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从丁公藤茎中分离得到的东莨菪苷通过抑制炎症和血管生成来抑制佐剂诱导的大鼠关节炎。

Scopolin isolated from Erycibe obtusifolia Benth stems suppresses adjuvant-induced rat arthritis by inhibiting inflammation and angiogenesis.

作者信息

Pan Rong, Dai Yue, Gao Xinghua, Xia Yufeng

机构信息

Department of Pharmacology of Chinese Materia Medica, China Pharmaceutical University, 1 Shennong Road, Nanjing, Jiangsu Province, China.

出版信息

Int Immunopharmacol. 2009 Jul;9(7-8):859-69. doi: 10.1016/j.intimp.2009.02.019. Epub 2009 Mar 25.

Abstract

Despite scopolin is a main coumarin constituent in the stems of Erycibe obtusifolia Benth, a herb drug that has long been utilized in traditional Chinese medicine for the treatment of rheumatoid arthritis, little information is available about the pharmacological activities of this compound. The present study was performed to investigate the anti-rheumatic effects of scopolin in adjuvant-induced arthritis (AIA) in rats, and explore the underlying mechanisms of action in views of anti-inflammatory and anti-angiogenic properties in the synovial tissues. Scopolin (50, 100 mg/kg), injected intraperitoneally for 10 days from the onset of secondary response, significantly inhibited both inoculated and non-inoculated paw swelling as well as articular index scores in AIA. Meanwhile, the mean body weight of rats treated with scopolin was higher than that of model group. Rats treated with high dose of scopolin (100 mg/kg) preserved a nearly normal histological architecture of the joints and showed a significant reduction of the new blood vessels in the synovial tissues. Additionally, scopolin could reduce IL-6, VEGF and FGF-2 expressions in rat synovial tissues. In conclusion, scopolin can reduce the clinical symptoms of rat AIA by inhibiting inflammation and angiogenesis, and this compound may be a potent agent for angiogenesis related diseases and can serve as a structural base for screening more potent synthetic analogs.

摘要

尽管东莨菪苷是丁公藤茎中的主要香豆素成分,丁公藤是一种长期用于治疗类风湿性关节炎的中药,但关于该化合物的药理活性的信息却很少。本研究旨在探讨东莨菪苷对大鼠佐剂性关节炎(AIA)的抗风湿作用,并从滑膜组织的抗炎和抗血管生成特性方面探讨其潜在的作用机制。从二次反应开始腹腔注射东莨菪苷(50、100mg/kg),连续10天,可显著抑制AIA中接种和未接种爪的肿胀以及关节指数评分。同时,东莨菪苷治疗的大鼠平均体重高于模型组。高剂量东莨菪苷(100mg/kg)治疗的大鼠关节组织学结构接近正常,滑膜组织中的新生血管显著减少。此外,东莨菪苷可降低大鼠滑膜组织中IL-6、VEGF和FGF-2的表达。总之,东莨菪苷可通过抑制炎症和血管生成来减轻大鼠AIA的临床症状,该化合物可能是治疗血管生成相关疾病的有效药物,并可作为筛选更有效合成类似物的结构基础。

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