BMC Neurosci
2010 Mar 3:11:31.
doi: 10.1186/1471-2202-11-31.
Neuroprotective effects of bis(7)-tacrine against glutamate-induced retinal ganglion cells damage
Jia Hua Fang 1, Xing Hua Wang, Zhi Rong Xu, Fa Gang Jiang
Affiliations expand
PMID: 20199668
PMCID: PMC2838896
DOI: 10.1186/1471-2202-11-31
Abstract
Background: Glutamate-mediated excitotoxicity, primarily through N-methyl-D-aspartate (NMDA) receptors, may be an important cause of retinal ganglion cells (RGCs) death in glaucoma and several other retinal diseases. Bis(7)-tacrine is a noncompetitive NMDA receptors antagonist that can prevent glutamate-induced hippocampal neurons damage. We tested the effects of bis(7)-tacrine against glutamate-induced rat RGCs damage in vitro and in vivo.
Results: In cultured neonatal rats RGCs, the MTT assay showed that glutamate induced a concentration- and time-dependent toxicity. Bis(7)-tacrine and memantine prevented glutamate-induced cell death in a concentration-dependent manner with IC50 values of 0.028 microM and 0.834 microM, respectively. The anti-apoptosis effects of bis(7)-tacrine were confirmed by annexin V-FITC/PI staining. In vivo, TUNEL analysis and retrograde labeling analysis found that pretreatment with bis(7)-tacrine(0.2 mg/kg) induced a significant neuroprotective effect against glutamate-induced RGCs damage.
Conclusions: Our results showed that bis(7)-tacrine had neuroprotective effects against glutamate-induced RGCs damage in vitro and in vivo, possibly through the drug's anti-NMDA receptor effects. These findings make bis(7)-tacrine potentially useful for treating a variety of ischemic or traumatic retinopathies inclusive of glaucoma.
参考连接：
https://pubpeer.com/publications/293001314558A00CE5435188E76148
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