Anti-Amyloid Aggregation Effects of Gobaishi (<i>Galla chinensis</i>) and Its Active Constituents

Alzheimer′s disease (AD) is a chronic neurodegenerative disorder that leads to memory loss and changes in mental and behavioral functions in elderly individuals. A major pathological feature of AD is the aggregation of amyloid-beta (Aβ) peptides, along with oxidative stress, inducing neurocellular a...

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Main Authors: Sharmin Akter, Takayuki Tohge, Sahithya Hulimane Ananda, Masahiro Kuragano, Kiyotaka Tokuraku, Koji Uwai
Format: Article
Language:English
Published: MDPI AG 2025-06-01
Series:Molecules
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Online Access:https://www.mdpi.com/1420-3049/30/13/2720
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author Sharmin Akter
Takayuki Tohge
Sahithya Hulimane Ananda
Masahiro Kuragano
Kiyotaka Tokuraku
Koji Uwai
author_facet Sharmin Akter
Takayuki Tohge
Sahithya Hulimane Ananda
Masahiro Kuragano
Kiyotaka Tokuraku
Koji Uwai
author_sort Sharmin Akter
collection DOAJ
description Alzheimer′s disease (AD) is a chronic neurodegenerative disorder that leads to memory loss and changes in mental and behavioral functions in elderly individuals. A major pathological feature of AD is the aggregation of amyloid-beta (Aβ) peptides, along with oxidative stress, inducing neurocellular apoptosis in the brain. Gobaishi (<i>Galla chinensis</i>), a traditional herbal medicine, has gained considerable attention for its constituents and potent therapeutic properties, particularly its strong inhibitory activity against Aβ fibril formation. In this study, we investigated the anti-Aβ aggregation effects of Gobaishi and its active constituents. We isolated two compounds by employing Thioflavin T (ThT) assay-guided fractionation, which were identified through various spectroscopic methods as pentagalloyl glucose (PGG) and methyl gallate (MG). Evaluation of their anti-Aβ aggregation effects revealed that PGG and MG contribute 1.5% and 0.7% of the activity of Gobaishi, respectively. In addition, PGG demonstrated significantly stronger DPPH radical scavenging activity (EC<sub>50</sub> = 1.16 µM) compared to MG (EC<sub>50</sub> = 6.44 µM). At a concentration of 30 µM, PGG significantly reduced the Aβ-induced cytotoxicity in SH-SY5Y cell lines compared to MG. Based on these findings, both Gobaishi and its active compound PGG are proposed as promising candidates for further investigation as potent anti-amyloidogenic agents in AD management.
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spelling doaj-art-319f5c60fda449149430ccab9b3cfbfc2025-08-20T02:36:32ZengMDPI AGMolecules1420-30492025-06-013013272010.3390/molecules30132720Anti-Amyloid Aggregation Effects of Gobaishi (<i>Galla chinensis</i>) and Its Active ConstituentsSharmin Akter0Takayuki Tohge1Sahithya Hulimane Ananda2Masahiro Kuragano3Kiyotaka Tokuraku4Koji Uwai5Laboratory of Organic Chemistry in Life Science, Muroran Institute of Technology, Muroran 050-8585, JapanLaboratory of Plant Secondary Metabolism, Nara Institute of Science and Technology, Nara 630-0192, JapanLaboratory of Protein Chemistry, Muroran Institute of Technology, Muroran 050-8585, JapanLaboratory of Protein Chemistry, Muroran Institute of Technology, Muroran 050-8585, JapanLaboratory of Protein Chemistry, Muroran Institute of Technology, Muroran 050-8585, JapanLaboratory of Organic Chemistry in Life Science, Muroran Institute of Technology, Muroran 050-8585, JapanAlzheimer′s disease (AD) is a chronic neurodegenerative disorder that leads to memory loss and changes in mental and behavioral functions in elderly individuals. A major pathological feature of AD is the aggregation of amyloid-beta (Aβ) peptides, along with oxidative stress, inducing neurocellular apoptosis in the brain. Gobaishi (<i>Galla chinensis</i>), a traditional herbal medicine, has gained considerable attention for its constituents and potent therapeutic properties, particularly its strong inhibitory activity against Aβ fibril formation. In this study, we investigated the anti-Aβ aggregation effects of Gobaishi and its active constituents. We isolated two compounds by employing Thioflavin T (ThT) assay-guided fractionation, which were identified through various spectroscopic methods as pentagalloyl glucose (PGG) and methyl gallate (MG). Evaluation of their anti-Aβ aggregation effects revealed that PGG and MG contribute 1.5% and 0.7% of the activity of Gobaishi, respectively. In addition, PGG demonstrated significantly stronger DPPH radical scavenging activity (EC<sub>50</sub> = 1.16 µM) compared to MG (EC<sub>50</sub> = 6.44 µM). At a concentration of 30 µM, PGG significantly reduced the Aβ-induced cytotoxicity in SH-SY5Y cell lines compared to MG. Based on these findings, both Gobaishi and its active compound PGG are proposed as promising candidates for further investigation as potent anti-amyloidogenic agents in AD management.https://www.mdpi.com/1420-3049/30/13/2720Gobaishipentagalloyl glucosemethyl gallateamyloid-betaantioxidant
spellingShingle Sharmin Akter
Takayuki Tohge
Sahithya Hulimane Ananda
Masahiro Kuragano
Kiyotaka Tokuraku
Koji Uwai
Anti-Amyloid Aggregation Effects of Gobaishi (<i>Galla chinensis</i>) and Its Active Constituents
Molecules
Gobaishi
pentagalloyl glucose
methyl gallate
amyloid-beta
antioxidant
title Anti-Amyloid Aggregation Effects of Gobaishi (<i>Galla chinensis</i>) and Its Active Constituents
title_full Anti-Amyloid Aggregation Effects of Gobaishi (<i>Galla chinensis</i>) and Its Active Constituents
title_fullStr Anti-Amyloid Aggregation Effects of Gobaishi (<i>Galla chinensis</i>) and Its Active Constituents
title_full_unstemmed Anti-Amyloid Aggregation Effects of Gobaishi (<i>Galla chinensis</i>) and Its Active Constituents
title_short Anti-Amyloid Aggregation Effects of Gobaishi (<i>Galla chinensis</i>) and Its Active Constituents
title_sort anti amyloid aggregation effects of gobaishi i galla chinensis i and its active constituents
topic Gobaishi
pentagalloyl glucose
methyl gallate
amyloid-beta
antioxidant
url https://www.mdpi.com/1420-3049/30/13/2720
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