Larrazábal-Fuentes María José, Fernández-Galleguillos Carlos, Palma-Ramírez Jenifer, Romero-Parra Javier, Sepúlveda Kevin, Galetovic Alexandra, González Jorge, Paredes Adrián, Bórquez Jorge, Simirgiotis Mario J, Echeverría Javier
Unidad Alimentos, Departamento de Ciencias de los Alimentos y Nutrición, Facultad de Ciencias de la Salud, Universidad de Antofagasta, Antofagasta, Chile.
Instituto de Farmacia, Facultad de Ciencias, Universidad Austral de Chile, Valdivia, Chile.
Front Pharmacol. 2020 Dec 4;11:594174. doi: 10.3389/fphar.2020.594174. eCollection 2020.
Phil. (Asteraceae) (known as copa-copa) is a native species of Chile used as an infusion in traditional medicine by Atacameños people in the Altiplano, highlands of northern Chile. In this research, we have investigated for the first time the cholinesterase inhibition potential against acetylcholinesterase (AChE) and butyrylcholinesterase (BChE), and the chemical profiling of the infusions prepared from the aerial parts of by high resolution spectrometry. In addition, total phenolic, total flavonoid content, antioxidant (DPPH, FRAP, and ORAC) and antiprozoal activity were tested. showed good inhibitory activity against AChE and BChE (3.92 ± 0.08 µg/ml and 44.13 ± 0.10 µg/ml). The infusion displayed a total phenolics content of 155.6 ± 2.9 mg of gallic acid equivalents/g and total flavonoid content of 5.5 ± 0.2 mg quercetin equivalents/g. Additionally, trypanocidal activity against was found (LD of 131.8 µg/ml). Forty-seven metabolites were detected in the infusion of including several phenolic acids and flavonoids which were rapidly identified using ultrahigh performance liquid chromatography orbitrap mass spectrometry analysis (UHPLC-Orbitrap-MS) for chemical profiling. The major compounds identified in the infusions were studied by molecular docking against AChE and BChE. The UHPLC-MS fingerprints generated can be also used for the authentication of these endemic species. These findings reveal that infusions can be used as beverages with protective effects.
菲利草(菊科)(又称柯帕柯帕)是智利本土物种,智利北部高原的阿塔卡马人在传统医学中用其制作浸剂。在本研究中,我们首次研究了其对乙酰胆碱酯酶(AChE)和丁酰胆碱酯酶(BChE)的胆碱酯酶抑制潜力,以及通过高分辨率光谱法对该植物地上部分制备的浸剂进行化学剖析。此外,还测试了总酚含量、总黄酮含量、抗氧化活性(DPPH、FRAP和ORAC)以及抗原虫活性。结果表明,该植物对AChE和BChE具有良好的抑制活性(分别为3.92±0.08μg/ml和44.13±0.10μg/ml)。浸剂的总酚含量为155.6±2.9mg没食子酸当量/g,总黄酮含量为5.5±0.2mg槲皮素当量/g。此外,还发现其对克氏锥虫具有杀锥虫活性(半数致死剂量为131.8μg/ml)。在该植物浸剂中检测到47种代谢物,包括几种酚酸和黄酮类化合物,通过超高效液相色谱-轨道阱质谱分析(UHPLC-Orbitrap-MS)快速鉴定以进行化学剖析。通过分子对接研究了浸剂中鉴定出的主要化合物与AChE和BChE的相互作用。生成的UHPLC-MS指纹图谱也可用于这些特有物种的鉴定。这些发现表明,菲利草浸剂可作为具有保护作用的饮品。