25;246:114956.