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亚马逊西帕鲁那提取物作为潜在的抗流感药物:代谢指纹图谱。

Amazonian Siparuna extracts as potential anti-influenza agents: Metabolic fingerprinting.

机构信息

Programa de Biotecnologia Vegetal e Bioprocessos (PBV), Universidade Federal do Rio de Janeiro, Rio de Janeiro, 21.941-902, Brazil; Instituto de Pesquisas de Produtos Naturais (IPPN), Universidade Federal do Rio de Janeiro, Rio de Janeiro, 21.941-902, Brazil.

Laboratório de Cromatografia e Espectrometria de Massas (LaCEM), Universidade Federal de Goiás, Goiânia, 74.690-900, Brazil.

出版信息

J Ethnopharmacol. 2021 Apr 24;270:113788. doi: 10.1016/j.jep.2021.113788. Epub 2021 Jan 8.

DOI:10.1016/j.jep.2021.113788
PMID:33429033
Abstract

ETHNOPHARMACOLOGICAL RELEVANCE

Siparuna species are used in Brazilian Folk Medicine for the treatment and prophylaxis of colds, fever, headache, gastrointestinal disorders and rheumatic pain.

AIM OF THE STUDY

This study aimed to investigate a possible anti-influenza activity of 25 extracts from leaves of Amazonian S. cristata, S. decipiens, S. glycycarpa, S. reginae and S. sarmentosa based on their folk medicinal uses as well as to investigate their metabolic fingerprinting. The chemical composition of the active extracts was further dereplicated.

MATERIAL AND METHODS

The chemical composition of the crude EtOH extracts from five Siparuna species were investigated by ESI (±) LC-QTOF-MS. Organic extracts were obtained by liquid-liquid partition with solvents of increasing polarity, generating 25 extracts which were subjected to a quick DI-ESI (±) IT-MS fingerprint analysis. These extracts were tested against influenza virus replication and cellular toxicity using MDCK cells and influenza A/Michigan/45/2015 (H1N1)pdm09 virus. The compounds in the active BuOH extracts from S. glycycarpa and S. sarmentosa were annotated by ESI (±) LC-QTOF-MS.

RESULTS

Analysis of the EtOH extracts revealed the presence of alkaloids and flavonoids, in the positive and negative ionization modes. Out of the 25 organic extracts screened for their antiviral activity, the BuOH extracts from S. glycycarpa and S. sarmentosa were the most active, inhibiting 96.0 ± 1.3% and 89.5 ± 0.8% of influenza virus replication 24 h post-infection. These inhibitory effects were maintained until 72hpi. Alkaloids, O- and C-flavonoid glycosides, dihydrochalcones and a procyanidin dimer were annotated in these extracts.

CONCLUSIONS

The inhibitory effect against influenza A(H1N1)pdm09 virus replication shown by Amazonian Siparuna species corroborates the use of these plants in Brazilian Folk Medicine, showing their potential as anti-influenza agents. These promising results stimulate the continuation of this study with the aim of isolating the compound(s) responsible for this bioactivity, thus contributing to a better knowledge of those species and to the research of natural products with potential anti-influenza activity.

摘要

民族药理学相关性

Siparuna 属植物在巴西民间医学中用于治疗和预防感冒、发热、头痛、胃肠疾病和风湿痛。

研究目的

本研究旨在基于亚马逊 Siparuna 属植物的民间药用用途,研究 25 种叶提取物对流感的潜在抗病毒活性,调查其代谢指纹图谱。进一步对活性提取物的化学成分进行去重复。

材料和方法

采用 ESI(+/-)LC-QTOF-MS 研究五种 Siparuna 属植物的粗 EtOH 提取物的化学成分。采用液液分配法用极性递增的溶剂提取有机提取物,生成 25 种提取物,对其进行快速 DI-ESI(+/-)IT-MS 指纹分析。用 MDCK 细胞和流感病毒 A/Michigan/45/2015(H1N1)pdm09 对这些提取物进行抗流感病毒复制和细胞毒性试验。通过 ESI(+/-)LC-QTOF-MS 对 S. glycycarpa 和 S. sarmentosa 的 BuOH 提取物中的化合物进行注释。

结果

分析 EtOH 提取物显示存在生物碱和类黄酮,在正、负离子模式下。在所筛选的 25 种具有抗病毒活性的有机提取物中,S. glycycarpa 和 S. sarmentosa 的 BuOH 提取物最为活跃,在感染后 24 小时抑制 96.0±1.3%和 89.5±0.8%的流感病毒复制。这些抑制作用持续到 72 小时。在这些提取物中注释了生物碱、O-和 C-类黄酮糖苷、二氢查耳酮和原花青素二聚体。

结论

亚马逊 Siparuna 属植物对甲型流感 A(H1N1)pdm09 病毒复制的抑制作用证实了这些植物在巴西民间医学中的应用,显示了它们作为抗流感药物的潜力。这些有希望的结果激发了继续进行这项研究的动力,目的是分离出负责这种生物活性的化合物,从而为更好地了解这些物种和研究具有抗流感活性的天然产物做出贡献。

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