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3,4-二氢-2,2-二甲基-2H-萘并[1,2-b]吡喃-5,6-二酮(β-拉帕醌)的抗炎和抗关节炎活性。

Anti-inflammatory and anti-arthritic activities of 3,4-dihydro-2,2-dimethyl-2H-naphthol[1,2-b]pyran-5,6-dione (β-lapachone).

机构信息

Department of Antibiotics, Federal University of Pernambuco, Rua Prof. Artur Sá, Cidade Universitária, Recife/PE, Brazil.

出版信息

Inflamm Res. 2013 Jan;62(1):107-13. doi: 10.1007/s00011-012-0557-0. Epub 2012 Sep 28.

Abstract

OBJECTIVE AND DESIGN

The purpose of this study was to evaluate the anti-inflammatory and anti-arthritic activities of 3,4-dihydro-2,2-dimethyl-2H-naphthol[1,2-b]pyran-5,6-dione (β-lapachone; β-lap) and to elucidate its probable mode of action.

METHODS

Carrageenan-induced paw edema, cell migration evaluation and production of pro-inflammatory cytokines tumor necrosis factor (TNF)-α, interleukin (IL)-6 and nitric oxide were used for this study. Freund's complete adjuvant (FCA)-induced arthritis was used as a model of chronic inflammation. β-Lap was tested in doses of 40 and 60 mg/kg, orally.

RESULTS

In the paw edema test, the dose of 60 mg/kg gave a higher percentage inhibition of edema (49.3 %) than control. β-Lap inhibited neutrophil migration and reduced concentrations of TNF-α, IL-6 and NO in peritoneal exudates of animals with peritonitis. In the arthritis test, β-lap inhibited edema and NO production in the serum of treated animals.

CONCLUSION

Significant anti-inflammatory and anti-arthritic activities were observed in animals treated with β-lap. The effects of β-lap can be attributed in part to immunomodulation with reduction of pro-inflammatory cytokines and NO.

摘要

目的和设计

本研究旨在评估 3,4-二氢-2,2-二甲基-2H-萘酚[1,2-b]吡喃-5,6-二酮(β-拉帕酮;β-拉帕)的抗炎和抗关节炎活性,并阐明其可能的作用机制。

方法

本研究采用角叉菜胶诱导的爪肿胀、细胞迁移评估以及促炎细胞因子肿瘤坏死因子(TNF)-α、白细胞介素(IL)-6 和一氧化氮的产生来进行研究。弗氏完全佐剂(FCA)诱导的关节炎被用作慢性炎症模型。β-拉帕以 40 和 60mg/kg 的剂量口服进行测试。

结果

在爪肿胀试验中,60mg/kg 的剂量对水肿的抑制率(49.3%)高于对照组。β-拉帕抑制中性粒细胞迁移,并降低腹膜炎动物腹腔渗出液中 TNF-α、IL-6 和 NO 的浓度。在关节炎试验中,β-拉帕抑制了治疗动物血清中的水肿和 NO 生成。

结论

β-拉帕治疗的动物表现出显著的抗炎和抗关节炎活性。β-拉帕的作用部分归因于免疫调节,可降低促炎细胞因子和 NO。

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