从缬草中分离并鉴定出6-甲基芹菜素，一种脑γ-氨基丁酸A（GABA(A)）受体的竞争性配体。

Isolation and identification of 6-methylapigenin, a competitive ligand for the brain GABA(A) receptors, from Valeriana wallichii.

作者信息

Wasowski Cristina, Marder Mariel, Viola Haydeé, Medina Jorge Horacio, Paladini Alejandro Constantino

机构信息

Instituto de Química y Fisicoquímica Biológicas, Facultad de Farmacia y Bioquímica, Juín, Buenos Aires, Argentina.

出版信息

Planta Med. 2002 Oct;68(10):934-6. doi: 10.1055/s-2002-34936.

DOI:10.1055/s-2002-34936

PMID:12391561

Abstract

Using the guidance by a competitive assay for the benzodiazepine binding site in the GABA(A) receptor, active compounds were isolated from the rhizomes and roots of Valeriana wallichii DC. The UV, NMR and mass spectral data permitted the identification of 6-methylapigenin. This flavonoid has a Ki = 495 nM for the BDZ-bs and a GABA ratio of 1.6-2.0, which suggests possible agonistic properties. The calculated percentage of 6-methylapigenin in the crude drug is in the range: 0.013% to 0.0013%.

摘要

利用竞争性分析γ-氨基丁酸A（GABA(A)）受体中苯二氮䓬结合位点的指导方法，从缬草的根茎和根中分离出活性化合物。紫外、核磁共振和质谱数据确定该化合物为6-甲基芹菜素。这种黄酮类化合物对苯二氮䓬结合位点的抑制常数（Ki）为495 nM，GABA比值为1.6 - 2.0，表明其可能具有激动特性。计算得出该生药中6-甲基芹菜素的含量范围为0.013%至0.0013%。