Anti-<i>Helicobacter pylori</i> and Anti-Inflammatory Sesquiterpenoids from the Rhizoma of <i>Atractylodes macrocephala</i>

<i>Helicobacter pylori</i>, a spiral-shaped bacterium found in the stomach, is associated with various gastrointestinal and systemic health conditions. Effective suppression of <i>H. pylori</i> is therefore critical for managing gastrointestinal diseases. In a search for natu...

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Main Authors: So Yeong Jeong, Dong-Min Kang, Hyun-Jun Kim, Sang Won Yeon, Hak Hyun Lee, Min Hee Kim, Bang Yeon Hwang, Mi-Jeong Ahn, Mi Kyeong Lee
Format: Article
Language:English
Published: MDPI AG 2025-07-01
Series:Molecules
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Online Access:https://www.mdpi.com/1420-3049/30/15/3142
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author So Yeong Jeong
Dong-Min Kang
Hyun-Jun Kim
Sang Won Yeon
Hak Hyun Lee
Min Hee Kim
Bang Yeon Hwang
Mi-Jeong Ahn
Mi Kyeong Lee
author_facet So Yeong Jeong
Dong-Min Kang
Hyun-Jun Kim
Sang Won Yeon
Hak Hyun Lee
Min Hee Kim
Bang Yeon Hwang
Mi-Jeong Ahn
Mi Kyeong Lee
author_sort So Yeong Jeong
collection DOAJ
description <i>Helicobacter pylori</i>, a spiral-shaped bacterium found in the stomach, is associated with various gastrointestinal and systemic health conditions. Effective suppression of <i>H. pylori</i> is therefore critical for managing gastrointestinal diseases. In a search for natural products with anti-<i>H. pylori</i> activity, the extract of <i>Atractylodes macrocephala</i> rhizoma showed significant inhibitory effects. Chromatographic purification of <i>A. macrocephala</i> extract yielded thirteen compounds, which were identified as ten sesquiterpenes and three polyacetylenes by spectroscopic analysis. The sesquiterpene compounds belong to the eudesmane or eudesmane lactone types and exhibited structure-dependent efficacy. The major eudesmane lactone sesquiterpene, atractylenolide I (<b>1</b>), showed strong inhibitory activity comparable to metronidazole, a positive control, and atractylenolide III (<b>3</b>) also showed good efficacy. However, structural modification such as hydroxylation, methylation, or acetylation of the sesquiterpenes led to reduced activity. In contrast, polyacetylene derivatives displayed only mild inhibitory effects. Further evaluation of the active compounds against three <i>H. pylori</i> strains such as 51, 43504, and 26695 showed that atractylenolide I (<b>1</b>) had potent inhibitory effects against all three strains, with MIC<sub>50</sub> values of ranging from 27.3 to 48.6 μM and MIC<sub>90</sub> values from 45.4 to 87.2 μM. Atractylenolide III (<b>3</b>) exhibited selective activity against strain 51 with MIC<sub>50</sub> value of 89.9 μM. Both compounds also exhibited anti-inflammatory activity with IC<sub>90</sub> values of 23.3 and 31.1 μM, respectively, although they showed little effect on urease. This is the first report on the anti-<i>H. pylori</i> efficacy of various constituents of <i>A. macrocephala</i> and comparative analysis of inhibitory effects against several strains, which will provide scientific evidence supporting its potential as therapeutic agent for <i>H. pylori</i>-related infection.
