美金刚
NMDA受体
兴奋毒性
化学
血脑屏障
谷氨酸受体
生物物理学
受体
药理学
生物化学
神经科学
生物
中枢神经系统
作者
I. Jénnifer Gómez,Petra Křížková,Anna Dolečková,Lucía Cardo,Cecilia Wetzl,Naděžda Pizúrová,Maurizio Prato,Jiřina Procházková,Lenka Zajı́čková
标识
DOI:10.1016/j.apmt.2024.102072
摘要
Multifunctional nanoparticles could be the hallmark for the treatment of neurodegenerative diseases. Dissociation of protein aggregates causing neuronal damage and transfer of specific drugs which can downregulate neuronal excitotoxicity by inhibiting glutamatergic N-Methyl-d-Aspartate-receptors (NMDA) and then reducing calcium influx are among the main factors to consider for proper therapy. Here, we present a multiplatform based on nitrogen-doped graphene quantum dots (NGQDs) with such functionalities. The NGQDs were functionalized with Memantine, the clinically used drug, via covalent and non-covalent coupling, and we confirmed that the pharmaceutical activity was not altered. Apart from that, using xCELLigence technology and flow cytometric analysis of ABC transporter function, we uncovered that the ABC transporters of the blood-brain barrier (BBB) do not affect the ability of NGQD to cross BBB. Surprisingly, this study found that NGQDs have an inhibitory effect on NMDA receptors, thus supporting the action of Memantine. Moreover, NGQDs and their derivatives demonstrated the potential to dissociate β-amyloid aggregates while possessing features suitable for bioimaging in various cell lines.
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