1. Iridal-Type Triterpenoids Displaying Human Neutrophil Elastase Inhibition and Anti-Inflammatory Effects from Belamcanda chinensis
- Author
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Yeong Jun Ban, Ki Hun Park, Marie Merci Nyiramana, Sang Soo Kang, Aizhamal Baiseitova, Dawon Kang, and Jeong Ho Kim
- Subjects
Lipopolysaccharides ,B. chinensis ,Human neutrophil ,Lipopolysaccharide ,Cell Survival ,medicine.drug_class ,Anti-Inflammatory Agents ,Molecular Conformation ,Pharmaceutical Science ,iridal-type triterpenoids ,Anti-inflammatory ,Article ,Iridaceae ,Analytical Chemistry ,Mice ,chemistry.chemical_compound ,QD241-441 ,Non-competitive inhibition ,Drug Discovery ,medicine ,Animals ,Humans ,Macrophage ,Physical and Theoretical Chemistry ,Binding site ,Cells, Cultured ,chemistry.chemical_classification ,Plant Extracts ,Organic Chemistry ,Elastase ,NF-kappa B ,Triterpenes ,anti-inflammation ,RAW 264.7 Cells ,Enzyme ,Biochemistry ,chemistry ,Chemistry (miscellaneous) ,Molecular Medicine ,Leukocyte Elastase ,human neutrophil elastase - 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.
- Published
- 2021