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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Main Authors:	Jeong Ho Kim, Yeong Jun Ban, Aizhamal Baiseitova, Marie Merci Nyiramana, Sang Soo Kang, Dawon Kang, Ki Hun Park
Format:	article
Language:	EN
Published:	MDPI AG 2021
Subjects:	<i>B. chinensis</i> iridal-type triterpenoids human neutrophil elastase anti-inflammation Organic chemistry QD241-441
Online Access:	https://doaj.org/article/866b08d6db5e43f28792960fe57c5848
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spelling	oai:doaj.org-article:866b08d6db5e43f28792960fe57c58482021-11-11T18:34:32ZIridal-Type Triterpenoids Displaying Human Neutrophil Elastase Inhibition and Anti-Inflammatory Effects from <i>Belamcanda chinensis</i>10.3390/molecules262166021420-3049https://doaj.org/article/866b08d6db5e43f28792960fe57c58482021-10-01T00:00:00Zhttps://www.mdpi.com/1420-3049/26/21/6602https://doaj.org/toc/1420-3049The 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>.Jeong Ho KimYeong Jun BanAizhamal BaiseitovaMarie Merci NyiramanaSang Soo KangDawon KangKi Hun ParkMDPI AGarticle<i>B. chinensis</i>iridal-type triterpenoidshuman neutrophil elastaseanti-inflammationOrganic chemistryQD241-441ENMolecules, Vol 26, Iss 6602, p 6602 (2021)
institution	DOAJ
collection	DOAJ
language	EN
topic	<i>B. chinensis</i> iridal-type triterpenoids human neutrophil elastase anti-inflammation Organic chemistry QD241-441
spellingShingle	<i>B. chinensis</i> iridal-type triterpenoids human neutrophil elastase anti-inflammation Organic chemistry QD241-441 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>
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>.
format	article
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
title	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_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_sort	iridal-type triterpenoids displaying human neutrophil elastase inhibition and anti-inflammatory effects from <i>belamcanda chinensis</i>
publisher	MDPI AG
publishDate	2021
url	https://doaj.org/article/866b08d6db5e43f28792960fe57c5848
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Iridal-Type Triterpenoids Displaying Human Neutrophil Elastase Inhibition and Anti-Inflammatory Effects from <i>Belamcanda chinensis</i>

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