Department of Organic Chemistry, Faculty of Sciences, University Autónoma of Madrid, Madrid, Spain.
Department of Pharmacology, Pharmacognosy and Botany, Faculty of Pharmacy, University Complutense of Madrid, Madrid, Spain.
Planta Med. 2021 Apr;87(5):383-394. doi: 10.1055/a-1264-0572. Epub 2020 Oct 2.
commonly known as Mashua, is an herbal remedy used in traditional Andean medicine for the relief of kidney and bladder pain, as well as contusions. This study aimed to evaluate the fractions and isolated compounds from with analgesic activity mediated by the transient receptor potential vanilloid-1 receptor. A bioguided phytochemical analysis based on NMR/MS was performed to identify the compounds of the -heptane fractions from samples of purple tubers of . The transient receptor potential vanilloid-1 agonist and antagonist activity were assessed through the measurement of intracellular Ca in HEK001 cells. The chemical structure determination led to the identification of two alkamides: -(2-hydroxyethyl)--docosatetraenamide (1: ) and -oleoyldopamine (2: ). Both compounds induced increased intracellular calcium flow with IC values of 3.2 M and 7.9 M, respectively, thus activating the transient receptor potential vanilloid-1 receptor. Our research is the first report to show that these two compounds isolated from can act as agonists of the transient receptor potential vanilloid-1 receptor, providing scientific evidence for the traditional use of this species in pain relief.
通常被称为玛苏亚，是一种草药，用于传统的安第斯医学缓解肾脏和膀胱疼痛，以及挫伤。本研究旨在评估 的馏分和分离化合物，具有瞬时受体电位香草素 1 受体介导的镇痛活性。基于 NMR/MS 的生物导向植物化学分析用于鉴定从 的紫色块茎样品中 -庚烷馏分的化合物。瞬时受体电位香草素 1 激动剂和拮抗剂活性通过测量 HEK001 细胞中的细胞内 Ca 来评估。化学结构测定导致鉴定出两种酰胺：-(2-羟乙基)--二十二碳四烯酰胺（1：）和 -油酰多巴胺（2：）。这两种化合物都能诱导细胞内钙流增加，IC 值分别为 3.2 μM 和 7.9 μM，从而激活瞬时受体电位香草素 1 受体。我们的研究首次表明，从 中分离出的这两种化合物可以作为瞬时受体电位香草素 1 受体的激动剂，为该物种在缓解疼痛中的传统用途提供了科学依据。
