Mullally M, Cayer C, Muhammad A, Walshe-Roussel B, Ahmed F, Sanchez-Vindas P E, Otarola Rojas M, Merali Z, Cal V, Durst T, Trudeau V L, Arnason J T
Department of Biology, University of Ottawa, Ottawa, ON, K1N 6N5 Canada.
University of Ottawa Institute of Mental Health Research, University of Ottawa, Ottawa, ON, Canada; School of Psychology, University of Ottawa, Ottawa, ON, K1N 6N5 Canada.
J Ethnopharmacol. 2016 Jun 5;185:147-54. doi: 10.1016/j.jep.2016.03.013. Epub 2016 Mar 10.
The medicinal plant, Piper amalago L. (Piperaceae), is used traditionally by Q'eqchi' Maya healers for the treatment of "susto" a culture-bound syndrome. Previous research suggests that susto symptoms may be a manifestation of anxiety. The objectives were to characterize the effect of ethanolic extract of P. amalago in behavioral assays of anxiety at doses representative of traditional use and to isolate active principles.
Rats treated orally with low dose ethanolic extracts of P. amalago leaves (8-75mg/kg) were tested in several behavioral paradigms including the elevated plus maze (EPM), social interaction (SI), and conditioned emotional response (CER) tests, and compared to diazepam, a positive control. The active anxiolytic principle was isolated by bioassay guided isolation using an in vitro GABAA competitive binding assay.
Extracts had significant anxiolytic activity in all behavioral tests, with the strongest activity in the SI and the CER paradigms. In an in vitro GABAA competitive binding assay, a 66.5µg/mL concentration of P. amalago ethanol extract displaced 50% of the GABAA-BZD receptor ligand [(3)H]-Flunitrazepam. Bioassay-guided fractionation identified a furofuran lignan, a molecule with structural similarity to yangambin, with high affinity for the GABAA-BZD receptor as the principle bioactive.
The results suggest that the ethnobotanical use of this plant may have a pharmacological basis in its anxiolytic activity, as demonstrated in animal behaviour tests.
药用植物亚马拉胡椒（Piper amalago L.，胡椒科），被基切玛雅治疗师传统上用于治疗“魂惊症”，这是一种文化相关综合征。先前的研究表明，魂惊症症状可能是焦虑的一种表现。目的是在代表传统用药剂量的情况下，在焦虑行为试验中表征亚马拉胡椒乙醇提取物的作用，并分离出活性成分。
用低剂量亚马拉胡椒叶乙醇提取物（8 - 75mg/kg）口服处理的大鼠，在包括高架十字迷宫（EPM）、社交互动（SI）和条件性情绪反应（CER）测试等几种行为范式中进行测试，并与阳性对照地西泮进行比较。通过使用体外GABAA竞争性结合试验的生物测定指导分离法分离出活性抗焦虑成分。
提取物在所有行为测试中均具有显著的抗焦虑活性，在SI和CER范式中活性最强。在体外GABAA竞争性结合试验中，浓度为66.5μg/mL的亚马拉胡椒乙醇提取物取代了50%的GABAA - BZD受体配体[（3）H] - 氟硝西泮。生物测定指导的分级分离鉴定出一种呋喃呋喃木脂素，一种与洋甘菊素结构相似的分子，对GABAA - BZD受体具有高亲和力，为主要生物活性成分。
结果表明，这种植物的民族植物学用途可能在其抗焦虑活性方面具有药理学基础，如在动物行为测试中所证明的那样。
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