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Antinociceptive and anti-inflammatory activities of a triterpene-rich fraction from Himatanthus drasticus

机译:喜马拉雅山富含三萜的馏分的镇痛和抗炎活性

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摘要

Himatanthus drasticus (Mart.) Plumel belongs to the Apocynaceae family and the latex from its trunk bark (Hd) is known as “janaguba milk”. This latex is widely used in Northeast Brazil, mainly in the Cariri region, for its gastroprotective, anti-inflammatory, and antitumor properties. The objective of this study was to investigate a triterpene-rich fraction (FJNB) from H. drasticus latex on acute models of nociception and inflammation and to clarify its mechanisms of action. Wistar rats or Swiss mice were subjected to the carrageenan-induced paw edema test or the formalin test, respectively, after the acute oral treatment with FJNB. The inflamed paws from the carrageenan-induced paw edema and formalin tests were processed for histological and immunohistochemical assays, respectively. The results were analyzed by ANOVA and considered significant at P<0.05. FJNB (10 mg/kg) decreased the paw edema by 25% at the 3rd h after the carrageenan injection. Indomethacin, used as reference, inhibited the paw edema by 59% at the same time-point. In the formalin test, FJNB inhibited the 1st phase by 27, 49, and 52% and the 2nd phase by 37, 50, and 67%, at the doses of 1, 5, and 10 mg/kg, respectively. In addition, FJNB significantly inhibited the expressions of inducible nitric oxide synthase (iNOS), cyclooxygenase-2 (COX-2), and the inflammatory cytokine tumor necrosis factor (TNF)-alpha. The histone deacetylase (HDAC) expression and the transcription factor nuclear factor kappa (NF-kB) were also inhibited at the same doses. In conclusion, the FJNB inhibitory actions on iNOS, COX-2, TNF-α, HDAC, and NF-kB could be involved with the drug anti-inflammatory activity.
机译:Himatanthus drasticus(Mart。)Plumel属于夹竹桃科,其树干树皮(Hd)中的乳胶被称为“ janaguba牛奶”。这种胶乳具有保护胃,消炎和抗肿瘤的特性,因此在巴西东北部(主要在卡里里地区)被广泛使用。这项研究的目的是调查嗜盐链球菌乳汁中富含三萜的部分(FJNB),用于急性伤害感受和炎症模型,并阐明其作用机理。在使用FJNB进行急性口服治疗后,分别对Wistar大鼠或瑞士小鼠进行了角叉菜胶诱发的爪水肿测试或福尔马林测试。角叉菜胶诱发的爪水肿和福尔马林试验中发炎的爪分别进行了组织学和免疫组织化学分析。通过ANOVA分析结果,认为在P <0.05时具有显着性。角叉菜胶注射后第3小时,FJNB(10 mg / kg)使爪水肿减少了25%。吲哚美辛用作参考,在同一时间点抑制爪水肿59%。在福尔马林测试中,FJNB以1、5和10 mg / kg的剂量分别抑制第一阶段27%,49%和52%,抑制第二阶段37%,50%和67%。此外,FJNB显着抑制诱导型一氧化氮合酶(iNOS),环氧合酶2(COX-2)和炎症性细胞因子肿瘤坏死因子(TNF)-α的表达。组蛋白脱乙酰基酶(HDAC)的表达和转录因子核因子kappa(NF-kB)也受到相同剂量的抑制。总之,FJNB对iNOS,COX-2,TNF-α,HDAC和NF-kB的抑制作用可能与药物的抗炎活性有关。

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