McIlhenny Ethan H, Riba Jordi, Barbanoj Manel J, Strassman Rick, Barker Steven A
Department of Comparative Biomedical Sciences, School of Veterinary Medicine, Louisiana State University, Baton Rouge, LA 70803, USA.
Biomed Chromatogr. 2011 Sep;25(9):970-84. doi: 10.1002/bmc.1551. Epub 2010 Nov 5.
Ayahuasca, also known as caapi or yage among various South American groups, holds a highly esteemed and millennia-old position in these cultures' medical and religious pharmacopeia. There is now an increasing interest in the potential for modern medical applications of ayahuasca, as well as concerns regarding its increasing potential for abuse. Toxicological and clinical research to address these issues will require information regarding its metabolism and clearance. Thus, a rapid, sensitive and specific method for characterization and quantitation of the major constituents and of the metabolites of ayahuasca in urine is needed. The present research provides a protocol for conducting such analyses. The characteristics of the method, conducted by sample dilution and using HPLC-electrospray ionization (ESI)-selected reaction monitoring (SRM)-tandem mass spectrometry, are presented. The application of the analytical protocol to urine samples collected from three individuals that were administered ayahuasca has also been demonstrated. The data show that the major metabolite of the hallucinogenic component of ayahuasca, N,N-dimethyltryptamine (DMT), is the corresponding N-oxide, the first time this metabolite has been described in in vivo studies in humans. Further, very little DMT was detected in urine, despite the inhibition of monoamine oxidase afforded by the presence of the harmala alkaloids in ayahuasca. The major harmala alkaloid excreted was tetrahydroharmine. Other excretion products and metabolites were also identified and quantified. The method described would be suitable for use in further toxicological and clinical research on ayahuasca.
在南美洲的不同群体中，阿亚瓦斯卡（Ayahuasca）也被称为卡皮（caapi）或亚热（yage），在这些文化的医学和宗教药典中占据着备受尊崇且有着数千年历史的地位。如今，人们对阿亚瓦斯卡的现代医学应用潜力越来越感兴趣，同时也对其滥用可能性的增加感到担忧。针对这些问题的毒理学和临床研究将需要有关其代谢和清除的信息。因此，需要一种快速、灵敏且特异的方法来表征和定量尿液中阿亚瓦斯卡的主要成分及其代谢物。本研究提供了进行此类分析的方案。介绍了通过样品稀释并使用高效液相色谱 - 电喷雾电离（ESI） - 选择反应监测（SRM） - 串联质谱法进行的该方法的特点。还展示了该分析方案在从三名服用阿亚瓦斯卡的个体收集的尿液样本中的应用。数据表明，阿亚瓦斯卡致幻成分的主要代谢物N，N - 二甲基色胺（DMT）是相应的N - 氧化物，这是该代谢物首次在人体体内研究中被描述。此外，尽管阿亚瓦斯卡中存在的哈马兰生物碱抑制了单胺氧化酶，但在尿液中检测到的DMT非常少。排泄的主要哈马兰生物碱是四氢哈马明。还鉴定并定量了其他排泄产物和代谢物。所描述的方法将适用于进一步开展关于阿亚瓦斯卡的毒理学和临床研究。
