Iridal-Type Triterpenoids Displaying Human Neutrophil Elastase Inhibition and Anti-Inflammatory Effects from <i>Belamcanda chinensis</i>
The aim of this study is to explore anti-inflammatory phytochemicals from <i>B. chinensis</i> based on the inhibition of pro-inflammatory enzyme, human neutrophil elastase (HNE) and anti-inflammatory activities in lipopolysaccharide (LPS)-stimulated RAW264.7 macrophage. Three stereoisome...
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MDPI AG
2021-10-01
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| Series: | Molecules |
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| Online Access: | https://www.mdpi.com/1420-3049/26/21/6602 |
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| author | Jeong Ho Kim Yeong Jun Ban Aizhamal Baiseitova Marie Merci Nyiramana Sang Soo Kang Dawon Kang Ki Hun Park |
| author_facet | Jeong Ho Kim Yeong Jun Ban Aizhamal Baiseitova Marie Merci Nyiramana Sang Soo Kang Dawon Kang Ki Hun Park |
| author_sort | Jeong Ho Kim |
| collection | DOAJ |
| description | The aim of this study is to explore anti-inflammatory phytochemicals from <i>B. chinensis</i> 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 (<b>1</b>–<b>3</b>) were isolated from the roots of <i>B. chinensis</i> and their stereochemistries were completely identified by NOESY spectra. These compounds were confirmed as reversible noncompetitive inhibitors against HNE with IC<sub>50</sub> 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 (<b>1</b>) and iridobelamal A (<b>2</b>) 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 <i>B. chinensis</i>. |
| first_indexed | 2024-03-10T05:55:57Z |
| format | Article |
| id | doaj.art-866b08d6db5e43f28792960fe57c5848 |
| institution | Directory Open Access Journal |
| issn | 1420-3049 |
| language | English |
| last_indexed | 2024-03-10T05:55:57Z |
| publishDate | 2021-10-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Molecules |
| spelling | doaj.art-866b08d6db5e43f28792960fe57c58482023-11-22T21:23:45ZengMDPI AGMolecules1420-30492021-10-012621660210.3390/molecules26216602Iridal-Type Triterpenoids Displaying Human Neutrophil Elastase Inhibition and Anti-Inflammatory Effects from <i>Belamcanda chinensis</i>Jeong Ho Kim0Yeong Jun Ban1Aizhamal Baiseitova2Marie Merci Nyiramana3Sang Soo Kang4Dawon Kang5Ki Hun Park6Division of Applied Life Science (BK21 plus), IALS, Gyeongsang National University, Jinju 52828, KoreaDivision of Applied Life Science (BK21 plus), IALS, Gyeongsang National University, Jinju 52828, KoreaDivision of Applied Life Science (BK21 plus), IALS, Gyeongsang National University, Jinju 52828, KoreaDepartment of Physiology, College of Medicine and Institute of Health Sciences, Gyeongsang National University, Jinju 52727, KoreaDepartment of Anatomy, Institute of Health Sciences, College of Medicine, Gyeongsang National University, Jinju 52727, KoreaDepartment of Physiology, College of Medicine and Institute of Health Sciences, Gyeongsang National University, Jinju 52727, KoreaDivision of Applied Life Science (BK21 plus), IALS, Gyeongsang National University, Jinju 52828, KoreaThe aim of this study is to explore anti-inflammatory phytochemicals from <i>B. chinensis</i> 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 (<b>1</b>–<b>3</b>) were isolated from the roots of <i>B. chinensis</i> and their stereochemistries were completely identified by NOESY spectra. These compounds were confirmed as reversible noncompetitive inhibitors against HNE with IC<sub>50</sub> 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 (<b>1</b>) and iridobelamal A (<b>2</b>) 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 <i>B. chinensis</i>.https://www.mdpi.com/1420-3049/26/21/6602<i>B. chinensis</i>iridal-type triterpenoidshuman neutrophil elastaseanti-inflammation |
| spellingShingle | Jeong Ho Kim Yeong Jun Ban Aizhamal Baiseitova Marie Merci Nyiramana Sang Soo Kang Dawon Kang Ki Hun Park Iridal-Type Triterpenoids Displaying Human Neutrophil Elastase Inhibition and Anti-Inflammatory Effects from <i>Belamcanda chinensis</i> Molecules <i>B. chinensis</i> iridal-type triterpenoids human neutrophil elastase anti-inflammation |
| title | Iridal-Type Triterpenoids Displaying Human Neutrophil Elastase Inhibition and Anti-Inflammatory Effects from <i>Belamcanda chinensis</i> |
| title_full | Iridal-Type Triterpenoids Displaying Human Neutrophil Elastase Inhibition and Anti-Inflammatory Effects from <i>Belamcanda chinensis</i> |
| title_fullStr | Iridal-Type Triterpenoids Displaying Human Neutrophil Elastase Inhibition and Anti-Inflammatory Effects from <i>Belamcanda chinensis</i> |
| title_full_unstemmed | Iridal-Type Triterpenoids Displaying Human Neutrophil Elastase Inhibition and Anti-Inflammatory Effects from <i>Belamcanda chinensis</i> |
| title_short | Iridal-Type Triterpenoids Displaying Human Neutrophil Elastase Inhibition and Anti-Inflammatory Effects from <i>Belamcanda chinensis</i> |
| title_sort | iridal type triterpenoids displaying human neutrophil elastase inhibition and anti inflammatory effects from i belamcanda chinensis i |
| topic | <i>B. chinensis</i> iridal-type triterpenoids human neutrophil elastase anti-inflammation |
| url | https://www.mdpi.com/1420-3049/26/21/6602 |
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