Anti-Inflammatory and Tau Phosphorylation–Inhibitory Effects of Eupatin
1
School of Pharmacy, College of Medicine, National Taiwan University, Taipei 10050, Taiwan
2
Graduate Institute of Cancer Biology and Drug Discovery, College of Medical Science and Technology, Taipei Medical University, Taipei 11031, Taiwan
3
Ph.D. Program for Cancer Molecular Biology and Drug Discovery, College of Medical Science and Technology, Taipei Medical University, Taipei 11031, Taiwan
4
Ph.D. Program in Biotechnology Research and Development, College of Pharmacy, Taipei Medical University, Taipei 11031, Taiwan
5
Biomedical Commercialization Center, Taipei Medical University, Taipei 11031, Taiwan
6
Master Program in Graduate Institute of Cancer Biology and Drug Discovery, College of Medical Science and Technology, Taipei Medical University, Taipei 11031, Taiwan
*
Author to whom correspondence should be addressed.
†
These authors contributed equally to this work.
Molecules 2020, 25(23), 5652; https://doi.org/10.3390/molecules25235652
Received: 9 November 2020
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Revised: 26 November 2020
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Accepted: 28 November 2020
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Published: 30 November 2020
(This article belongs to the Section Natural Products Chemistry)
Alzheimer’s disease (AD), which is among the most prevalent neurodegenerative diseases, manifests as increasing memory loss and cognitive decline. Tau phosphorylation and aggregation are strongly linked to neurodegeneration, as well as associated with chronic neuroinflammatory processes. The anti-inflammation effects of natural products have led to wide recognition of their potential for use in treating and preventing AD. This study investigated whether eupatin, a polymethoxyflavonoid found in Artemisia species, has inhibitory effects on neuroinflammation and tau phosphorylation. We treated mouse macrophages and microglia cells with lipopolysaccharides (LPSs) to activate inflammatory signals, and we treated neuronal cells with a protein phosphatase 2A inhibitor, okadaic acid (OA), or transfection with pRK5-EGFP-Tau P301L plasmid to induce tau phosphorylation. The results indicated that eupatin significantly reduced the LPS-induced protein expression and phosphorylation of p65 and inducible nitric oxide synthase as well as downstream products interleukin 6 and nitrite, respectively. Furthermore, eupatin markedly inhibited the expression of phospho-tau in response to OA treatment and plasmid transfection. We discovered that this inhibition was achieved through the inhibition of glycogen synthase kinase 3β (GSK3β), and molecular docking results suggested that eupatin can sufficiently bind to the GSK3β active site. Our results demonstrate that eupatin has neuroprotective effects, making it suitable for AD treatment.
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MDPI and ACS Style
Chou, C.-H.; Hsu, K.-C.; Lin, T.E.; Yang, C.-R. Anti-Inflammatory and Tau Phosphorylation–Inhibitory Effects of Eupatin. Molecules 2020, 25, 5652. https://doi.org/10.3390/molecules25235652
AMA Style
Chou C-H, Hsu K-C, Lin TE, Yang C-R. Anti-Inflammatory and Tau Phosphorylation–Inhibitory Effects of Eupatin. Molecules. 2020; 25(23):5652. https://doi.org/10.3390/molecules25235652
Chicago/Turabian StyleChou, Ching-Hsuan, Kai-Cheng Hsu, Tony E. Lin, and Chia-Ron Yang. 2020. "Anti-Inflammatory and Tau Phosphorylation–Inhibitory Effects of Eupatin" Molecules 25, no. 23: 5652. https://doi.org/10.3390/molecules25235652
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