抗肿瘤药物羧胺三唑的抗炎镇痛作用  

Anti-inflammatory and Analgesic Potency of Carboxyamidotriazole,a Tumoristatic Agent

作　　者：郭磊[1] 李娟[1] 叶华[1] 郑茹[1] 郝晓健[1] 陈文颖[1] 鞠瑞[1] 姚伊人[1] 杨惠芬[1] 于晓丽[1] 叶菜英[1] 张德昌[1] 

机构地区：[1]中国医学科学院北京协和医学院基础医学研究所药理室,北京100005

出　　处：《中国医学科学院学报》2009年第3期315-321,I0002,共8页Acta Academiae Medicinae Sinicae

基　　金：科技部国际合作项目(2005DFA31110)~~

摘　　要：目的探讨抗肿瘤药物羧胺三唑(CAI)是否具有抗炎镇痛作用并初步考察其作用机制。方法采用巴豆油诱导小鼠耳肿胀模型、棉球肉芽肿模型和大鼠佐剂性关节炎模型评价CAI的抗炎作用。检测CAI对血管内皮生长因子(VEGF)或组胺诱导的小鼠背部皮肤局部血管通透性的影响,以及对炎症部位和血清中致炎细胞因子肿瘤坏死因子α(TNF-α)和白细胞介素1β(IL-1β)水平的影响。采用醋酸致小鼠扭体模型和福尔马林致痛模型评价CAI的镇痛作用。结果CAI对急慢性炎症均有明显抑制作用,对VEGF或组胺诱导的血管通透性增加有明显缓解作用,对致炎细胞因子TNF-α和IL-1β有明显抑制作用。CAI对外周炎性疼痛也有明显治疗作用。结论CAI是一种极具开发潜力的抗炎镇痛物质。Objective To explore the potential anti-inflammatory and analgesic activities of carboxyamidotriazole （CAI）. Methods A variety of animal models, including the croton oil-induced ear edema, the cotton-induced granuloma, the rat adjuvant-induced arthritis, were used to evaluate anti-inflammatory effect of CAl. Vascular endothelial growth factor （VEGF） - or histamine-stimulated local vascular permeability in mouse modulated by CAI was also determined. In addition, we assessed the effect of CAI on the levels of proinflammatory cytokines tumor necrosis factor-or （TNF-α） and interleukin-1β （IL-1β） at the site of inflammation and in sera. Moreover, antinociceptive effect of CAI on inflammatory pain was assessed using acetic acidinduced writhing model and the formalin test. Results CAI significantly inhibited acute and chronic phases of inflammation, reduced VEGF or histamine-induced vascular permeability, and showed marked inhibition of proinflammatory eytokines such as TNF-α and IL-1 β. CAI also showed potential therapeutic effect on peripheral inflammatory pain. Conclusion CAI is a promising anti-inflammatory and analgesic agent.

关 键 词：羧胺三唑 抗炎作用 镇痛作用 

分 类 号：R961[医药卫生—药理学]