Department of Clinical and Experimental Medicine and Pharmacology, School of Medicine, University of Messina, Italy.
Respir Res. 2010 Feb 22;11(1):19. doi: 10.1186/1465-9921-11-19.
Liver x receptor alpha (LXRalpha) and beta (LXRbeta) are members of the nuclear receptor super family of ligand-activated transcription factors, a super family which includes the perhaps better known glucocorticoid receptor, estrogen receptor, thyroid receptor, and peroxisome proliferator-activated receptors. There is limited evidence that LXL activation may reduces acute lung inflammation. The aim of this study was to investigate the effects of T0901317, a potent LXR receptor ligand, in a mouse model of carrageenan-induced pleurisy.
Injection of carrageenan into the pleural cavity of mice elicited an acute inflammatory response characterized by: accumulation of fluid containing a large number of neutrophils (PMNs) in the pleural cavity, infiltration of PMNs in lung tissues and subsequent lipid peroxidation, and increased production of nitrite/nitrate (NOx), tumor necrosis factor-alpha, (TNF-alpha) and interleukin-1beta (IL-1beta). Furthermore, carrageenan induced the expression of iNOS, nitrotyrosine and PARP, as well as induced apoptosis (TUNEL staining and Bax and Bcl-2 expression) in the lung tissues.
Administration of T0901317, 30 min after the challenge with carrageenan, caused a significant reduction in a dose dependent manner of all the parameters of inflammation measured.
Thus, based on these findings we propose that LXR ligand such as T0901317, may be useful in the treatment of various inflammatory diseases.
肝 X 受体α(LXRα)和β(LXRβ)是核受体超家族配体激活转录因子的成员,该超家族包括更为人熟知的糖皮质激素受体、雌激素受体、甲状腺受体和过氧化物酶体增殖物激活受体。有有限的证据表明 LXL 激活可能减轻急性肺炎症。本研究的目的是研究 T0901317(一种有效的 LXR 受体配体)在卡拉胶诱导胸膜炎的小鼠模型中的作用。
向小鼠胸膜腔注射卡拉胶可引发急性炎症反应,其特征为:胸膜腔内积聚含有大量中性粒细胞(PMN)的液体、PMN 在肺组织中的浸润以及随后的脂质过氧化作用,以及亚硝酸盐/硝酸盐(NOx)、肿瘤坏死因子-α(TNF-α)和白细胞介素-1β(IL-1β)的产生增加。此外,卡拉胶诱导 iNOS、硝基酪氨酸和 PARP 的表达,并在肺组织中诱导细胞凋亡(TUNEL 染色和 Bax 和 Bcl-2 表达)。
在卡拉胶挑战后 30 分钟给予 T0901317 可显著降低所有炎症参数的剂量依赖性。
因此,基于这些发现,我们提出 LXR 配体如 T0901317 可能对各种炎症性疾病的治疗有用。