Literature DB >> 28810246

GPER Agonist G1 Attenuates Neuroinflammation and Dopaminergic Neurodegeneration in Parkinson Disease.

Jing Guan1, Beibei Yang, Yi Fan, Ji Zhang.   

Abstract

OBJECTIVE: Epidemiological studies have shown that women of reproductive age have much less possibility of developing Parkinson disease (PD) than men. The beneficial effect of estrogen also has been well-described in both culture and animal models of PD. G protein-coupled estrogen receptor (GPER) is a membrane-associated estrogen receptor, and displayed a neuroprotective role in a mouse model of PD. Since GPER is highly expressed in microglia, we speculate that GPER mediates the neuroprotective function of estradiol through suppressing the neuroinflammation of PD.
METHODS: We investigated the effects of GPER agonist G1 and GPER antagonist G15 on the neurodegeneration of dopaminergic neuron, the activation of microglia, and the production of IL-1β, TNF-α, and IL-6 in 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP)-induced animal model of parkinsonism. Furthermore, we confirmed the effects of GPER activation on the production of IL-1β, TNF-α, and IL-6 in an in vitro MPP+ model in BV2 microglial cells.
RESULTS: After 12-day treatment with G1, mice showed an increase in the number of tyrosine hydroxylase-immunoreactive cells, reduced activation of microglia, and the abatement of proinflammatory cytokines, and the anti-inflammatory effect of G1 was abolished by G15. Meanwhile, in vitro studies demonstrated that GPER activation also reduced the release of proinflammatory cytokines from BV2 microglial cells after MPP+ stimulation.
CONCLUSION: Our data suggest that GPER mediates the anti-neuroinflammatory effect of estrogen in experimental PD progression.
© 2017 S. Karger AG, Basel.

Entities:  

Keywords:  G protein-coupled estrogen receptor; Neuroinflammation; Parkinson disease

Mesh:

Substances:

Year:  2017        PMID: 28810246     DOI: 10.1159/000478908

Source DB:  PubMed          Journal:  Neuroimmunomodulation        ISSN: 1021-7401            Impact factor:   2.492


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