Wei Bo, Yang Zhong-Duo, Shi Dan-Feng, Yao Xiao-Jun, Wang Ming-Gang
School of Life Science and Engineering, Lanzhou University of Technology, Lanzhou 730050, PR China.
School of Life Science and Engineering, Lanzhou University of Technology, Lanzhou 730050, PR China.; Wenzhou Research Institute of Pump and Valve Engineering, Lanzhou University of Technology, Wenzhou 325105, PR China.
Iran J Pharm Res. 2016 Fall;15(4):885-892.
Seven stilbenes and one catechin were bioactivity-guidedly isolated from the rhizomes of . Their structures were identified as piceatannol (1), resveratrol (2), piceid (3), rhapontigenin (4), piceatannol-3-O-β-D-glucopyranoside (5), rhaponticin (6), catechin (7) and desoxyrhapontigenin (8). Anti-monoamine oxidase (MAO) activities of compounds 1-8 were tested. Compounds 1 and 8 showed significant MAO inhibitory activities with IC values 16.4 ± 1.5 μM and 11.5 ± 1.1, respectively, when the IC value of iproniazid as a standard was 6.5 ± 0.5 μM. The selectivity of compounds 1-8 against MAO-A and MAO-B were also evaluated. The results showed that compounds 4˴6˴8 preferred to inhibit MAO-A rather than MAO-B with selectivity values ([IC of MAO-B]/ [IC of MAO-A]) of 4.74, 10.01 and 9.42, respectively. The preliminary structure-activity relationships (SARs) of these compounds were discussed and the molecular modeling was also performed to explore the binding mode of inhibitors at the active site of MAO-A and MAO-B.
从……的根茎中通过生物活性导向法分离出七种芪类化合物和一种儿茶素。它们的结构被鉴定为白皮杉醇（1）、白藜芦醇（2）、白藜芦醇苷（3）、rhapontigenin（4）、白皮杉醇-3-O-β-D-吡喃葡萄糖苷（5）、rhaponticin（6）、儿茶素（7）和去氧rhapontigenin（8）。测试了化合物1-8的抗单胺氧化酶（MAO）活性。当作为标准的异烟肼的IC值为6.5±0.5μM时，化合物1和8显示出显著的MAO抑制活性，IC值分别为16.4±1.5μM和11.5±1.1。还评估了化合物1-8对MAO-A和MAO-B的选择性。结果表明，化合物4、6、8更倾向于抑制MAO-A而非MAO-B，选择性值（[MAO-B的IC值]/[MAO-A的IC值]）分别为4.74、10.01和9.42。讨论了这些化合物的初步构效关系（SARs），并进行了分子模拟以探索抑制剂在MAO-A和MAO-B活性位点的结合模式。
