Department of Pharmaceutical Sciences, University of Basel, Basel, Switzerland.
Planta Med. 2012 Mar;78(5):440-7. doi: 10.1055/s-0031-1298229. Epub 2012 Jan 31.
EtOAc extracts from two batches of Morus alba root bark (Sang bai pi) potentiated γ-aminobutyric acid (GABA)-induced chloride influx in Xenopus oocytes, which transiently expressed GABA (A) receptors of the subunit composition α₁β₂γ(2S). With the aid of HPLC-based activity profiling of the extract from the first batch, activity was traced to a peak subsequently identified as sanggenon G (3). The second batch had a different phytochemical profile, and HPLC-based activity profiling led to the identification of sanggenon C (4) and a stereoisomer of sanggenon D (2) as positive GABA (A) receptor modulators. The structurally related compound kuwanon L (1) was inactive. The sanggenons represent a new scaffold of positive GABA (A) receptor modulators.
从两批桑白皮（SangbaiPi）中提取的 EtOAc 提取物增强了瞬时表达 GABA(A)受体亚基组成 α₁β₂γ(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。借助于第一批提取物的基于 HPLC 的活性分析，活性追踪到一个随后被鉴定为桑根酮 G（3）的峰。第二批具有不同的植物化学特征，基于 HPLC 的活性分析导致鉴定出桑根酮 C（4）和桑根酮 D（2）的立体异构体为阳性 GABA(A)受体调节剂。结构相关的化合物 kuwanon L（1）没有活性。桑根酮代表了一种新的阳性 GABA(A)受体调节剂支架。
