Experimental Physiopathology Laboratory, University of the Extreme-South Catarinense, Criciúma, SC, Brazil.
Inflamm Res. 2010 Sep;59(9):783-9. doi: 10.1007/s00011-010-0190-8. Epub 2010 Apr 3.
We report the effects of the gastrin-releasing peptide (GRP) receptor antagonist RC-3095 in an acute inflammation model induced by carrageenan.
Male Wistar rats received saline or saline containing 2% lambda-carrageenan into the pleural cavity, with some also receiving RC-3095 3 mg/kg subcutaneously, immediately after surgery. Four hours later, the rats were killed and pleural exudate was obtained for evaluation of total cell count, lactate dehydrogenase activity, total protein, cytokines analysis and nitrite/nitrate concentrations; myeloperoxidase (MPO) activity and oxidative stress were evaluated in the lung.
RC-3095 exhibited pronounced anti-inflammatory actions by inhibition of leukocyte influx and blockade of MPO, nitrite/nitrate and cytokine levels. Moreover, the results showed that RC-3095 elicits action against oxidative damage in lipids and proteins, as well as increasing cell viability.
The present findings suggest that GRP plays a role in acute inflammation that can be related with the reduction of oxidative damage and that it could be effective in therapeutic applications.
我们报告胃泌素释放肽(GRP)受体拮抗剂 RC-3095 在角叉菜胶诱导的急性炎症模型中的作用。
雄性 Wistar 大鼠接受盐水或含有 2% lambda-角叉菜胶的盐水注入胸腔,其中一些大鼠在手术后立即接受皮下注射 3mg/kg 的 RC-3095。4 小时后,处死大鼠并获得胸腔渗出液,以评估总细胞计数、乳酸脱氢酶活性、总蛋白、细胞因子分析和亚硝酸盐/硝酸盐浓度;在肺中评估髓过氧化物酶(MPO)活性和氧化应激。
RC-3095 通过抑制白细胞浸润和阻断 MPO、亚硝酸盐/硝酸盐和细胞因子水平,表现出明显的抗炎作用。此外,结果表明 RC-3095 可引发对脂质和蛋白质的氧化损伤的作用,并增加细胞活力。
目前的研究结果表明,GRP 在急性炎症中发挥作用,这可能与氧化损伤的减少有关,并且它可能在治疗应用中有效。