Flavonoids isolated from Tibetan medicines, binding to GABA(A) receptor and the anticonvulsant activity
文献类型：期刊论文
| 作者 | Liu, Zenggen ; Lindemeyer, A. Kerstin; Liang, Jing; Wanner, Martin; Shao, Xuesi M.; Shao, Yun; Tao, Yanduo; Olsen, Richard W.
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| 刊名 | PHYTOMEDICINE
 |
| 出版日期 | 2018 |
| 卷号 | 50 |
| 关键词 | Flavonoids Tibetan herbs GABA(A) receptor Structure-activity relationships Seizures |
| 英文摘要 | Background: : Our previous studies on Asterothamnus centrali-asiaticus Novopokr. (ACN) and Arenaria kansuensis Maxim. (AKM) had led to the isolation of some phytochemical constituents and evaluation of anticonvulsant effect based on their extracts. ACN and AKM have been widely used in traditional Tibetan herbs for neuropsychiatric diseases and cardiopulmonary disorders. Purpose: : The purpose is to investigate structure-activity relationships of flavonoids isolated from ACN and AKM, for binding to the benzodiazepine site (BZ-S) of gamma-aminobutyric acid type A (GABA(A)) receptor complex, and to search for anticonvulsant compounds without undesirable effects such as myorelaxation and sedation. Study design and methods: : The affinities of these flavonoids for the BZ-S of GABA(A) receptors were determined by [H-3]flunitrazepam binding to mouse cerebellum membranes in vitro. And the anticonvulsant, myorelaxant and sedative effects were determined by pentylenetetrazol (PTZ)-induced seizure and electrogenic seizure protection, rotarod test and locomotor activity test, respectively. Results: : Fifteen and thirteen flavonoids were isolated from ACN and AKM, respectively. Structure-activity relationships analysis indicated that 6-and/or 8-OMe flavones exhibited the most potent binding affinity to GABA(A) receptors. Furthermore, 2',4',5,7-tetrahydroxy-5',6-dimethoxyflavone (DMF, IC50 value of 0.10 mu M), a flavone isolated from ACN, presented high anticonvulsant activity against chemical-induced seizures and electrogenic seizures, without myorelaxation and sedation. Conclusion: : This study suggested that these flavones, especially DMF, are new BZ receptor ligands and prospective therapeutic candidates for seizures. |
| 源URL | [http://210.75.249.4/handle/363003/59938]  |
| 专题 | 西北高原生物研究所_中国科学院西北高原生物研究所 |
| 推荐引用方式 GB/T 7714 | Liu, Zenggen,Lindemeyer, A. Kerstin,Liang, Jing,et al. Flavonoids isolated from Tibetan medicines, binding to GABA(A) receptor and the anticonvulsant activity[J]. PHYTOMEDICINE,2018,50. |
| APA | Liu, Zenggen.,Lindemeyer, A. Kerstin.,Liang, Jing.,Wanner, Martin.,Shao, Xuesi M..,...&Olsen, Richard W..(2018).Flavonoids isolated from Tibetan medicines, binding to GABA(A) receptor and the anticonvulsant activity.PHYTOMEDICINE,50. |
| MLA | Liu, Zenggen,et al."Flavonoids isolated from Tibetan medicines, binding to GABA(A) receptor and the anticonvulsant activity".PHYTOMEDICINE 50(2018). |
入库方式： OAI收割
来源：西北高原生物研究所
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