Anti-Amyloid Aggregation Effects of Gobaishi () 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 apoptosis in the brain. Gobaishi (), 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 = 1.16 µM) compared to MG (EC = 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.