Celecoxib is a highly selective cyclooxygenase-2 (COX-2) inhibitor with an IC50 value of 40nM[1]. Celecoxib is a selective nonsteroidal anti-inflammatory drug (NSAID) commonly used to treat acute pain, osteoarthritis (OA), rheumatoid arthritis (RA), juvenile rheumatoid arthritis and ankylosing spondylitis (AS)[2]. Celecoxib has strong anti-tumor activity and can prevent and treat a variety of cancers such as pancreatic cancer, breast cancer, ovarian cancer, and non-small cell lung cancer[3]. Celecoxib can prevent the occurrence of colorectal adenomatous polyps[4].
In vitro, Celecoxib (0.8, 2.0, 4.0, 8.0µg/mL) treated tenocytes for 24h dose-dependently inhibited cell viability and migration, but did not change cell morphology or cause cell necrosis[5]. Celecoxib (1-100μM) treated human osteoblasts for 24h, inhibited cell proliferation in a dose-dependent manner and caused an increase in intracellular Ca2+ concentration[6].
In vivo, Celecoxib (100mg/kg) was orally administered to mice with lung cancer model and unilateral lung resection, inhibiting lung cancer metastasis and the increase in plasma PGE2 levels[7]. Celecoxib (10, 20mg/kg) was orally administered to rats with gastric cancer model, significantly reducing the incidence and growth of gastric cancer in rats[8].
References:
[1] Cao H, Yu R, Choi Y, et al. Discovery of cyclooxygenase inhibitors from medicinal plants used to treat inflammation[J]. Pharmacological research, 2010, 61(6): 519-524.
[2] Frampton J E, Keating G M. Celecoxib: a review of its use in the management of arthritis and acute pain[J]. Drugs, 2007, 67: 2433-2474.
[3] Jendrossek V. Targeting apoptosis pathways by Celecoxib in cancer[J]. Cancer letters, 2013, 332(2): 313-324.
[4] Arber N, Eagle C J, Spicak J, et al. Celecoxib for the prevention of colorectal adenomatous polyps[J]. New England Journal of Medicine, 2006, 355(9): 885-895.
[5] Tsai W C, Hsu C C, Chou S W, et al. Effects of celecoxib on migration, proliferation and collagen expression of tendon cells[J]. Connective tissue research, 2007, 48(1): 46-51.
[6] Wang J L, Lin K L, Chen J S, et al. Effect of celecoxib on Ca2+ movement and cell proliferation in human osteoblasts[J]. Biochemical pharmacology, 2004, 67(6): 1123-1130.
[7] Zhang S, Da L, Yang X, et al. Celecoxib potentially inhibits metastasis of lung cancer promoted by surgery in mice, via suppression of the PGE2-modulated β-catenin pathway[J]. Toxicology letters, 2014, 225(2): 201-207.
[8] Hu P J, Yu J, Zeng Z R, et al. Chemoprevention of gastric cancer by celecoxib in rats[J]. Gut, 2004, 53(2): 195-200.
Celecoxib是一种高度选择性的环氧合酶-2（COX-2）抑制剂，IC50值为40nM[1]。Celecoxib是一种选择性非甾体抗炎药（NSAID），常用于治疗急性疼痛、骨关节炎（OA）、类风湿性关节炎（RA）、幼年类风湿性关节炎和强直性脊柱炎（AS）等[2]。Celecoxib 具有强大的抗肿瘤活性，能够预防和治疗胰腺癌、乳腺癌、卵巢癌、非小细胞肺癌等多种癌症[3]。Celecoxib能够预防结直肠腺瘤性息肉的发生[4]。
在体外，Celecoxib（0.8, 2.0, 4.0, 8.0µg/mL）处理肌腱细胞24h，剂量依赖性地抑制了细胞活力和迁移，但不改变细胞形态或造成细胞坏死[5]。Celecoxib（1-100μM）处理人成骨细胞24h，剂量依赖性地抑制了细胞增殖，引起了细胞内Ca2+浓度的增加[6]。
在体内，Celecoxib（100mg/kg）通过口服治疗肺癌模型并做了单侧肺切除手术的小鼠，抑制了肺癌转移，抑制了血浆PGE2水平的升高[7]。Celecoxib（10、20mg/kg）通过口服治疗胃癌模型大鼠，显著降低了大鼠胃癌的发病率和生长[8]。