1. Neferine, a bisbenzylisoquinoline alkaloid of Nelumbo nucifera, inhibits glutamate release in rat cerebrocortical nerve terminals through 5-HT
- Author
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Kun Chieh, Yeh, Chi Feng, Hung, Ya Fan, Lin, Der Chen, Chang, Ming Shang, Pai, and Su Jane, Wang
- Subjects
Cerebral Cortex ,Male ,Nerve Endings ,Dose-Response Relationship, Drug ,Glutamic Acid ,Nelumbo ,Benzylisoquinolines ,Protein Structure, Secondary ,Rats ,Molecular Docking Simulation ,Rats, Sprague-Dawley ,Alkaloids ,Receptor, Serotonin, 5-HT1A ,Animals ,Excitatory Amino Acid Antagonists ,Drugs, Chinese Herbal - Abstract
Neferine, a bisbenzylisoquinoline alkaloid present in Nelumbo nucifera, has been reported to exhibit neuroprotective effects. Because reduced glutamatergic transmission through inhibition of glutamate release has been proposed as a mechanism of neuroprotection, we investigated whether and how neferine inhibits glutamate release in the nerve terminals of the cerebral cortex of rats. The results demonstrated that neferine inhibits the glutamate release that is evoked by the potassium channel blocker 4-aminopyridine, doing so in a dose-dependent manner. This effect was prevented by removing extracellular calcium and blocking vesicular transporters or N- and P/Q-type calcium channels but not by blocking glutamate transporters. Neferine decreased the 4-aminopyridine-stimulated elevation in intrasynaptosomal calcium concentration; however, it had no effect on the synaptosomal membrane potential. The inhibition of glutamate release by neferine was also eliminated by the selective 5-hydroxytryptamine 1A (5HT
- Published
- 2020