Quercetin Reduces Cortical GABAergic Transmission and Alleviates MK-801-Induced Hyperactivity
文献类型：期刊论文
| 作者 | Fan, Hui-Ran1,2,3; Du, Wei-Feng2; Zhu, Tao2; Wu, Yan-Jiao1; Liu, Yan-Mei4; Wang, Qi1; Wang, Qin1; Gu, Xue1; Shan, Xingyue4; Deng, Shining4 |
| 刊名 | EBioMedicine
 |
| 出版日期 | 2018-08 |
| 卷号 | 34页码:201-213 |
| ISSN号 | 2352-3964 |
| DOI | 10.1016/j.ebiom.2018.07.031 |
| 文献子类 | Article |
| 英文摘要 | An imbalance between neuronal excitation and inhibition represents a core feature in multiple neuropsychiatry disorders, necessitating the development of novel strategies to calibrate the excitatory-inhibitory balance of therapeutics. Here we identify a natural compound quercetin that reduces prefrontal cortical GABAergic transmission and alleviates the hyperactivity induced by glutamatergic N-methyl-d-aspartate receptor antagonist MK-801. Quercetin markedly reduced the GABA-activated currents in a noncompetitive manner in cultured cortical neurons, and moderately inhibited spontaneous and electrically-evoked GABAergic inhibitory postsynaptic current in mouse prefrontal cortical slices. Notably, systemic and prefrontal-specific delivery of quercetin reduced basal locomotor activity in addition to alleviated the MK-801-induced hyperactivity. The effects of quercetin were not exclusively dependent on α5-subunit-containing A type GABA receptors (GABARs), as viral-mediated, region-specific genetic knockdown of the α5-subunit in prefrontal cortex improved the MK-801-evoked psychotic symptom but reserved the pharmacological responsivity to quercetin. Both interventions together completely normalized the locomotor activity. Together, quercetin as a negative allosteric GABAR modulator exerted antipsychotic activity, facilitating further therapeutic development for the excitatory-inhibitory imbalance disorders. |
| 语种 | 英语 |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/266543]  |
| 专题 | 中国科学院上海药物研究所 |
| 通讯作者 | Li, Wei-Guang; Li, Fei |
| 作者单位 | 1.Collaborative Innovation Center for Brain Science, Department of Anatomy and Physiology, Shanghai Jiao Tong University School of Medicine, Shanghai 200025, China; 2.Department of Chinese Materia Medica, College of Pharmaceutical Science, Zhejiang Chinese Medical University, Hangzhou 310053, China; 3.Developmental and Behavioral Pediatric Department, Ministry of Education-Shanghai Key Laboratory of Children's Environmental Health, Shanghai Institute for Pediatric Research, Xin Hua Hospital Affiliated Shanghai Jiao Tong University School of Medicine, Shanghai 200092, China; 4.Developmental and Behavioral Pediatric Department, Ministry of Education-Shanghai Key Laboratory of Children's Environmental Health, Shanghai Institute for Pediatric Research, Xin Hua Hospital Affiliated Shanghai Jiao Tong University School of Medicine, Shanghai 200092, China |
| 推荐引用方式 GB/T 7714 | Fan, Hui-Ran,Du, Wei-Feng,Zhu, Tao,et al. Quercetin Reduces Cortical GABAergic Transmission and Alleviates MK-801-Induced Hyperactivity[J]. EBioMedicine,2018,34:201-213. |
| APA | Fan, Hui-Ran.,Du, Wei-Feng.,Zhu, Tao.,Wu, Yan-Jiao.,Liu, Yan-Mei.,...&Li, Fei.(2018).Quercetin Reduces Cortical GABAergic Transmission and Alleviates MK-801-Induced Hyperactivity.EBioMedicine,34,201-213. |
| MLA | Fan, Hui-Ran,et al."Quercetin Reduces Cortical GABAergic Transmission and Alleviates MK-801-Induced Hyperactivity".EBioMedicine 34(2018):201-213. |
入库方式： OAI收割
来源：上海药物研究所
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