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spelling doaj-art-10f75b3dcd6c413d89cdab4f72fea4ae2025-08-20T03:02:55ZengMDPI AGMolecules1420-30492025-07-013015314210.3390/molecules30153142Anti-<i>Helicobacter pylori</i> and Anti-Inflammatory Sesquiterpenoids from the Rhizoma of <i>Atractylodes macrocephala</i>So Yeong Jeong0Dong-Min Kang1Hyun-Jun Kim2Sang Won Yeon3Hak Hyun Lee4Min Hee Kim5Bang Yeon Hwang6Mi-Jeong Ahn7Mi Kyeong Lee8College of Pharmacy, Chungbuk National University, Cheongju 28160, Republic of KoreaCollege of Pharmacy and Research Institute of Pharmaceutical Sciences, Gyeongsang National University, Jinju 52828, Republic of KoreaForest Medicinal Resources Research Center, National Institute of Forest Science, Yeongju 36040, Republic of KoreaCollege of Pharmacy, Chungbuk National University, Cheongju 28160, Republic of KoreaCollege of Pharmacy, Chungbuk National University, Cheongju 28160, Republic of KoreaCollege of Pharmacy, Chungbuk National University, Cheongju 28160, Republic of KoreaCollege of Pharmacy, Chungbuk National University, Cheongju 28160, Republic of KoreaCollege of Pharmacy and Research Institute of Pharmaceutical Sciences, Gyeongsang National University, Jinju 52828, Republic of KoreaCollege of Pharmacy, Chungbuk National University, Cheongju 28160, Republic of Korea<i>Helicobacter pylori</i>, a spiral-shaped bacterium found in the stomach, is associated with various gastrointestinal and systemic health conditions. Effective suppression of <i>H. pylori</i> is therefore critical for managing gastrointestinal diseases. In a search for natural products with anti-<i>H. pylori</i> activity, the extract of <i>Atractylodes macrocephala</i> rhizoma showed significant inhibitory effects. Chromatographic purification of <i>A. macrocephala</i> extract yielded thirteen compounds, which were identified as ten sesquiterpenes and three polyacetylenes by spectroscopic analysis. The sesquiterpene compounds belong to the eudesmane or eudesmane lactone types and exhibited structure-dependent efficacy. The major eudesmane lactone sesquiterpene, atractylenolide I (<b>1</b>), showed strong inhibitory activity comparable to metronidazole, a positive control, and atractylenolide III (<b>3</b>) also showed good efficacy. However, structural modification such as hydroxylation, methylation, or acetylation of the sesquiterpenes led to reduced activity. In contrast, polyacetylene derivatives displayed only mild inhibitory effects. Further evaluation of the active compounds against three <i>H. pylori</i> strains such as 51, 43504, and 26695 showed that atractylenolide I (<b>1</b>) had potent inhibitory effects against all three strains, with MIC<sub>50</sub> values of ranging from 27.3 to 48.6 μM and MIC<sub>90</sub> values from 45.4 to 87.2 μM. Atractylenolide III (<b>3</b>) exhibited selective activity against strain 51 with MIC<sub>50</sub> value of 89.9 μM. Both compounds also exhibited anti-inflammatory activity with IC<sub>90</sub> values of 23.3 and 31.1 μM, respectively, although they showed little effect on urease. This is the first report on the anti-<i>H. pylori</i> efficacy of various constituents of <i>A. macrocephala</i> and comparative analysis of inhibitory effects against several strains, which will provide scientific evidence supporting its potential as therapeutic agent for <i>H. pylori</i>-related infection.https://www.mdpi.com/1420-3049/30/15/3142<i>Atractylodes macrocephala</i>anti-<i>Helicobacter pylori</i>sesquiterpeneatractylenolide Ianti-inflammatory
spellingShingle So Yeong Jeong
Dong-Min Kang
Hyun-Jun Kim
Sang Won Yeon
Hak Hyun Lee
Min Hee Kim
Bang Yeon Hwang
Mi-Jeong Ahn
Mi Kyeong Lee
Anti-<i>Helicobacter pylori</i> and Anti-Inflammatory Sesquiterpenoids from the Rhizoma of <i>Atractylodes macrocephala</i>
Molecules
<i>Atractylodes macrocephala</i>
anti-<i>Helicobacter pylori</i>
sesquiterpene
atractylenolide I
anti-inflammatory
title Anti-<i>Helicobacter pylori</i> and Anti-Inflammatory Sesquiterpenoids from the Rhizoma of <i>Atractylodes macrocephala</i>
title_full Anti-<i>Helicobacter pylori</i> and Anti-Inflammatory Sesquiterpenoids from the Rhizoma of <i>Atractylodes macrocephala</i>
title_fullStr Anti-<i>Helicobacter pylori</i> and Anti-Inflammatory Sesquiterpenoids from the Rhizoma of <i>Atractylodes macrocephala</i>
title_full_unstemmed Anti-<i>Helicobacter pylori</i> and Anti-Inflammatory Sesquiterpenoids from the Rhizoma of <i>Atractylodes macrocephala</i>
title_short Anti-<i>Helicobacter pylori</i> and Anti-Inflammatory Sesquiterpenoids from the Rhizoma of <i>Atractylodes macrocephala</i>
title_sort anti i helicobacter pylori i and anti inflammatory sesquiterpenoids from the rhizoma of i atractylodes macrocephala i
topic <i>Atractylodes macrocephala</i>
anti-<i>Helicobacter pylori</i>
sesquiterpene
atractylenolide I
anti-inflammatory
url https://www.mdpi.com/1420-3049/30/15/3142
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