黄芩茎叶黄酮作为GABA_A受体BZD结合部位配体(英文)

Flavonoids of the stems and leaves of Scutellaria baicalensis Georgi as ligands of the GABA_A receptor benzodiazepine binding site

目的从黄芩地上部分中寻找活性成分。方法利用各种柱色谱 (硅胶、SephadexLH 2 0、D10 1大孔吸附树脂和聚酰胺 )分离黄芩地上部分的活性成分。结果从黄芩地上部分的水提取物中分离得到 7种黄酮类化合物。其中白杨素对GABAA 受体的BZD结合部位有较高的亲和力 ,其IC50 值为 0 6 7μmol/L。 7种黄酮类化合物亲和力的排列顺序为 :白杨素 >汉黄芩苷元 >红花素 >黄芩素 >5 ,6 ,7 三羟基 4′ 甲氧基黄酮 >异红花素 >白杨素 7 葡萄糖醛酸苷。

Aim To search for bioactive constituents of the aerial part of Scutellaria baicalensis Georgi.Methods Various column chromatography with silica gel,D 101 resin,Sephadex LH 20 and polyamide were employed for the isolation and purification of bioactive constituents.Results Seven flavonoids(wogonin,chrysin,5,6,7 trihydroxy 4′ methoxyflavone,carthamindin,isocarthamidin,scutellarein,chrysin 7 O β D glucuronide)were isolated from a water extract of the leaves of Scutellaria baicalensis Georgi.Among the isolated compounds,chrysin showed a high affinity to the benzodiazepine site of the GABA A receptor with an IC 50 value of 0 67 μmol/L.Based on binding to BZD S,the order of the affinity among these compounds was chrysin>wogonin>carthamidin>scutellarein>5,6,7 trihydroxy 4′ methoxyflavone>isocarthamidin>chrysin 7 O β D glucuronide.