Centro de Investigación Biomédica del Sur, Instituto Mexicano del Seguro Social (IMSS), Argentina No. 1, Col. Centro, CP 62790, Xochitepec, Morelos, Mexico.
J Ethnopharmacol. 2011 Sep 1;137(1):724-9. doi: 10.1016/j.jep.2011.06.029. Epub 2011 Jul 1.
Galphimine-B (G-B) is a nor-seco triterpene with an anxiolytic-like effect obtained from the plant species Galphimia glauca Cav. By means of a double blind clinical trial, it has been demonstrated that the extract from this plant, standardized in G-B content, possesses therapeutic effectiveness in patients with generalized anxiety. The mechanism of action of this compound remains unknown to date, but it has already demonstrated a non interaction with the γ-aminobutyric acid (GABA)ergic system. For this reason, the objective of this work was to evaluate the pharmacological interaction between G-B with the 5-hydroxytryptamine 1A (5HT(1A)) and 5-hydroxytryptamine 2A (5HT(2A)) serotonergic receptors on CA1 neurons of hippocampus.
Electrophysiological records were performed as the frequency of discharge of in vivo CA1 cells from dorsal hippocampus in rats.
G-B was able to increase the frequency of discharge of neurons of the CA1 cells with some characteristics that support an interaction with the serotonergic system in this zone. It was demonstrated that this triterpene modulates the induced response of 5HT(1A) receptors, in an allosteric manner.
This effect demonstrated an interaction between G-B and the serotonergic system in dorsal hippocampus and evidenced that the mechanism of action of this compound could involve a complex series of actions on different neurotransmitter systems related with the anxiety disorder.
Galphimine-B(G-B)是一种具有抗焦虑样作用的 nor-seco 三萜,从 Galphimia glauca Cav 植物中获得。通过双盲临床试验,已经证明该植物提取物,以 G-B 含量标准化,对广泛性焦虑症患者具有治疗效果。该化合物的作用机制至今尚不清楚,但已证明它与γ-氨基丁酸(GABA)能系统没有相互作用。出于这个原因,这项工作的目的是评估 G-B 与海马 CA1 神经元上的 5-羟色胺 1A(5HT(1A))和 5-羟色胺 2A(5HT(2A))血清素受体之间的药理相互作用。
电生理记录作为来自大鼠背侧海马 CA1 细胞的体内 CA1 细胞放电频率进行。
G-B 能够增加 CA1 细胞神经元的放电频率,具有一些支持该三萜在该区域与血清素系统相互作用的特征。证明该三萜以变构方式调节 5HT(1A)受体的诱导反应。
这种作用证明了 G-B 与背侧海马中的血清素系统之间的相互作用,并表明该化合物的作用机制可能涉及与焦虑症相关的不同神经递质系统的一系列复杂作用。