替米沙坦在实验性诱导的慢性炎症大鼠模型中的抗炎活性：与地塞米松的比较研究。
Anti-inflammatory activity of telmisartan in rat models of experimentally-induced chronic inflammation: Comparative study with dexamethasone.
机构信息
Department of Pharmacology, College of Pharmacy, University of Basrah, Iraq.
出版信息
Saudi Pharm J. 2011 Jan;19(1):29-34. doi: 10.1016/j.jsps.2010.10.004. Epub 2010 Nov 4.
Recently, significant progress has been made through the application of peroxisome proliferator activated receptor-γ (PPAR-γ) agonists as anti-inflammatory drugs that are efficacious, relatively free of side effects, and can be used effectively for a long time. The present study was designed to evaluate the dose-response relationship of the anti-inflammatory activity of telmisartan in rat models of chronic inflammation. The study protocol includes four stages: First stage: 48 rats were allocated into eight groups, each containing six rats, for the study of the anti-inflammatory activity of different doses of telmisartan in rat model of formaldehyde-induced chronic inflammation. Second stage: six rats were used to study the anti-inflammatory activity of telmisartan (1.5 mg/kg) in combination with dexamethasone (0.5 mg/kg) in the same model. Third stage: 48 rats were allocated into eight groups, each containing six rats, for the study of the anti-inflammatory activity of telmisartan in rat model of cotton pellet-induced granuloma. Fourth stage: six rats were used to study the anti-inflammatory activity of telmisartan (1.5 mg/kg) when used as adjuvant with dexamethasone (0.5 mg/kg) in the same model. Telmisartan in a dose-dependent pattern (0.1, 0.2. 0.4, 0.6, 1.5, 3 mg/kg) significantly suppressed inflammation in rat models of formaldehyde-induced chronic inflammation and cotton pellet-induced granuloma. When combined with dexamethasone, telmisartan (1.5 mg/kg body weight) significantly suppressed inflammation in both models, which is significantly higher than all of the effects produced by other approaches of treatment when telmisartan used alone. In conclusion, telmisartan decreased formaldehyde-induced chronic inflammation and cotton-pellet induced granuloma in rats in a dose-dependent pattern. Therefore, it may be considered as a potential treatment for chronic inflammatory conditions in human.
最近，通过应用过氧化物酶体增殖物激活受体-γ（PPAR-γ）激动剂作为有效、副作用相对较少且可长期有效使用的抗炎药物，取得了显著进展。本研究旨在评估替米沙坦在大鼠慢性炎症模型中的抗炎活性的剂量反应关系。研究方案包括四个阶段：第一阶段：将 48 只大鼠分为 8 组，每组 6 只，用于研究不同剂量替米沙坦对甲醛诱导的慢性炎症大鼠模型的抗炎活性。第二阶段：用 6 只大鼠研究替米沙坦（1.5mg/kg）与地塞米松（0.5mg/kg）联合在同一模型中的抗炎活性。第三阶段：将 48 只大鼠分为 8 组，每组 6 只，用于研究替米沙坦对大鼠棉球肉芽肿模型的抗炎活性。第四阶段：用 6 只大鼠研究替米沙坦（1.5mg/kg）作为佐剂与地塞米松（0.5mg/kg）在同一模型中的抗炎活性。替米沙坦呈剂量依赖性（0.1、0.2、0.4、0.6、1.5、3mg/kg）显著抑制甲醛诱导的慢性炎症和大鼠棉球肉芽肿模型的炎症。与地塞米松联合使用时，替米沙坦（1.5mg/kg 体重）显著抑制两种模型的炎症，明显高于替米沙坦单独使用时的其他治疗方法的所有效果。总之，替米沙坦以剂量依赖的方式减少甲醛诱导的慢性炎症和大鼠棉球肉芽肿。因此，它可能被认为是人类慢性炎症疾病的一种潜在治疗方法。
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