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Panaxadiol inhibits synaptic dysfunction in Alzheimer's disease and targets the Fyn protein in APP/PS1 mice and APP-SH-SY5Y cells

Bibliographic

Year of Publication:
2019
Contact PI Name:
Jingxian Yang
Contact PI Affiliation:
School of Pharmacy, Liaoning University of Traditional Chinese Medicine, Dalian, China
Co-Authors:
Xicai Liang, Yingjia Yao, Ying Lin, Liang Kong, Honghe Xiao, Yue Shi
Primary Reference (PubMED ID):
Funding Source:
National Natural Science Foundation of China
Study Goal and Principal Findings:

Aim: Alzheimer's disease (AD), a neurodegenerative disease, is characterized by memory loss and synaptic damage. Up to now, there are limited drugs to cure or delay the state of this illness. Recently, the Fyn tyrosine kinase is implicated in AD pathology triggered by synaptic damage. Thus, Fyn inhibition may prevent or delay the AD progression. Therefore, in this paper, we investigated whether Panaxadiol could decrease synaptic damage in AD and the underlying mechanism.

Main Methods: The ability of learning and memory of mice has detected by Morris Water Maze. The pathological changes detected by H&E staining and Nissl staining. The percentage of cell apoptosis and the calcium concentration were detected by Flow Cytometry in vitro. The amount of synaptic protein and related proteins in the Fyn/GluN2B/CaMKIIα signaling pathway were detected by Western Blot.

Key Findings: In the present article, Panaxadiol could significantly improve the ability of learning and memory of mice and reduce its synaptic dysfunction. Panaxadiol could down-regulate GluN2B's phosphorylation level by inhibition Fyn kinase activity, Subsequently, decrease Ca2+-mediated synaptic damage, reducing LDH leakage, inhibiting apoptosis in AD, resulting in facilitating the cells survival. For the underlying molecular mechanism, we used PP2 to block the Fyn/GluN2B/CaMKIIα signaling pathway. The results from WB showed that the expression of related proteins in the Fyn signaling pathway decreased with PP2 treated.

Significance: Our results indicate that Panaxadiol could decrease synaptic damage, which will cause AD via inhibition of the Fyn/GluN2B/CaMKIIα signaling pathway. Thus, the Panaxadiol is a best promising candidate to test as a potential therapy for AD.

Therapeutic Agent

Therapeutic Information:
Therapy Type:
Small Molecule
Therapeutic Agent:
Panaxadiol
Therapeutic Target:
Tyrosine Protein Kinase FYN
Therapy Type:
Small Molecule
Therapeutic Agent:
PP2
Therapeutic Target:
Multi Target

Animal Model

Model Information:
Species:
Mouse
Model Type:
APPxPS1
Strain/Genetic Background:
C57BL/6
Animal Model Notes:
The authors do not specify which APP/PS1 model is used in this study.

Experimental Design

Is the following information reported in the study?:
Power/Sample Size Calculation
Randomized into Groups
Blinded for Treatment
Blinded for Outcome Measures
Pharmacokinetic Measures
Pharmacodynamic Measures
Toxicology Measures
ADME Measures
Biomarkers
Dose
Formulation
Route of Delivery
Duration of Treatment
Frequency of Administration
Age of Animal at the Beginning of Treatment
Age of Animal at the End of Treatment
Sex as a Biological Variable
Study Balanced for Sex as a Biological Variable
Number of Premature Deaths
Number of Excluded Animals
Statistical Plan
Genetic Background
Inclusion/Exclusion Criteria Included
Conflict of Interest

Outcomes

Outcome Measured
Outcome Parameters
Behavioral
Morris Water Maze
Histopathology
Neuronal Loss
Neurodegeneration
Biochemical
Synaptophysin
Tyrosine Protein Kinase FYN
Glutamate Ionotropic Receptor NMDA Type Subunit 2B (GluN2B/NR2B)
phospho-Glutamate Ionotropic Receptor NMDA Type Subunit 2B (phospho-GluN2B/NR2B)
Calcium Calmodulin Kinase II (CAMKII)
phospho-Tyrosine Protein Kinase FYN (phospho-FYN)
Amyloid Precursor Protein (APP)
Lactate Dehydrogenase (LDH)
Intracellular Calcium Concentration
Immunochemistry
Green Fluorescent Protein (GFP)
Cell Biology
Cell Viability
Flow Cytometry
Apoptosis