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Alkylamides from Acmella oleracea: antinociceptive effect and molecular docking with cannabinoid and TRPV1 receptors
Natural Product Research ( IF 1.9 ) Pub Date : 2022-11-04 , DOI: 10.1080/14786419.2022.2142221
Raíssa M Kao Yien 1 , Anne Caroline C Gomes 2 , Rodolfo Goetze Fiorot 3 , Ana Luísa Palhares Miranda 1 , Gilda A Neves 4 , Brenda da Silva Andrade 4 , Fernanda N Costa 5 , Jorge Luiz Mendonça Tributino 4 , Naomi Kato Simas 1
Affiliation  

Abstract

Alkylamides are secondary metabolites in Acmella oleracea and display wide applications in treating several diseases. Since alkylamides can inhibit pain, this work aims to evaluate the antinociceptive profile of A. Oleracea methanolic extracts used in vivo and in silico assays. The extracts inhibited the neurogenic and inflammatory phases of the formalin test, ratifying the antinociceptive effect of alkylamides. Furthermore, the results from molecular docking demonstrated the interaction of A. oleracea alkylamides with the CB1/CB2 and TRPV1 receptors. Additionally, the crude methanolic extract of flowers did not induce potential side effects related to the classical cannabinoid tetrad: hypolocomotion and catalepsy. In conclusion, this work confirms the potential of the alkylamides of A. Oleracea as antinociceptive agents and, for the first time, correlates its effects with the endocannabinoid and vanilloid systems through in silico assays.



中文翻译:

来自 Acmella oleracea 的烷基酰胺:抗伤害作用以及与大麻素和 TRPV1 受体的分子对接

摘要

烷基酰胺是Acmella oleracea的次生代谢产物,在治疗多种疾病方面具有广泛的应用。由于烷基酰胺可以抑制疼痛,因此这项工作旨在评估苦苣菜甲醇提取物在体内计算机测定中的镇痛作用。这些提取物抑制了福尔马林试验的神经源性和炎症阶段,证实了烷基酰胺的抗伤害作用。此外,分子对接结果证明了甘蓝烷基酰胺与CB1/CB2和TRPV1受体的相互作用。此外,花的粗甲醇提取物不会引起与经典大麻素四联体相关的潜在副作用:运动减退和僵直症。总之,这项工作证实了甘蓝烷基酰胺作为抗伤害药的潜力,并首次通过计算机模拟分析将其作用与内源性大麻素和香草酸系统关联起来。

更新日期:2022-11-04
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