Aspirin (Acetylsalicylic Acid) is a COX inhibitor that inhibits COX1 and COX2 (IC50=5/210 μg/mL) with selective, irreversible, and oral activity. Aspirin is also a histone deacetylase inhibitor that up-regulates the cell cycle blocking protein, p21. Aspirin has a variety of activities. Aspirin has anti-inflammatory, antipyretic and analgesic, and antiplatelet aggregation activities.

COX-1:5μg/mL, COX-2:210 μg/mL

方法: 结直肠癌细胞 SW620、LoVo、RKO 和 DLD-1 用 Aspirin (2 mM) 和 Cisplatin (5-80 µM) 处理 48 h，使用 MTT assay 检测细胞活力。
结果: 联合用药更有效地降低了结肠癌细胞的生存能力。联合治疗导致 Cisplatin 的 IC50 值显著降低。[1]
方法: 成骨细胞 MG-63 用 Aspirin (1-1000 µM) 处理 24 h，使用 Flow cytometry 检测细胞周期。
结果: 1、10、20 µM 剂量的 Aspirin 治疗 24 h 后，对 MG-63 细胞周期无明显影响。然而，在 100 和 1000 µM 的剂量下，G0/G1 期的细胞百分比显著增加。[2]

方法: 为检测体内抗肿瘤活性，将 Aspirin (100 mg/kg，灌胃给药，每天一次) 和 Cisplatin (3 mg/kg，腹腔注射，每三天一次) 给药给携带 LoVo 异种移植物的裸鼠，持续 18 天。
结果: Aspirin 与 Cisplatin 协同抑制结肠癌裸鼠移植瘤生长，并且这些作用至少部分通过调节 PI3K-Akt、RAF-MEK-ERK 和 NF-κB/COX-2 信号通路发挥。[1]

Chondrocytes are isolated from articular cartilage of donors with no articular disease. Unstimulated and interleukin 1 (IL-1) stimulated chondrocytes are used as models to study the effects of drugs on COX-1 and COX-2. Cells are incubated with vehicle or drugs (Asprin); supernatants are removed and the level of prostaglandin E2 (PGE2) in each sample is determined by enzyme immunoassay. IC50s are calculated from the reduction in PGE2 content by different concentrations of the test substance by linear regression analysis[5].