Abstract
The aim of this study is to explore anti-inflammatory phytochemicals from B. chinensis based on the inhibition of pro-inflammatory enzyme, human neutrophil elastase (HNE) and anti-inflammatory activities in lipopolysaccharide (LPS)-stimulated RAW264.7 macrophage. Three stereoisomers of iridal-type triterpenoids (1–3) were isolated from the roots of B. chinensis and their stereochemistries were completely identified by NOESY spectra. These compounds were confirmed as reversible noncompetitive inhibitors against HNE with IC50 values of 6.8–27.0 µM. The binding affinity experiment proved that iridal-type triterpenoids had only a single binding site to the HNE enzyme. Among them, isoiridogermanal (1) and iridobelamal A (2) displayed significant anti-inflammatory effects by suppressing the expressions of pro-inflammatory cytokines, such as iNOS, IL-1β, and TNF-α through the NF-κB pathway in LPS-stimulated RAW264.7 cells. This is the first report that iridal-type triterpenoids are considered responsible phytochemicals for anti-inflammatory effects of B. chinensis.
Highlights
Publisher’s Note: MDPI stays neutral with regard to jurisdictional claims in published maps and institutional affiliations
Belamcanda chinensis (L.) DC known as She Gan has been used in Traditional Chinese
Medicine (TCM) for the clinical treatment of respiratory diseases including bronchitis, asthma, sore throat and so on [1], which have been listed in Chinese Pharmacopoeia
Summary
Publisher’s Note: MDPI stays neutral with regard to jurisdictional claims in published maps and institutional affiliations. Belamcanda chinensis (L.) DC known as She Gan has been used in Traditional Chinese. Medicine (TCM) for the clinical treatment of respiratory diseases including bronchitis, asthma, sore throat and so on [1], which have been listed in Chinese Pharmacopoeia (Committee for the Pharmacopoeia of P.R. China, 2015). The phytochemical constituents of B. chinensis are flavonoids including isoflavones, flavones, and flavonols [3]. Many reports elucidated that isoflavones are major metabolites among phenolic compounds and the uniqueness of this plant is to have triterpenoids with iridal skeleton [4]. This study focused on the phytochemicals which could be attributed to the anti-inflammation potential of B. chinensis, based on human neutrophil elastase (HNE)
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