Hou Wen-Chi, Lin Rong-Dih, Chen Cheng-Tang, Lee Mei-Hsien
Graduate Institute of Pharmacognosy, Taipei Medical University, 250 Wu-Hsing Street, Taipei 110, Taiwan.
J Ethnopharmacol. 2005 Aug 22;100(1-2):216-20. doi: 10.1016/j.jep.2005.03.017.
Attenuation of monoamine oxidase B (MAO-B) activity may provide protection against oxidative neurodegeneration. For this reason, inhibition of MAO-B activity is used as part of the treatment of Parkinson's and Alzheimer's patients. The hook of Uncaria rhynchophylla (Miq.) Jacks. (Rubiaceae) is a traditional Chinese herbal drug that is generally used to treat convulsive disorders. In this study, the fractionation and purification of Uncaria rhynchophylla extracts using a bioguided assay isolated two known compounds, (+)-catechin and (-)-epicatechin. The compounds inhibited MAO-B, as measured by an assay of rat brain MAO-B separated by electrophoresis on a 7.5% native polyacrylamide gel. The IC(50) values of (+)-catechin and (-)-epicatechin were 88.6 and 58.9 microM, respectively, and inhibition occurred in a dose-dependent manner, as measured by the fluorescence method. The Lineweaver-Burk plot revealed K(i) values for (+)-catechin and (-)-epicatechin of 74 and 21 microM, respectively. This suggests that these two compounds, isolated here for the first time from Uncaria rhynchophylla, might be able to protect against neurodegeneration in vitro, and, therefore, the molecular mechanism deserves further study. This finding may also increase interest in the health benefits of Uncaria rhynchophylla.
单胺氧化酶B(MAO - B)活性的减弱可能为氧化型神经退行性变提供保护。基于此,抑制MAO - B活性被用于帕金森病和阿尔茨海默病患者的部分治疗中。钩藤(茜草科)是一种传统的中草药,通常用于治疗惊厥性疾病。在本研究中,采用生物导向分析法对钩藤提取物进行分离纯化,分离出两种已知化合物,(+)-儿茶素和(-)-表儿茶素。通过在7.5%天然聚丙烯酰胺凝胶上进行电泳分离大鼠脑MAO - B的分析方法测定,这些化合物可抑制MAO - B。采用荧光法测定,(+)-儿茶素和(-)-表儿茶素的IC50值分别为88.6和58.9微摩尔,且抑制作用呈剂量依赖性。Lineweaver - Burk图显示,(+)-儿茶素和(-)-表儿茶素的K i值分别为74和21微摩尔。这表明,这两种首次从钩藤中分离出的化合物可能在体外具有预防神经退行性变的作用,因此,其分子机制值得进一步研究。这一发现也可能会增加人们对钩藤健康益处的关注。