Department of Medicine, Division of Rheumatology, New York University School of Medicine, 450 E 29th Street, New York, NY 10016, USA.
Inflammation. 2012 Oct;35(5):1706-14. doi: 10.1007/s10753-012-9488-8.
Celecoxib (Celebrex(®)), a non-steroidal anti-inflammatory drug and selective cyclooxygenase-2 inhibitor, is widely used to treat arthritis and other inflammatory disorders. Awareness of its anti-proliferative properties has prompted another indication for its use, in preventing colon polyps in high-risk populations. Farnesylthiosalicylic acid (FTS; Salirasib(®)), designed to inhibit oncogenic Ras and currently under evaluation in phase I/II and II clinical trials, was recently shown by our group to exert anti-inflammatory effects on both lymphocytes and mast cells. Here we examined whether celecoxib combined with FTS would enhance this anti-inflammatory activity. While each drug separately inhibited Ras activation in these cells, their combination yielded more marked inhibition as well as further inhibition of ERK phosphorylation, lymphocyte adhesion, and interleukin-2 secretion. The inhibitory effects, moreover, were independent of prostaglandin E(2) secretion. These data point to the promising potential of combined treatment with celecoxib and FTS for inflammatory disorders involving lymphocytes.
塞来昔布(西乐葆),一种非甾体类抗炎药和选择性环氧化酶-2 抑制剂,广泛用于治疗关节炎和其他炎症性疾病。人们意识到其具有抗增殖特性,因此将其另一个用途是用于预防高危人群的结肠息肉。法呢基硫代水杨酸(FTS;Salirasib)旨在抑制致癌 Ras,目前正在 I/II 期和 II 期临床试验中进行评估,我们小组最近发现它对淋巴细胞和肥大细胞均具有抗炎作用。在这里,我们研究了塞来昔布与 FTS 联合使用是否会增强这种抗炎活性。虽然两种药物单独抑制了这些细胞中的 Ras 激活,但联合使用可产生更显著的抑制作用,以及进一步抑制 ERK 磷酸化、淋巴细胞黏附和白细胞介素-2 分泌。此外,这些抑制作用与前列腺素 E2 分泌无关。这些数据表明,联合使用塞来昔布和 FTS 治疗涉及淋巴细胞的炎症性疾病具有很大的潜力。