毛地黄黄酮和玄参黄酮抑制[~3H]地西泮和体外大鼠脑膜的结合(英文)

Inhibition of [methyl-3H]diazepam binding to rat brain membranes in vitro by dinatin and skrofulein

从阿拉伯艾蒿提取到两种苯并二氮杂受体的配基,毛地黄黄酮和玄参黄酮。两种化合物在体外可抑制[~3H]地西泮和大鼠皮层细胞膜的结合,IC_(50)值分别为1.3μmol·L^(-1)和23μmol·L^(-1)。两种化合物GABA比分别为1.1和1.2,都可少量增加[^(35)S]TBPS的结合,提示这种化合物是苯并二氮杂受体的拮抗剂或部分激动剂。

Two flavones, 4', 5, 7-trihy-droxy-6-methoxy flavone (dinatin) and 4', 5-dihydroxy-6, 7-dimethoxy flavone (skroful-ein) , were extracted from Artemisia herba alba L. Dinatin and skrofulein inhibited the binding of [methyl-3H]diazepam to rat brain membranes in vitro with IC50 of 1. 3 and 23 μmol ·L-1, respectively. The GABA-ratios (the ratio of IC50 values in the absence/presence of GABA in the binding assay) were 1. 1 and 1. 2 for dinatin and skrofulein, respectively. Both flavones induced a slight increase in [35 S ] TBPS binding. The data suggest that the flavones are antagonists or partial agonists of benzodiazepine receptors.