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从无苞片威尔布兰迪亚(Wilbrandia ebracteata Cogn.)中分离出的一种三萜类化合物的抗炎作用

Anti-inflammatory effects of a triterpenoid isolated from Wilbrandia ebracteata Cogn.

作者信息

Siqueira Jarbas Mota, Peters Rodrigo Rebelo, Gazola Andressa Córneo, Krepsky Patrícia Baier, Farias Mareni Rocha, Rae Giles Alexander, de Brum-Fernandes Artur José, Ribeiro-do-Valle Rosa Maria

机构信息

Department of Pharmacology - Federal University of Santa Catarina, Florianópolis, SC, Brazil.

出版信息

Life Sci. 2007 Mar 20;80(15):1382-7. doi: 10.1016/j.lfs.2006.12.021. Epub 2007 Jan 11.

DOI:10.1016/j.lfs.2006.12.021
PMID:17286991
Abstract

Wilbrandia ebracteata (WE), a Brazilian medicinal plant used in folk medicine for the treatment of rheumatic diseases, displays anti-inflammatory properties and constitutes a rich source of cucurbitacins and cucurbitacin-related compounds. The current study investigated the potential anti-inflammatory properties of Dihydrocucurbitacin B (DHCB), a cucurbitacin-derived compound isolated from roots of WE, in some in vivo and in vitro experimental models. Intraperitoneal treatment of mice with DHCB reduced both carrageenan-induced paw edema (0.3, 1 and 3 mg/kg caused inhibitions of 26, 44 and 56 % at 2 h after stimulation, respectively) and pleurisy (10 mg/kg inhibited leukocyte numbers and LTB(4) levels in the pleural fluid by 51 and 75% at 6 h after cavity challenge, respectively). In vitro, DHCB (up to 10 microg/mL) failed to modify LTB(4) production by human neutrophils or PGE(2) production by COS-7 cells transfected with COX-1, but PGE(2) production by COX-2 transfected COS-7 cells was markedly inhibited (by 72%). The levels of COX-1 or COX-2 proteins in IL-1alpha-stimulated NIH3T3 cells were unaffected by DHCB. The results corroborate the potential anti-inflammatory properties ascribed to W. ebracteata Cogn. in folk medicine and suggest that they might be attributed, at least in part, to the capacity of one of this plants main constituents, DHCB, to inhibit COX-2 activity (but not its expression) during inflammation.

摘要

威尔布兰迪亚无苞片植物(WE)是一种巴西药用植物,在民间医学中用于治疗风湿性疾病,具有抗炎特性,是葫芦素和葫芦素相关化合物的丰富来源。本研究在一些体内和体外实验模型中,研究了从WE根部分离出的葫芦素衍生化合物二氢葫芦素B(DHCB)的潜在抗炎特性。用DHCB腹腔注射处理小鼠,可减轻角叉菜胶诱导的爪肿胀(0.3、1和3mg/kg分别在刺激后2小时引起26%、44%和56%的抑制)和胸膜炎(10mg/kg在胸腔攻击后6小时分别使胸腔积液中的白细胞数量和白三烯B4(LTB4)水平抑制51%和75%)。在体外,DHCB(高达10μg/mL)未能改变人中性粒细胞产生LTB4或转染COX-1的COS-7细胞产生前列腺素E2(PGE2)的情况,但转染COX-2的COS-7细胞产生PGE2的情况受到明显抑制(抑制率为72%)。DHCB不影响IL-1α刺激的NIH3T3细胞中COX-1或COX-2蛋白的水平。这些结果证实了民间医学中赋予威尔布兰迪亚无苞片植物的潜在抗炎特性,并表明它们可能至少部分归因于该植物的主要成分之一DHCB在炎症过程中抑制COX-2活性(而非其表达)的能力。

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