Hwang Ji-Sang, Lee Seon A, Hong Seong Su, Lee Kyong Soon, Lee Myung Koo, Hwang Bang Yeon, Ro Jai Seup
College of Pharmacy, Chungbuk National University, Cheongju 361-763, Korea.
Arch Pharm Res. 2005 Feb;28(2):190-4. doi: 10.1007/BF02977714.
In our search for monoamine oxidase (MAO) inhibitors from natural resources, we found that the methanol extract of the roots of Sophora flavescens showed an inhibitory effect on mouse brain monoamine oxidase (MAO). Bioactivity-guided isolation of the extract yielded two known flavonoids, formononetin (1) and kushenol F (2), as active compounds along with three inactive compounds, oxymatrine (3), trifolirhizin (4), and beta-sitosterol (5). Formononetin (1) and kushenol F (2) showed significant inhibitory effects on MAO in a dose-dependent manner with IC50 values of 13.2 and 69.9 microM, respectively. Formononetin (1) showed a slightly more potent inhibitory effect against MAO-B (IC50: 11.0 microM) than MAO-A (IC50: 21.2 microM). Kushenol F (2) also preferentially inhibited the MAO-B activity than MAO-A activity with the IC50 values of 63.1 and 103.7 microM, respectively.
在我们从自然资源中寻找单胺氧化酶(MAO)抑制剂的过程中,我们发现苦参根的甲醇提取物对小鼠脑单胺氧化酶(MAO)具有抑制作用。通过生物活性导向的提取物分离,得到了两种已知的黄酮类化合物,芒柄花黄素(1)和苦参醇F(2)作为活性化合物,以及三种无活性化合物,氧化苦参碱(3)、三叶豆紫檀苷(4)和β-谷甾醇(5)。芒柄花黄素(1)和苦参醇F(2)对MAO表现出显著的剂量依赖性抑制作用,IC50值分别为13.2和69.9 microM。芒柄花黄素(1)对MAO-B(IC50:11.0 microM)的抑制作用比对MAO-A(IC50:21.2 microM)稍强。苦参醇F(2)也优先抑制MAO-B活性而非MAO-A活性,IC50值分别为63.1和103.7 microM。