基于 HPLC 的苦参（苦参根）中 GABA A 受体调节剂的活性分析。
HPLC-based activity profiling for GABAA receptor modulators from the traditional Chinese herbal drug Kushen (Sophora flavescens root).
机构信息
Institute of Pharmaceutical Biology, University of Basel, Klingelbergstrasse 50, 4056, Basel, Switzerland.
出版信息
Mol Divers. 2011 May;15(2):361-72. doi: 10.1007/s11030-010-9297-7. Epub 2011 Jan 5.
Abstract
An EtOAc extract from the roots of Sophora flavescens (Kushen) potentiated γ-aminobutyric acid (GABA)-induced chloride influx in Xenopus oocytes transiently expressing GABA(A) receptors with subunit composition, α (1) β (2) γ (2S). HPLC-based activity profiling of the extract led to the identification of 8-lavandulyl flavonoids, kushenol I, sophoraflavanone G, (-)-kurarinone, and kuraridine as GABA(A) receptor modulators. In addition, a series of inactive structurally related flavonoids were characterized. Among these, kushenol Y (4) was identified as a new natural product. The 8-lavandulyl flavonoids are first representatives of a novel scaffold for the target.
摘要
苦参根的 EtOAc 提取物增强了在表达 GABA(A) 受体亚基组成α(1)β(2)γ(2S)的非洲爪蟾卵母细胞中γ-氨基丁酸（GABA）诱导的氯离子内流。基于 HPLC 的提取物活性分析导致鉴定出 8-薰衣草基黄酮、苦参醇 I、槐属黄酮 G、(-)-苦参酮和苦参啶作为 GABA(A)受体调节剂。此外，还表征了一系列结构上无活性的相关黄酮类化合物。其中，苦参醇 Y(4)被鉴定为一种新的天然产物。8-薰衣草基黄酮是该靶标的新型支架的首批代表。
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