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Biseugenol Exhibited Anti-Inflammatory and Anti-Asthmatic Effects in an Asthma Mouse Model of Mixed-Granulocytic Asthma

机译:Biseudenol在混合粒细胞哮喘的哮喘小鼠模型中表现出抗炎和抗哮喘作用

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摘要

In the present work, the anti-inflammatory and antiasthmatic potential of biseugenol, isolated as the main component from n-hexane extract from leaves of Nectandra leucantha and chemically prepared using oxidative coupling from eugenol, was evaluated in an experimental model of mixed-granulocytic asthma. Initially, in silico studies of biseugenol showed good predictions for drug-likeness, with adherence to Lipinski’s rules of five (RO5), good Absorption, Distribution, Metabolism and Excretion (ADME) properties and no alerts for Pan-Assay Interference Compounds (PAINS), indicating adequate adherence to perform in vivo assays. Biseugenol (20 mg·kg−1) was thus administered intraperitoneally (four days of treatment) and resulted in a significant reduction in both eosinophils and neutrophils of bronchoalveolar lavage fluid in ovalbumin-sensitized mice with no statistical difference from dexamethasone (5 mg·kg−1). As for lung function parameters, biseugenol (20 mg·kg−1) significantly reduced airway and tissue damping in comparison to ovalbumin group, with similar efficacy to positive control dexamethasone. Airway hyperresponsiveness to intravenous methacholine was reduced with biseugenol but was inferior to dexamethasone in higher doses. In conclusion, biseugenol displayed antiasthmatic effects, as observed through the reduction of inflammation and airway hyperresponsiveness, with similar effects to dexamethasone, on mixed-granulocytic ovalbumin-sensitized mice.
机译:在目前的作品中,在混合粒细胞哮喘的实验模型中评估了来自N-己烷提取物的Biseudugol的抗炎和抗炎潜力,从N-己烷提取物中脱脂,并使用氧化偶联的化学制备。在混合粒细胞哮喘的实验模型中评价。最初,在Biseugenol的Silico研究中表现出对药物相似性的良好预测,遵守Lipinski的五(RO5)的规则,良好的吸收,分布,新陈代谢和排泄(ADME)性质,并且没有针对泛测定干涉化合物的警报(疼痛) ,表明在体内测定中表现足够的依从性。因此腹膜内施用(20mg·kg-1)(治疗4天),导致卵蛋白敏化小鼠的嗜酸性血粒细胞和中性粒细胞的显着减少,与地塞米松没有统计学差异(5 mg·kg -1)。对于肺功能参数,与卵滤液组相比,Biseudenol(20mg·Kg-1)显着降低了气道和组织阻尼,具有与阳性对照塞米松的疗效相似。通过Biseudenol降低了静脉内甲素的气道高反应性,但较低剂量较差。总之,白杨烯醇显示抗炎作用,如通过减少炎症和气道高反应性的观察到,在混合粒细胞蛋白敏化小鼠对地塞米松的效果类似。

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