腺苷A2A受体激动剂CGS 21680不能改善葡聚糖硫酸钠诱导的小鼠结肠炎病程。
The adenosine A2A receptor agonist CGS 21680 fails to ameliorate the course of dextran sulphate-induced colitis in mice.
作者信息
Selmeczy Z, Csóka B, Pacher P, Vizi E S, Haskó G
机构信息
Department of Pharmacology, Institute of Experimental Medicine, Hungarian Academy of Sciences, Budapest, Hungary.
出版信息
Inflamm Res. 2007 May;56(5):204-9. doi: 10.1007/s00011-006-6150-7.
OBJECTIVE
In this study we investigated the effect of CGS 21680 (2-p-(2-Carboxyethyl)phenethylamino-5-N-ethylcarboxamidoadenosine hydrochloride), an adenosine A2A receptor agonist, in a model of dextran sulphate sodium (DSS)-induced colitis.
METHODS
NMRI mice were fed 5 % (w/v) DSS, and were treated intraperitoneally with 0.5 mg/kg CGS 21680 or vehicle for 10 days. Changes of bodyweight, colon length, the incidence of rectal bleeding, levels of macrophage inflammatory protein (MIP)-1alpha, MIP-2, interferon gamma, interleukin (IL)-1beta, IL-12 and tumour necrosis factor-alpha from homogenates of colon biopsies, and the release of [3H]acetylcholine (ACh) from longitudinal muscle strip were determined.
RESULTS
DSS significantly decreased bodyweight, colon length, and it increased the incidence of rectal bleeding and levels of MIP-1alpha, MIP-2 and IL-1beta compared to DSS-untreated animals. CGS 21680 had no effect on these changes. No change could be observed in release of ACh in DSS-induced colitis with or without CGS 21680.
CONCLUSION
In summary, CGS 21680 is ineffective in ameliorating DSS-induced colitis in mice.
目的
在本研究中，我们调查了腺苷A2A受体激动剂CGS 21680（2 - 对 -（2 - 羧乙基）苯乙氨基 - 5 - N - 乙基甲酰胺基腺苷盐酸盐）在葡聚糖硫酸钠（DSS）诱导的结肠炎模型中的作用。
方法
给NMRI小鼠喂食5%（w/v）的DSS，并腹腔注射0.5 mg/kg的CGS 21680或赋形剂，持续10天。测定体重变化、结肠长度、直肠出血发生率、结肠活检匀浆中巨噬细胞炎性蛋白（MIP）-1α、MIP - 2、干扰素γ、白细胞介素（IL）-1β、IL - 12和肿瘤坏死因子 - α的水平，以及纵向肌条中[3H]乙酰胆碱（ACh）的释放。
结果
与未用DSS处理的动物相比，DSS显著降低了体重和结肠长度，并增加了直肠出血发生率以及MIP - 1α、MIP - 2和IL - 1β的水平。CGS 21680对这些变化没有影响。在有或没有CGS 21680的DSS诱导的结肠炎中，未观察到ACh释放的变化。
结论
总之，CGS 21680在改善小鼠DSS诱导的结肠炎方面无效。
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