Herrera-Ruiz Maribel, González-Cortazar Manasés, Jiménez-Ferrer Enrique, Zamilpa Alejandro, Alvarez Laura, Ramírez Guillermo, Tortoriello Jaime
Centro de Investigación Biomédica del Sur, Instituto Mexicano del Seguro Social, Argentina No. 1, Centro, 62790 Xochitepec, Morelos, México.
J Nat Prod. 2006 Jan;69(1):59-61. doi: 10.1021/np050305x.
The anxiolytic effects of galphimine B (1), galphimine A (2), and galphimine E (3), natural nor-secofriedelanes isolated from Galphimia glauca, as well as derivatives obtained by acetylation (4), hydrogenation of the C-1/C-2 double bond (5), basic hydrolysis followed by hydrogenation of the C-1/C-2 double bond (6), and deacetylation (7) of galphimine E (3), were evaluated on ICR mice exposed to the elevated plus-maze test. This study also included the evaluation of a galphimines-rich fraction (GRF) with a known concentration of 1-3, obtained from the dry leaves of G. glauca. Intraperitoneal administration of 15 mg/kg of 1, 2, 6, and GRF (1 h before testing) caused an anxiolytic-like effect in the animals, increasing significantly (p <0.001) the percentage of time of permanence and the number of crossings toward the open arms of the plus-maze. No activity was detected after administration of compounds 3, 4, 5, and 7. These results showed that GRF had activity similar to the most active pure galphimines (1 and 2) and that, like for the spasmolytic activity previously reported, the main determining factor responsible for the anxiolytic activity of the compounds was the presence of free hydroxyl groups at C-4, C-6, and C-7 and the presence of the double bond in the A ring.
对从光萼紫薇（Galphimia glauca）中分离得到的天然降羽扇豆烷类化合物galphimine B（1）、galphimine A（2）和galphimine E（3），以及通过对galphimine E（3）进行乙酰化（4）、C-1/C-2双键氢化（5）、碱性水解后再进行C-1/C-2双键氢化（6）和脱乙酰化（7）得到的衍生物，在接受高架十字迷宫试验的ICR小鼠上评估了它们的抗焦虑作用。本研究还包括对从光萼紫薇干叶中获得的已知浓度为1 - 3的富含galphimines的组分（GRF）进行评估。腹腔注射15 mg/kg的1、2、6和GRF（在测试前1小时）在动物身上产生了抗焦虑样作用，显著增加（p <0.001）了在十字迷宫开放臂上停留的时间百分比和穿越次数。给予化合物3、4、5和7后未检测到活性。这些结果表明，GRF具有与活性最强的纯galphimines（1和2）相似的活性，并且与先前报道的解痉活性一样，化合物抗焦虑活性的主要决定因素是C-4、C-6和C-7位存在游离羟基以及A环中存在双键。
