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Natural Products with Anti-neuroinflammatory Activity

A special issue of International Journal of Molecular Sciences (ISSN 1422-0067). This special issue belongs to the section "Bioactives and Nutraceuticals".

Deadline for manuscript submissions: closed (30 December 2024) | Viewed by 593

Special Issue Editor


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Guest Editor
Shaanxi Key Laboratory of Natural Products & Chemical Biology, College of Chemistry and Pharmacy, Northwest A&F University, Yangling 712100, China
Interests: natural products; biological activity; structure determination; structure-activity relationships; mechanism of action; chemical synthesis of natural products

Special Issue Information

Dear Colleagues,

Chronic, excessive neuroinflammation is a key feature of neurodegenerative diseases including Alzheimer’s disease (AD) and Parkinson’s disease (PD). Microglia are the resident immune cells of the central nervous system (CNS) and subserve numerous supportive functions, contributing to diverse processes such as neurodevelopment, synaptic maintenance and remodeling, synaptic plasticity, and promotion of myelination. As an important component of microglial cells, the inflammasomes play an important role in the immune response and disease development. After exposure to certain exogenous stimuli, for example, lipopolysaccharide (LPS), the inflammatory stimulus activates the pyrin domain-containing protein 3 (NLRP3) inflammasome and the formation of the multi-protein inflammasome complex. The inflammasome complex contributes to the auto-catalysis of pro-caspase 1, generating the components of mature caspase-1. Active caspase-1 then processes the release of the pro-inflammatory cytokines IL-1β and IL-18, leading to pro-inflammatory demise of microglia. Natural products from plants and microorganisms have now become promising candidates as therapeutic agents because of their anti-inflammatory properties. Phytochemicals including flavonoids, terpenoids, alkaloids, and lignans have generated interest as inflammasome inhibitor candidates for relevant inflammatory diseases within the nervous system. Considering their natural scarcity, chemical synthesis will be highly desirable to facilitate in-depth biological mechanism research. The discovery of small-molecular inhibitors targeting NLRP3 inflammasome is an attractive therapeutic strategy for the treatment of neurodegenerative diseases.

Prof. Dr. Jin-Ming Gao
Guest Editor

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Keywords

  • natural product chemistry
  • natural product synthesis
  • neurodegenerative diseases
  • anti-neuroinflammatory
  • molecular mechanism
  • biological probes
  • targeting inflammasomes
  • NLRP3

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Published Papers (1 paper)

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Research

19 pages, 7441 KiB  
Article
Neuroprotective Effect of Nor-Prenylated Acylphloroglucinols from Hypericum perforatum L. (St John’s Wort) in the MPTP-Induced Zebrafish Model
by Wuyang Liu, Peng Zhao, Yihan Liu, Xiangyan Meng, Jinyan Xie, Junmian Tian and Jinming Gao
Int. J. Mol. Sci. 2025, 26(7), 3096; https://doi.org/10.3390/ijms26073096 - 27 Mar 2025
Viewed by 326
Abstract
Hypericum perforatum L. (St John’s wort) has been widely studied and used for antidepressant treatment, as well as, rarely, featuring in studies on its chemical composition for Parkinson’s disease (PD) treatment. Five new nor-prenylated acylphloroglucinols with a cyclohexanone core, norperforatums A–E ( [...] Read more.
Hypericum perforatum L. (St John’s wort) has been widely studied and used for antidepressant treatment, as well as, rarely, featuring in studies on its chemical composition for Parkinson’s disease (PD) treatment. Five new nor-prenylated acylphloroglucinols with a cyclohexanone core, norperforatums A–E (15), together with four known analogs [(2R,3R,4S,6R)-3-methyl-4,6-di(3-methyl-2-butenyl)-2-(2-methyl-1-oxopropyl)-3-(4-methyl-3-pentenyl)cyclohexanone (6), hyperscabrin B (7), (2R,3R,4S,6R)-6-methoxycarbonyl-3-methyl-4,6-di(3-methyl-2-butenyl)-2-(2-methyl-1-oxopropyl)-3-(4-methyl-3-pentenyl)cyclohexanone (8), and hyperscabin K (9)], were isolated from the aerial parts of H. perforatum. The structures and absolute configurations of the new compounds were characterized by multiple spectroscopic means, including nuclear magnetic resonance (NMR), high-resolution electrospray ionization mass spectrometry (HR-ESI-MS), ultraviolet visible absorption spectroscopy (UV), infrared spectroscopy (IR), calculated electronic circular dichroism (ECD) data, and X-ray signal crystal diffraction. In addition, the efficacy of these isolations was evaluated against 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP)-induced PD in zebrafish larvae. Compound 9 had the best therapeutic effect, by significantly increasing the total distance traveled and the mean speed of movement in PD dyskinesia zebrafish larvae. Moreover, it enhanced superoxide dismutase (SOD) activity and inhibited reactive oxygen species (ROS) production in a dose-dependent manner. These results suggest that compound 9 may have ameliorative effects on PD symptoms by inhibiting oxidative stress. This study provides new insights into the treatment of H. perforatum for PD. Full article
(This article belongs to the Special Issue Natural Products with Anti-neuroinflammatory Activity)
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