Flavonoid Myricetin Modulates GABAA Receptor Activity through Activation of Ca2+ Channels and CaMK-II Pathway
Joint Authors
Zhang, Xiao Hu
Ma, Ze Gang
Rowlands, Dewi Kenneth
Gou, Yu Lin
Fok, Kin Lam
Wong, Hau Yan
Yu, Mei Kuen
Tsang, Lai Ling
Mu, Li
Chen, Lei
Yung, Wing Ho
Chung, Yiu Wa
Zhang, Bei Lin
Zhao, Hua
Chan, Hsiao Chang
Source
Evidence-Based Complementary and Alternative Medicine
Issue
Vol. 2012, Issue 2012 (31 Dec. 2012), pp.1-10, 10 p.
Publisher
Hindawi Publishing Corporation
Publication Date
2012-11-11
Country of Publication
Egypt
No. of Pages
10
Main Subjects
Abstract EN
The flavonoid myricetin is found in several sedative herbs, for example, the St.
John's Wort, but its influence on sedation and its possible mechanism of action are unknown.
Using patch-clamp technique on a brain slice preparation, the present study found that myricetin promoted GABAergic activity in the neurons of hypothalamic paraventricular nucleus (PVN) by increasing the decay time and frequency of the inhibitory currents mediated by GABAA receptor.
This effect of myricetin was not blocked by the GABAA receptor benzodiazepine- (BZ-) binding site antagonist flumazenil, but by KN-62, a specific inhibitor of the Ca2+/calmodulin-stimulated protein kinase II (CaMK-II).
Patch clamp and live Ca2+ imaging studies found that myricetin could increase Ca2+ current and intracellular Ca2+ concentration, respectively, via T- and L-type Ca2+ channels in rat PVN neurons and hypothalamic primary culture neurons.
Immunofluorescence staining showed increased phosphorylation of CaMK-II after myricetin incubation in primary culture of rat hypothalamic neurons, and the myricetin-induced CaMK-II phosphorylation was further confirmed by Western blotting in PC-12 cells.
The present results suggest that myricetin enhances GABAA receptor activity via calcium channel/CaMK-II dependent mechanism, which is distinctively different from that of most existing BZ-binding site agonists of GABAA receptor.
American Psychological Association (APA)
Zhang, Xiao Hu& Ma, Ze Gang& Rowlands, Dewi Kenneth& Gou, Yu Lin& Fok, Kin Lam& Wong, Hau Yan…[et al.]. 2012. Flavonoid Myricetin Modulates GABAA Receptor Activity through Activation of Ca2+ Channels and CaMK-II Pathway. Evidence-Based Complementary and Alternative Medicine،Vol. 2012, no. 2012, pp.1-10.
https://search.emarefa.net/detail/BIM-992621
Modern Language Association (MLA)
Zhang, Xiao Hu…[et al.]. Flavonoid Myricetin Modulates GABAA Receptor Activity through Activation of Ca2+ Channels and CaMK-II Pathway. Evidence-Based Complementary and Alternative Medicine No. 2012 (2012), pp.1-10.
https://search.emarefa.net/detail/BIM-992621
American Medical Association (AMA)
Zhang, Xiao Hu& Ma, Ze Gang& Rowlands, Dewi Kenneth& Gou, Yu Lin& Fok, Kin Lam& Wong, Hau Yan…[et al.]. Flavonoid Myricetin Modulates GABAA Receptor Activity through Activation of Ca2+ Channels and CaMK-II Pathway. Evidence-Based Complementary and Alternative Medicine. 2012. Vol. 2012, no. 2012, pp.1-10.
https://search.emarefa.net/detail/BIM-992621
Data Type
Journal Articles
Language
English
Notes
Includes bibliographical references
Record ID
BIM-992621