Abstract
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.
Highlights
Asthma is a chronic inflammatory condition that affects more than 200 million people around the globe, according to the World Health Organization [1,2]
Chemical Characterization and 13 C NMR as well as HRESIMS spectra of natural product were compared with those reported in the literature [9], allowing for the identification of biseugenol (Figure 1)
There is the asthmatic endotype characterized by a high infiltration of both eosinophils and neutrophils on bronchoalveolar lavage fluid, which is denominated mixed-granulocytic asthma and is usually more severe, with high remodeling and reduced pulmonary capacity [15]
Summary
Asthma is a chronic inflammatory condition that affects more than 200 million people around the globe, according to the World Health Organization [1,2]. Molecules 2020, 25, 5384; doi:10.3390/molecules25225384 www.mdpi.com/journal/molecules severe airway obstruction, higher rate of exacerbations and increased health-related costs [5]. For this type of asthma, there is no specific treatment available; a therapy gap exists and must be fulfilled [5]. Molecules 2020, 25, 5384 compounds from this extract, magnolol, acts as an inhibitor of T-lymphocyte proliferation, resulting in corticosteroid-sparing effects in severe asthmatic patients [7]. This compound possesses high structural similarity and to biseugenol
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