Celecoxib (SC 58635) is a non-steroidal anti-inflammatory agent, a COX-2 inhibitor (IC50=40 nM), with selectivity. Celecoxib has anti-inflammatory and analgesic activity and can be used for the treatment of osteoarthritis, rheumatoid arthritis, and acute pain.

COX-2:40 nM

方法：鼻咽癌 (NPC) 细胞系 HNE1 和 CNE1-LMP1 用 Celecoxib (5-75 µM) 处理 48 h，使用 MTT assay 检测细胞活力。
结果：Celecoxib 的抑制作用以剂量依赖的方式发生。Celecoxib 在 HNE1 和 CNE1-LMP1 中的平均 IC50 值分别为 32.86±1.13 µmol/L 和 61.31±4.30 µmol/L。[1]
方法：人正常肝细胞 L02 用 PA (200 µM) 和 Celecoxib (5-40 µM) 处理 24 h，使用 Western Blot 检测靶点蛋白表达水平。
结果：PA 诱导 COX-2 上调，LC3 II/I 和 p62 的蛋白质表达增加。PA和 Celecoxib 联用，COX-2 和 p62 的蛋白水平显著降低，LC3 II/I 增加。[2]

方法：为测试是否能降低放射性肺炎的死亡率，将 Celecoxib (25  mg/kg in 0.5% methyl cellulose and 0.025% Tween 20 in sterile water) 灌胃给药给局部胸部照射 (LTI) 的 C3Hf/KamLaw 小鼠。从 LTI 当天或 40 或 80 天后开始给药，每天两次，持续四十天。
结果：Celecoxib 相对于 LTI 的时间决定了疗效。只有当 Celecoxib 在 LTI 后 80 天开始使用时，死亡时间才能显著缩短，这与肺炎的表达时间相对应。对于这些小鼠，死亡率的降低被量化为治疗组与未治疗组的死亡率的风险比为 0.36。[3]

COX enzyme assay in vitro: Expression of COX protein in insect cells is determined by assessing PG-synthetic capability in homogenates from cells incubated for 3 days with COX-1 or COX-2 baculovirus. Cells expressing COX-1 or COX-2 are homogenized and incubated with arachidonic acid (10 μM). COX activity is determined by monitoring PG production. No COX activity is detected in mock-infected Sf9 cells. Celecoxib are preincubated with crude 1% CHAPS homogenates (2-10 μg of protein) for 10 minutes before addition of arachidonic acid. PGE2 formed is detected by ELISA after 10 minute incubation.

The antiproliferative effect of Celecoxib on NPC cells is assessed using an MTT assay. Cells are seeded into 96-well plates and allowed to attach for 24 hours. The cells are then treated with increasing concentrations of Celecoxib (0 to 75 μM) dissolved in DMSO (final concentration ≤0.1%) and incubated for up to 48 hours. After the incubation, 20 μL of MTT dye (5 mg/mL) are added to each well and cells are incubated at 37 °C for 4 hours. After removing the supernatants, the crystals are dissolved in DMSO and the absorbance is measured at 490 nm. The half-maximal inhibitory concentration (IC50) values and the 95% confidence intervals are calculated using probit regression using SPSS 15.0 software. The experiment is performed in triplicate and repeated at least three times.(Only for Reference)