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Identification of TRPV1 Ion Channels Agonists of Tropaeolum tuberosum in Human Skin Keratinocytes
Planta Medica ( IF 2.7 ) Pub Date : 2020-10-02 , DOI: 10.1055/a-1264-0572
Luis Apaza Ticona 1, 2 , Ángel Rumbero Sánchez 1 , Cristina Thiebaut Estrada 3 , Olga M Palomino 2
Affiliation  

Tropaeolum tuberosum, 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 T. tuberosum 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 n-heptane fractions from samples of purple tubers of T. tuberosum. The transient receptor potential vanilloid-1 agonist and antagonist activity were assessed through the measurement of intracellular Ca2+ in HEK001 cells. The chemical structure determination led to the identification of two alkamides: N-(2-hydroxyethyl)-7Z,10Z,13Z,16Z-docosatetraenamide (1: ) and N-oleoyldopamine (2: ). Both compounds induced increased intracellular calcium flow with IC50 values of 3.2 nM and 7.9 nM, respectively, thus activating the transient receptor potential vanilloid-1 receptor. Our research is the first report to show that these two compounds isolated from T. tuberosum 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.

中文翻译:

人皮肤角质形成细胞中马铃薯TRPV1离子通道激动剂的鉴定

Tropaeolum tuberosum,通常被称为 Mashua,是一种草药,用于传统的安第斯医学中,用于缓解肾脏和膀胱疼痛以及挫伤。本研究旨在评估具有由瞬时受体电位 vanilloid-1 受体介导的镇痛活性的马铃薯馏分和分离化合物。进行了基于 NMR/MS 的生物引导植物化学分析,以从马铃薯紫色块茎样品中鉴定正庚烷级分的化合物。通过测量 HEK001 细胞中的细胞内 Ca2+ 来评估瞬时受体电位 vanilloid-1 激动剂和拮抗剂的活性。化学结构测定导致鉴定出两种烷酰胺:N-(2-羟乙基)-7Z,10Z,13Z,16Z-二十二碳四烯酰胺 (1: ) 和 N-油酰多巴胺 (2: )。两种化合物均诱导细胞内钙流增加,IC50 值分别为 3.2 nM 和 7.9 nM,从而激活瞬时受体电位 vanilloid-1 受体。我们的研究是第一份报告表明从马铃薯中分离出的这两种化合物可以作为瞬时受体电位 vanilloid-1 受体的激动剂,为该物种在缓解疼痛中的传统用途提供科学证据。
更新日期:2020-10-02
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