title: Baicalein, a Constituent of Scutellaria baicalensis, Reduces Glutamate Release and Protects Neuronal Cell Against Kainic Acid-Induced Excitotoxicity in Rats.
abstract: Interest in the health benefits of flavonoids, particularly their effects on neurodegenerative disease, is increasing. This study evaluated the role of baicalein, a flavonoid compound isolated from the traditional Chinese medicine Scutellaria baicalensis, in glutamate release and glutamate neurotoxicity in the rat hippocampus. In the rat hippocampal nerve terminals (synaptosomes), baicalein inhibits depolarization-induced glutamate release, and this phenomenon is prevented by chelating the extracellular Ca[Formula: see text] ions and blocking presynaptic Cav2.2 (N-type) and Cav2.1 (P/Q-type) channel activity. In slice preparations, whole cell patch-clamp experiments revealed that baicalein reduced the frequency of miniature excitatory postsynaptic currents, without affecting their amplitude. In a kainic acid rat model, intraperitoneally administering baicalein to rats before the kainic acid intraperitoneal injection substantially attenuated kainic acid-induced neuronal cell death, c-Fos expression, and the activation of the mammalian target of rapamycin in the hippocampus. This study is the first to demonstrate that the natural compound baicalein inhibits glutamate release from hippocampal nerve terminals, and executes a protective action against kainic acid-induced excitotoxicity in vivo. The findings enhance the understanding of baicalein's action in the brain, and suggest that this natural compound is valuable for treating brain disorders related to glutamate excitotoxicity.
authors.affiliation: * School of Medicine, Fu Jen Catholic University, New Taipei City 24205, Taiwan.|† Department of Anesthesiology, Shin Kong Wu Ho-Su Memorial Hospital, Taipei 111, Taiwan.
authors.forename: Yi
authors.initials: Y
authors.lastname: Chang
authors.affiliation: ‡ Department of Anesthesiology, Far-Eastern Memorial Hospital, New Taipei City 22060, Taiwan.|§ Department of Mechanical Engineering, Yuan Ze University, Taoyuan 320, Taiwan.
authors.forename: Cheng Wei
authors.initials: CW
authors.lastname: Lu
authors.affiliation: ‡ Department of Anesthesiology, Far-Eastern Memorial Hospital, New Taipei City 22060, Taiwan.|§ Department of Mechanical Engineering, Yuan Ze University, Taoyuan 320, Taiwan.
authors.forename: Tzu Yu
authors.initials: TY
authors.lastname: Lin
authors.affiliation: ‡ Department of Anesthesiology, Far-Eastern Memorial Hospital, New Taipei City 22060, Taiwan.
authors.forename: Shu Kuei
authors.initials: SK
authors.lastname: Huang
authors.affiliation: * School of Medicine, Fu Jen Catholic University, New Taipei City 24205, Taiwan.
authors.forename: Su Jane
authors.initials: SJ
authors.lastname: Wang
mesh_terms: D000818:Animals; D001921:Brain / Q000166:cytology / Q000187:drug effects / Q000502:physiology; D001927:Brain Diseases / Q000188:drug therapy* / Q000235:genetics / Q000378:metabolism / Q000503:physiopathology*; D002118:Calcium / Q000378:metabolism; D020864:Calcium Channels, N-Type / Q000235:genetics / Q000378:metabolism; D019706:Excitatory Postsynaptic Potentials / Q000187:drug effects; D044950:Flavanones / Q000008:administration & dosage*; D018698:Glutamic Acid / Q000378:metabolism / Q000633:toxicity*; D006801:Humans; D007608:Kainic Acid / Q000009:adverse effects; D008297:Male; D009474:Neurons / Q000187:drug effects* / Q000378:metabolism; D010936:Plant Extracts / Q000008:administration & dosage*; D020011:Protective Agents / Q000008:administration & dosage*; D051381:Rats; D017207:Rats, Sprague-Dawley; D031364:Scutellaria baicalensis / Q000378:metabolism
chemical_list: D002118:Calcium; D020864:Calcium Channels, N-Type; D044950:Flavanones; D018698:Glutamic Acid; D007608:Kainic Acid; D010936:Plant Extracts; D020011:Protective Agents; C499814:Scutellaria baicalensis extract; C006680:baicalein
keywords: Baicalein; Excitotoxicity; Glutamate Release; Hippocampus; Kainic Acid; Neuroprotection